Sigma 1 Receptor Chaperone: Pharmacology and Therapeutic Perspectives

Therapeutic Targets: Modulation, Inhibition, and Activation

Volumn , Issue , 2012, Pages 225-278

  Zamanillo, Daniel ^a   Portillo Salido, Enrique ^a   Vela, José Miguel ^a   Romero, Luz ^a  

^a Drug Discovery and Preclinical Development   (Spain)

Author keywords

1 receptor pharmacological modulation, and cardiac effects; 1 receptor, a dynamic modulatory protein; Cellular effects modulated by 1 receptor; New potential therapeutic use of selective 1 receptor ligands; Sigma 1 receptor chaperone, pharmacology and therapeutic

Indexed keywords

EID: 84867375290     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1002/9781118185537.ch6     Document Type: Chapter

References (303)

1. Abou-Gharbia M, Ablordeppey SY, Glennon RA. Sigma receptors and their ligands: The sigma enigma. Annu Rep Med Chem 28:1-10 (1993).
2. Allahtavakoli M, Jarrott B. Sigma-1 receptor ligand PRE-084 reduced infarct volume, neurological deficits, pro-inflammatory cytokines and enhanced anti-inflammatory cytokines after embolic stroke in rats. Brain Res Bull 85:219-224 (2011).
3. Alonso G, Phan V, Guillemain I, Saunier M, Legrand A, Anoal M, Maurice T. Immunocytochemical localization of the sigma (1) receptor in the adult rat central nervous system. Neuroscience 97:155-170 (2000).
4. Antonini V, Marrazzo A, Kleiner G, Coradazzi M, Ronsisvalle S, Prezzavento O, Ronsisvalle G, Leanza G. Anti-amnesic and neuroprotective actions of the sigma-1 receptor agonist (-)-MR22 in rats with selective cholinergic lesion and amyloid infusion. J Alzheimer's Dis 24:569-586 (2011).
5. Ault DT, Radeff JM,Werling LL. Modulation of [3H]dopamine release from rat nucleus accumbens by neuropeptide Y may involve a sigma1-like receptor. J Pharmacol Exp Ther 284:553-560 (1998).
6. Ault DT, Werling LL. Differential modulation of NMDA-stimulated [3H]dopamine release from rat striatum by neuropeptide Y and sigma receptor ligands. Brain Res 760:210-217 (1997).
7. Ault DT, Werling LL. Neuropeptide Y-mediated enhancement of NMDA-stimulated [3H]dopamine release from rat prefrontal cortex is reversed by sigma1 receptor antagonists. Schizophr Res 31:27-36 (1998).
8. Ault DT, Werling LL. SH-SY5Y cells as a model for sigma receptor regulation of potassium-stimulated dopamine release. Brain Res 877:354-360 (2000).
9. Aydar E, Palmer CP, Djamgoz MB. Sigma receptors and cancer: Possible involvement of ion channels. Cancer Res 64:5029-5035 (2004).
10. Aydar E, Palmer CP, Klyachko VA, Jackson MB. The sigma receptor as a ligandregulated auxiliary potassium channel subunit. Neuron 34:399-410 (2002).
11. Bebarova M, Matejovic P, Pasek M, Novakova M. Effect of haloperidol on transient outward potassium current in rat ventricular myocytes. Eur J Pharmacol 550:15-23 (2006).
12. Beckett S. E-5842 (Laboratories Dr Esteve). IDrugs 3:666-668 (2000).
13. Bergeron R, De Montigny C, Debonnel G. Biphasic effects of sigma ligands on the neuronal response to N-methyl-D-aspartate. Naunyn Schmiedebergs Arch Pharmacol 351:252-260 (1995).
14. Bergeron R, De Montigny C, Debonnel G. Effect of short-term and long-term treatments with sigma ligands on the N-methyl-D-aspartate response in the CA3 region of the rat dorsal hippocampus. Br J Pharmacol 120:1351-1359 (1997).
15. Bergeron R, De Montigny C, Debonnel G. Potentiation of neuronal NMDA response induced by dehydroepiandrosterone and its suppression by progesterone: Effects mediated via sigma receptors. J Neurosci 16:1193-1202 (1996).
16. Bergeron R, De Montigny C, Debonnel G. Pregnancy reduces brain sigma receptor function. Br J Pharmacol 127:1769-1776 (1999).
17. Bergeron R, Debonnel G, De Montigny C. Modification of the N-methyl-D-aspartate response by antidepressant sigma receptor ligands. Eur J Pharmacol 240:319-323 (1993).
18. Bergeron R, Debonnel G. Effects of low and high doses of selective sigma ligands: Further evidence suggesting the existence of different subtypes of sigma receptors. Psychopharmacology (Berl) 129:215-224 (1997).
19. Bermack J, Lavoie N, Dryver E, Debonnel G. Effects of sigma ligands on NMDA receptor function in the bulbectomy model of depression: A behavioural study in the rat. Int J Neuropsychopharmacol 5:53-62 (2002).
20. Bermack JE, Debonnel G. Distinct modulatory roles of sigma receptor subtypes on glutamatergic responses in the dorsal hippocampus. Synapse 55:37-44 (2005).
21. Bermack JE, Debonnel G. Effects of OPC-14523, a combined sigma and 5-HT1a ligand, on pre- and post-synaptic 5-HT1a receptors. J Psychopharmacol 21:85-92 (2007).
22. Bermack JE, Debonnel G. Modulation of serotonergic neurotransmission by short- and long-term treatments with sigma ligands. Br J Pharmacol 134:691-699 (2001).
23. Bermack JE, Debonnel G. The role of sigma receptors in depression. J Pharmacol Sci 97:317-336 (2005).
24. Bermack JE, Haddjeri N, Debonnel G. Effects of the potential antidepressant OPC- 14523 [1-[3-[4- (3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3, 4-dihydro-2-qu inolinone monomethanesulfonate] a combined sigma and 5-HT1A ligand: Modulation of neuronal activity in the dorsal raphe nucleus. J Pharmacol Exp Ther 310:578-583 (2004).
25. Bhuiyan MS, Fukunaga K. Stimulation of sigma-1 receptor signaling by dehydroepiandrosterone ameliorates pressure overload-induced hypertrophy and dysfunctions in ovariectomized rats. Expert Opin Ther Targets 13:1253-1265 (2009).
26. Bhuiyan MS, Fukunaga K. Targeting sigma-1 receptor signaling by endogenous ligands for cardioprotection. Expert Opin Ther Targets 15:145-155 (2011).
27. Bhuiyan MS, Tagashira H, Fukunaga K. Dehydroepiandrosterone-mediated stimulation of sigma-1 receptor activates Akt-eNOS signaling in the thoracic aorta of ovariectomized rats with abdominal aortic banding. Cardiovasc Ther 29:219-230 (2010).
28. Bhuiyan MS, Tagashira H, Fukunaga K. Sigma-1 receptor stimulation with fluvoxamine activates Akt-eNOS signaling in the thoracic aorta of ovariectomized rats with abdominal aortic banding. Eur J Pharmacol 650:621-628 (2011).
29. Borison RL, Diamond BI, Dren AT. Does sigma receptor antagonism predict clinical antipsychotic efficacy? Psychopharmacol Bull 27:103-106 (1991).
30. Bouchard P, Maurice T, St Pierre S, Privat A, Quirion R. Neuropeptide Y and the calcitonin gene-related peptide attenuate learning impairments induced by MK-801 via a sigma receptor-related mechanism. Eur J Neurosci 9:2142-2151 (1997).
31. Bouchard P, Monnet F, Bergeron R, Roman F, Junien JL, De Montigny C, Debonnel G, Quirion R. In vivo modulation of sigma receptor sites by calcitonin gene-related peptide in the mouse and rat hippocampal formation: Radioligand binding and electrophysiological studies. Eur J Neurosci 7:1952-1962 (1995).
32. Bourrie B, Bribes E, De Nys N, Esclangon M, Garcia L, Galiegue S, Lair P, Paul R, Thomas C, Vernieres JC, Casellas P. SSR125329A, a high affinity sigma receptor ligand with potent anti-inflammatory properties. Eur J Pharmacol 456:123-131 (2002).
33. Bowen WD, Tolentino PJ, Kirschner BN, Varghese P, de Costa BR, Rice KC. Sigma receptors and signal transduction: Negative modulation of signaling through phosphoinositide- linked receptor systems. NIDA Res Monogr 133:69-93 (1993).
34. Brammer MK, Gilmore DL, Matsumoto RR. Interactions between 3, 4-methylenedioxymethamphetamine and sigma1 receptors. Eur J Pharmacol 553:141-145 (2006).
35. Bubenikova-Valesova V, Horacek J, Vrajova M, Hoschl C. Models of schizophrenia in humans and animals based on inhibition of NMDA receptors. Neurosci Biobehav Rev 32:1014-1023 (2008).
36. Calderon SN, Izenwasser S, Heller B, Gutkind JS, Mattson MV, Su TP, Newman AH. Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. J Med Chem 37:2285-2291 (1994).
37. Carnally SM, Johannessen M, Henderson RM, Jackson MB, Edwardson JM. Demonstration of a direct interaction between sigma-1 receptors and acid-sensing ion channels. Biophys J 98:1182-1191 (2010).
38. Cendan CM, Pujalte JM, Portillo-Salido E, Baeyens JM. Antinociceptive effects of haloperidol and its metabolites in the formalin test in mice. Psychopharmacology (Berl) 182:485-493, (2005).
39. Cendan CM, Pujalte JM, Portillo-Salido E, Montoliu L, Baeyens JM. Formalin-induced pain is reduced in sigma (1) receptor knockout mice. Eur J Pharmacol 511:73-74, (2005).
40. Chaki S, Okuyama S, Ogawa S, Tanaka M, Muramatsu M, Nakazato A, Tomisawa K. Solubilization and characterization of binding sites for [3H]NE-100, a novel and potent sigma 1 ligand, from guinea pig brain. Life Sci 59:1331-1340 (1996).
41. Chen HS, Lipton SA. The chemical biology of clinically tolerated NMDA receptor antagonists. J Neurochem 97:1611-1626 (2006).
42. Cheng ZX, Lan DM, Wu PY, Zhu YH, Dong Y, Ma L, Zheng P. Neurosteroid dehydroepiandrosterone sulphate inhibits persistent sodium currents in rat medial prefrontal cortex via activation of sigma-1 receptors. Exp Neurol 210:128-136 (2008).
43. Chien CC, Pasternak GW. (-)-Pentazocine analgesia in mice: Interactions with a sigma receptor system. Eur J Pharmacol 294:303-308 (1995).
44. Chien CC, Pasternak GW. Functional antagonism of morphine analgesia by (+)-pentazocine: evidence for an anti-opioid sigma 1 system. Eur J Pharmacol 250:R7-R8 (1993).
45. Chien CC, Pasternak GW. Selective antagonism of opioid analgesia by a sigma system. J Pharmacol Exp Ther 271:1583-1590 (1994).
46. Chien CC, Pasternak GW. Sigma antagonists potentiate opioid analgesia in rats. Neurosci Lett 190:137-139 (1995).
47. Chou YC, Liao JF, Chang WY, Lin MF, Chen CF. Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan. Brain Res 821:516-519 (1999).
48. Chouinard G, Annable L. An early phase II clinical trial of BW234U in the treatment of acute schizophrenia in newly admitted patients. Psychopharmacology (Berl) 84:282- 284 (1984).
49. Cobos EJ, Baeyens JM, Del Pozo E. Phenytoin differentially modulates the affinity of agonist and antagonist ligands for sigma 1 receptors of guinea pig brain. Synapse 55:192-195 (2005).
50. Cobos EJ, Entrena JM, Nieto FR, Cendan CM, Del Pozo E. Pharmacology and therapeutic potential of sigma (1) receptor ligands. Curr Neuropharmacol 6:344-366 (2008).
51. Cobos EJ, Lucena G, Baeyens JM, Del Pozo E. Differences in the allosteric modulation by phenytoin of the binding properties of the sigma1 ligands [3H] (+)-pentazocine and [3H]NE-100. Synapse 59:152-161 (2006).
52. Collier TL, Waterhouse RN, Kassiou M. Imaging sigma receptors: Applications in drug development. Curr Pharm Desing 13:51-72 (2007).
53. Contreras PC, Quirion R, Gehlert DR, Contreras ML, O'Donohue TL. Autoradiographic distribution of non-dopaminergic binding sites labeled by [3H]haloperidol in rat brain. Neurosci Lett 75:133-140 (1987).
54. Cottraux J, Mollard E, Bouvard M, Marks I. Exposure therapy, fluvoxamine, or combination treatment in obsessive-compulsive disorder: One-year followup. Psychiatry Res 49:63-75 (1993).
55. Dahmen N, Fischer V, Hodl P, Rujescu D, Reuss S, Bartoszyk GD, Hiemke C. Induction of c-fos gene expression by the selective sigma receptor ligand EMD 57445 in rat brain. Eur Neuropsychopharmacol 6:237-243 (1996).
56. Davidson J, Miller R, Wingfield M, Zung W, Dren AT. The first clinical study of BW- 234U in schizophrenia. Psychopharmacol Bull 18:173-176 (1982).
57. de la Puente B, Nadal X, Portillo-Salido E, Sanchez-Arroyos R, Ovalle S, Palacios G, Muro A, Romero L, Entrena JM, Baeyens JM, Lopez-Garcia JA, Maldonado R, Zamanillo D, Vela JM. Sigma-1 receptors regulate activity-induced spinal sensitization and neuropathic pain after peripheral nerve injury. Pain 145:294-303 (2009).
58. De Montigny C, Monnet FP, Fournier A, Debonnel G. Sigma ligands and neuropeptide Y selectively potentiate the NMDA response in the rat CA3 dorsal hippocampus: In vivo electrophysiological studies. Clin Neuropharmacol 15 (Suppl 1, Pt A):145A-146A (1992).
59. Debonnel G, De Montigny C. Modulation of NMDA and dopaminergic neurotransmissions by sigma ligands: Possible implications for the treatment of psychiatric disorders. Life Sci 58:721-734 (1996).
60. DeHaven-Hudkins DL, Ford-Rice FY, Allen JT, Hudkins RL. Allosteric modulation of ligand binding to [3H] (+)pentazocine-defined sigma recognition sites by phenytoin. Life Sci 53:41-48 (1993).
61. Dhir A, Kulkarni S. Involvement of sigma (sigma1) receptors in modulating the antidepressant effect of neurosteroids (dehydroepiandrosterone or pregnenolone) in mouse tail-suspension test. J Psychopharmacol 22:691-696 (2008).
62. Dhir A, Kulkarni SK. Involvement of sigma-1 receptor modulation in the antidepressant action of venlafaxine. Neurosci Lett 420:204-208 (2007).
63. Diaz JL, Zamanillo D, Corbera J, Baeyens JM, Maldonado R, Pericas MA, Vela JM, Torrens A. Selective sigma-1 (sigma1) receptor antagonists: Emerging target for the treatment of neuropathic pain. Cent Nerv Syst Agents Med Chem 9:172-183 (2009).
64. Ding YS, Fowler JS, Dewey SL, Wolf AP, Logan J, Gatley SJ, Volkow ND, Shea C, Taylor DP. Synthesis and PET studies of fluorine-18-BMY 14802: A potential antipsychotic drug. J Nucl Med 34:246-254 (1993).
65. Dong LY, Cheng ZX, Fu YM, Wang ZM, Zhu YH, Sun JL, Dong Y, Zheng P. Neurosteroid dehydroepiandrosterone sulfate enhances spontaneous glutamate release in rat prelimbic cortex through activation of dopamine D1 and sigma-1 receptor. Neuropharmacology 52:966-974 (2007).
66. Drews E, Zimmer A. Central sensitization needs sigma receptors. Pain 145:269-270 (2009).
67. Egashira N, Harada S, Okuno R, Matsushita M, Nishimura R, Mishima K, Iwasaki K, Orito K, Fujiwara M. Involvement of the sigma1 receptor in inhibiting activity of fluvoxamine on marble-burying behavior: Comparison with paroxetine. Eur J Pharmacol 563:149-154 (2007).
68. Entrena JM, Cobos EJ, Nieto FR, Cendan CM, Baeyens JM, Del Pozo E. Antagonism by haloperidol and its metabolites of mechanical hypersensitivity induced by intraplantar capsaicininmice:Roleof sigma-1receptors.Psychopharmacology (Berl)205:21-33(2009).
69. Entrena JM, Cobos EJ, Nieto FR, Cendan CM, Gris G, Del Pozo E, Zamanillo D, Baeyens JM. Sigma-1 receptors are essential for capsaicin-induced mechanical hypersensitivity: Studies with selective sigma-1 ligands and sigma-1 knockout mice. Pain 143:252-261 (2009).
70. Ferris RM, Tang FL, Chang KJ, Russell A. Evidence that the potential antipsychotic agent rimcazole (BW 234U) is a specific, competitive antagonist of sigma sites in brain. Life Sci 38:2329-2337 (1986).
71. Fleckenstein AE, Volz TJ, Riddle EL, Gibb JW, Hanson GR. New insights into the mechanism of action of amphetamines. Annu Rev Pharmacol Toxicol 47:681-698 (2007).
72. Fontanilla D, Johannessen M, Hajipour AR, Cozzi NV, Jackson MB, Ruoho AE. The hallucinogen N, N-dimethyltryptamine (DMT) is an endogenous sigma-1 receptor regulator. Science 323:934-937 (2009).
73. Frieboes RM, Murck H, Antonijevic I, Kraus T, Hinze-Selch D, Pollmacher T, Steiger A. Characterization of the sigma ligand panamesine, a potential antipsychotic, by immune response in patients with schizophrenia and by sleep-EEG changes in normal controls. Psychopharmacology (Berl) 141:107-110 (1999).
74. Frieboes RM, Murck H,Wiedemann K, Holsboer F, Steiger A. Open clinical trial on the sigma ligand panamesine in patients with schizophrenia. Psychopharmacology (Berl) 132:82-88 (1997).
75. Fritz M, Klement S, El Rawas R, Saria A, Zernig G. Sigma1 receptor antagonist BD1047 enhances reversal of conditioned place preference from cocaine to social interaction. Pharmacology 87:45-48 (2011).
76. Fu Y, Zhao Y, Luan W, Dong LY, Dong Y, Lai B, Zhu Y, Zheng P. Sigma-1 receptors amplify dopamine D1 receptor signaling at presynaptic sites in the prelimbic cortex. Biochim Biophys Acta 1803:1396-408 (2010).
77. Garces-Ramirez L, Green JL, Hiranita T, Kopajtic TA, Mereu M, Thomas AM, Mesangeau C, Narayanan S, McCurdy CR, Katz JL, Tanda G. Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis. Biol Psychiatry 69:208-217 (2011).
78. Gerlach K, Uhlig T, Plathof J, Klassen A, Stoll KD, Schmucker P, Hueppe M. Effects of opipramol as an evening anaesthesiologic premedication. Neuropsychobiology 46:161-166 (2002).
79. Gewirtz GR, Gorman JM, Volavka J, Macaluso J, Gribkoff G, Taylor DP, Borison R. BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology 10:37-40 (1994).
80. Gilmore DL, Liu Y, Matsumoto RR. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Rev 10:1-22 (2004).
81. Gonzalez GM, Werling LL. Release of [3H]dopamine from guinea pig striatal slices is modulated by sigma1 receptor agonists. Naunyn Schmiedebergs Arch Pharmacol 356:455-461 (1997).
82. Gonzalez-Alvear GM, Werling LL. Sigma1 receptors in rat striatum regulate NMDAstimulated [3H]dopamine release via a presynaptic mechanism. Eur J Pharmacol 294:713-719 (1995).
83. Goyagi T, Goto S, Bhardwaj A, Dawson VL, Hurn PD, KirschJr., Neuroprotective effect of sigma (1)-receptor ligand 4-phenyl-1- (4-phenylbutyl) piperidine (PPBP) is linked to reduced neuronal nitric oxide production. Stroke 32:1613-1620 (2001).
84. Green AR, Mechan AO, Elliott JM, O'Shea E, Colado MI. The pharmacology and clinical pharmacology of 3,4-methylenedioxymethamphetamine (MDMA, "ecstasy"). Pharmacol Rev 55:463-508 (2003).
85. Grunder G, Muller MJ, Andreas J, Heydari N,Wetzel H, Schlosser R, Schlegel S, Nickel O, Eissner D, Benkert O. Occupancy of striatal D (2)-like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic. Psychopharmacology (Berl) 146:81-86 (1999).
86. Guitart X, Codony X, Monroy X. Sigma receptors: Biology and therapeutic potential. Psychopharmacology (Berl) 174:301-319 (2004).
87. Guitart X, Farre AJ. The effect of E-5842, a sigma receptor ligand and potential atypical antipsychotic, on Fos expression in rat forebrain. Eur J Pharmacol 363:127-130 (1998).
88. Guzman-Lenis MS, Navarro X, Casas C. Selective sigma receptor agonist 2- (4- morpholinethyl)1-phenylcyclohexanecarboxylate (PRE084) promotes neuroprotection and neurite elongation through protein kinase C (PKC) signaling on motoneurons. Neuroscience 162:31-38 (2009).
89. Hanner M, Moebius FF, Flandorfer A, Knaus HG, Striessnig J, Kempner E, Glossmann H. Purification, molecular cloning, and expression of the mammalian sigma1-binding site. Proc Natl Acad Sci USA 93:8072-8077 (1996).
90. Harada Y, Hara H, Sukamoto T. Characterization of specific (+)-[3H]N-allylnormetazocine and [3H]1, 3-di (2-tolyl)guanidine binding sites in porcine gastric fundic mucosa. J Pharmacol Exp Ther 269:905-910 (1994).
91. Hashimoto K, Fujita Y, Iyo M. Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of fluvoxamine: role of sigma-1 receptors. Neuropsychopharmacology 32:514-521 (2007).
92. Hashimoto K, Ishiwata K. Sigma receptor ligands: possible application as therapeutic drugs and as radiopharmaceuticals. Curr Pharm Design 12:3857-3876 (2006).
93. Hashimoto K, London ED. Interactions of erythro-ifenprodil, threo-ifenprodil, erythroiodoifenprodil, and eliprodil with subtypes of sigma receptors. Eur J Pharmacol 273:307-310 (1995).
94. Hayashi T, Justinova Z, Hayashi E, Cormaci G, Mori T, Tsai SY, Barnes C, Goldberg SR, Su TP. Regulation of sigma-1 receptors and endoplasmic reticulum chaperones in the brain of methamphetamine self-administering rats. J Pharmacol Exp Ther 332:1054-1063 (2010).
95. Hayashi T, Maurice T, Su TP. Ca (2+) signaling via sigma (1)-receptors: Novel regulatory mechanism affecting intracellular Ca (2+) concentration. J Pharmacol Exp Ther 293:788-798 (2000).
96. Hayashi T, Su T. The sigma receptor: Evolution of the concept in neuropsychopharmacology. Curr Neuropharmacol 3:267-280 (2005).
97. Hayashi T, Su TP. An update on the development of drugs for neuropsychiatric disorders: Focusing on the sigma 1 receptor ligand. Expert Opin Ther Targets 12:45-58 (2008).
98. Hayashi T, Su TP. Cholesterol at the endoplasmic reticulum: Roles of the sigma-1 receptor chaperone and implications thereof in human diseases. Subcell Biochem 51:381-398 (2010).
99. Hayashi T, Su TP. Intracellular dynamics of sigma-1 receptors (sigma (1) binding sites) in NG108-15 cells. J Pharmacol Exp Ther 306:726-733 (2003).
100. Hayashi T, Su TP. Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca (2+) signaling and cell survival. Cell 131:596-610 (2007).
101. Hayashi T, Su TP. Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs 18:269-284 (2004).
102. Hayashi T, Su TP. The potential role of sigma-1 receptors in lipid transport and lipid raft reconstitution in the brain: Implication for drug abuse. Life Sci 77:1612-1624 (2005).
103. Hayashi T, Tsai SY, Mori T, Fujimoto M, Su TP. Targeting ligand-operated chaperone sigma-1 receptors in the treatment of neuropsychiatric disorders. Expert Opin Ther Targets 15:557-577 (2011).
104. Hellewell SB, Bowen WD. A sigma-like binding site in rat pheochromocytoma (PC12) cells: Decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain. Brain Res 527:244-253 (1990).
105. Hellewell SB, Bruce A, Feinstein G, Orringer J, Williams W, Bowen WD. Rat liver and kidney contain high densities of sigma 1 and sigma 2 receptors: Characterization by ligand binding and photoaffinity labeling. Eur J Pharmacol 268:9-18 (1994).
106. Hofner G, Wanner KT. [3H]ifenprodil binding to NMDA receptors in porcine hippocampal brain membranes. Eur J Pharmacol 394:211-219 (2000).
107. Hohagen F, Winkelmann G, Rasche-Ruchle H, Hand I, Konig A, Munchau N, Hiss H, Geiger-Kabisch C, Kappler C, Schramm P, Rey E, Aldenhoff J, Berger M. Combination of behaviour therapy with fluvoxamine in comparison with behaviour therapy and placebo. Results of a multicentre study. Br J Psychiatry Suppl 71-78 (1998).
108. HongW, Nuwayhid SJ,Werling LL. Modulation of bradykinin-induced calcium changes in SH-SY5Y cells by neurosteroids and sigma receptor ligands via a shared mechanism. Synapse 54:102-110 (2004).
109. Huber MT, Gotthardt U, SchreiberW, Krieg JC. Efficacy and safety of the sigma receptor ligand EMD 57445 (panamesine) in patients with schizophrenia: An open clinical trial. Pharmacopsychiatry 32:68-72 (1999).
110. Irons J. Fluvoxamine in the treatment of anxiety disorders. Neuropsychiatr Dis Treat 1:289-299 (2005).
111. Ishiguro H, Ohtsuki T, Toru M, Itokawa M, Aoki J, Shibuya H, Kurumaji A, Okubo Y, Iwawaki A, Ota K, Shimizu H, Hamaguchi H, Arinami T. Association between polymorphisms in the type 1 sigma receptor gene and schizophrenia. Neurosci Lett 257:45-48 (1998).
112. Itzhak Y, Stein I, Zhang SH, Kassim CO, Cristante D. Binding of sigma-ligands to C57BL/6 mouse brain membranes: Effects of monoamine oxidase inhibitors and subcellular distribution studies suggest the existence of sigma-receptor subtypes. J Pharmacol Exp Ther 257:141-148 (1991).
113. Jaen JC, Caprathe BW, Pugsley TA,Wise LD, Akunne H. Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors. J Med Chem 36:3929-3936 (1993).
114. Johannessen M, Fontanilla D, Mavlyutov T, Ruoho AE, Jackson MB. Antagonist action of progesterone at sigma-receptors in the modulation of voltage-gated sodium channels. Am J Physiol Cell Physiol 300:C328-C337 (2011).
115. Johannessen M, Ramachandran S, Riemer L, Ramos-Serrano A, Ruoho AE, Jackson MB. Voltage-gated sodium channel modulation by sigma-receptors in cardiac myocytes and heterologous systems. Am J Physiol Cell Physiol 296:C1049-C1057 (2009).
116. Junien JL, Roman FJ, Brunelle G, Pascaud X. JO1784, a novel sigma ligand, potentiates [3H]acetylcholine release from rat hippocampal slices. Eur J Pharmacol 200:343-345 (1991).
117. Kalia LV, Kalia SK, SalterMW. NMDA receptors in clinical neurology: Excitatory times ahead. Lancet Neurol 7:742-755 (2008).
118. Kamei H, Kameyama T, Nabeshima T. (+)-SKF-10, 047 and dextromethorphan ameliorate conditioned fear stress via dopaminergic systems linked to phenytoinregulated sigma 1 sites. Eur J Pharmacol 309:149-158 (1996).
119. Kamei H, Noda Y, Kameyama T, Nabeshima T. Role of (+)-SKF-10, 047-sensitive subpopulation of sigma 1 receptors in amelioration of conditioned fear stress in rats: association with mesolimbic dopaminergic systems. Eur J Pharmacol 319:165-172 (1997).
120. Kanzaki A, Okumura K, Ujike H, Tsuchida K, Akiyama K, Otsuki S. BMY-14802 reverses the reduction of striatal dopamine release induced by (+)-3-[3-hydroxyphenyl]- N- (1-propyl)piperidine. J Neur Transm Gen Sect 90:137-144 (1992).
121. Kashiwagi H, McDunn JE, Simon PO Jr, Goedegebuure PS, Vangveravong S, Chang K, Hotchkiss RS, Mach RH, Hawkins WG. Sigma-2 receptor ligands potentiate conventional chemotherapies and improve survival in models of pancreatic adenocarcinoma. J Transl Med 7:24 (2009).
122. Kast RE. Glioblastoma: Looking at the currently marketed sigma-1 agonists and antagonists. Neoplasia 9:689 (2007).
123. Kato K, Hayako H, Ishihara Y, Marui S, Iwane M, Miyamoto M. TAK-147, an acetylcholinesterase inhibitor, increases choline acetyltransferase activity in cultured rat septal cholinergic neurons. Neurosci Lett 260:5-8 (1999).
124. Kawasaki Y, Kohno T, Zhuang ZY, Brenner GJ, Wang H, Van Der MC, Befort K, Woolf CJ, Ji RR. Ionotropic and metabotropic receptors, protein kinase A, protein kinase C, and Src contribute to C-fiber-induced ERK activation and cAMP response element-binding protein phosphorylation in dorsal horn neurons, leading to central sensitization. J Neurosci 24:8310-8321 (2004).
125. Kedjouar B, Daunes S, Vilner BJ, Bowen WD, Klaebe A, Faye JC, Poirot M. Structural similitudes between cytotoxic antiestrogen-binding site (AEBS) ligands and cytotoxic sigma receptor ligands. Evidence for a relationship between cytotoxicity and affinity for AEBS or sigma-2 receptor but not for sigma-1 receptor. Biochem Pharmacol 58:1927-1939 (1999).
126. Kim FJ, Kovalyshyn I, Burgman M, Neilan C, Chien CC, Pasternak GW. Sigma 1 receptor modulation of G-protein-coupled receptor signaling: Potentiation of opioid transduction independent from receptor binding. Mol Pharmacol 77:695-703 (2010).
127. KimHW, Kwon YB, Roh DH, Yoon SY, Han HJ, KimKW, Beitz AJ, Lee JH. Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice. Br J Pharmacol 148:490-498 (2006).
128. Kim HW, Roh DH, Yoon SY, Seo HS, Kwon YB, Han HJ, Kim KW, Beitz AJ, Lee JH. Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKCand PKA-dependent phosphorylation of the NR1 subunit in mice. Br J Pharmacol 154:1125-1134 (2008).
129. King M, Pan YX, Mei J, Chang A, Xu J, Pasternak GW. Enhanced kappa-opioid receptor-mediated analgesia by antisense targeting the sigma1 receptor. Eur J Pharmacol 331:R5-R6 (1997).
130. Kobayashi T, Matsuno K, Mita S. Regional differences of the effect of sigma receptor ligands on the acetylcholine release in the rat brain. J Neural Transm 103:661-669 (1996).
131. Kovacs KJ, Larson AA. Discrepancies in characterization of sigma sites in the mouse central nervous system. Eur J Pharmacol 285:127-134 (1995).
132. Kulkarni SK, Dhir A. sigma-1 receptors in major depression and anxiety. Expert Rev Neurother 9:1021-1034 (2009).
133. Langa F, Codony X, Tovar V, Lavado A, Gimenez E, Cozar P, Cantero M, Dordal A, Hernandez E, Perez R, Monroy X, Zamanillo D, Guitart X, Montoliu L. Generation and phenotypic analysis of sigma receptor type I (sigma 1) knockout mice. Eur J Neurosci 18:2188-2196 (2003).
134. LePage KT, Ishmael JE, Low CM, Traynelis SF, Murray TF. Differential binding properties of [3H]dextrorphan and [3H]MK-801 in heterologously expressed NMDA receptors. Neuropharmacology 49:1-16 (2005).
135. Lever JR, Gustafson JL, Xu R, Allmon RL, Lever SZ. Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse 59:350-358 (2006).
136. Lucas G, Rymar VV, Sadikot AF, Debonnel G. Further evidence for an antidepressant potential of the selective sigma1 agonist SA 4503: Electrophysiological, morphological and behavioural studies. Int J Neuropsychopharmacol 11:485-495 (2008).
137. Lupardus PJ, Wilke RA, Aydar E, Palmer CP, Chen Y, Ruoho AE, Jackson MB. Membrane-delimited coupling between sigma receptors and K+ channels in rat neurohypophysial terminals requires neither G-protein nor ATP. J Physiol 526 (Pt 3):527-539 (2000).
138. Mach RH, Wu L, West T, Whirrett BR, ChildersSr., The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors. Life Sci 64:L131-L137 (1999).
139. Mamiya T, Noda Y, Noda A, Hiramatsu M, Karasawa K, Kameyama T, Furukawa S, Yamada K, Nabeshima T. Effects of sigma receptor agonists on the impairment of spontaneous alternation behavior and decrease of cyclic GMP level induced by nitric oxide synthase inhibitors in mice. Neuropharmacology 39:2391-2398 (2000).
140. Martin WR, Eades CG, Thompson JA, Huppler RE, Gilbert PE. The effects of morphineand nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog. J Pharmacol Exp Ther 197:517-532 (1976).
141. Martina M, Turcotte ME, Halman S, Bergeron R. The sigma-1 receptor modulates NMDA receptor synaptic transmission and plasticity via SK channels in rat hippocampus. J Physiol 578:143-157 (2007).
142. Matos FF, Korpinen C, Yocca FD. 5-HT1A receptor agonist effects of BMY-14802 on serotonin release in dorsal raphe and hippocampus. Eur J Pharmacol 317:49-54 (1996).
143. Matsumoto RR, Bowen WD, Tom MA, Vo VN, Truong DD, de Costa BR. Characterization of two novel sigma receptor ligands: Antidystonic effects in rats suggest sigma receptor antagonism. Eur J Pharmacol 280:301-310 (1995).
144. Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Hauck NA. Rimcazole analogs attenuate the convulsive effects of cocaine: Correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology 41:878-886 (2001).
145. Matsumoto RR, McCracken KA, Pouw B, Zhang Y, Bowen WD. Involvement of sigma receptors in the behavioral effects of cocaine: Evidence from novel ligands and antisense oligodeoxynucleotides. Neuropharmacology 42:1043-1055 (2002).
146. Matsumoto RR, Pouw B. Correlation between neuroleptic binding to sigma (1) and sigma (2) receptors and acute dystonic reactions. Eur J Pharmacol 401:155-160 (2000).
147. Matsumoto RR, Shaikh J, Wilson LL, Vedam S, Coop A. Attenuation of methamphetamine- induced effects through the antagonism of sigma (sigma) receptors: Evidence from in vivo and in vitro studies. Eur Neuropsychopharmacol 18:871-881 (2008).
148. Matsuno K, Kobayashi T, Tanaka MK, Mita S. Sigma 1 receptor subtype is involved in the relief of behavioral despair in the mouse forced swimming test. Eur J Pharmacol 312:267-271, (1996).
149. Matsuno K, Nakazawa M, Okamoto K, Kawashima Y, Mita S. Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur J Pharmacol 306:271-279, (1996).
150. Matthews RT, McMillen BA, Sallis R, Blair D. Effects of BMY 14802, a potential antipsychotic drug, on rat brain dopaminergic function. J Pharmacol Exp Ther 239:124- 131 (1986).
151. Maurice T, Casalino M, Lacroix M, Romieu P. Involvement of the sigma 1 receptor in the motivational effects of ethanol in mice. Pharmacol Biochem Behav 74:869-876 (2003).
152. Maurice T, Gregoire C, Espallergues J. Neuro (active)steroids actions at the neuromodulatory sigma1 (sigma1) receptor: Biochemical and physiological evidences, consequences in neuroprotection. Pharmacol Biochem Behav 84:581-597 (2006).
153. Maurice T, Martin-Fardon R, Romieu P, Matsumoto RR. Sigma (1) (sigma (1)) receptor antagonists represent a new strategy against cocaine addiction and toxicity. Neurosci Biobehav Rev 26:499-527 (2002).
154. Maurice T, Meunier J, Feng B, Ieni J, Monaghan DT. Interaction with sigma (1) protein, but not N-methyl-D-aspartate receptor, is involved in the pharmacological activity of donepezil. J Pharmacol Exp Ther 317:606-614 (2006).
155. Maurice T, Phan VL, Privat A. The anti-amnesic effects of sigma1 (sigma1) receptor agonists confirmed by in vivo antisense strategy in the mouse. Brain Res 898:113-121, (2001).
156. Maurice T, Phan VL, Urani A, Kamei H, Noda Y, Nabeshima T. Neuroactive neurosteroids as endogenous effectors for the sigma1 (sigma1) receptor: Pharmacological evidence and therapeutic opportunities. Jpn J Pharmacol 81:125-155 (1999).
157. Maurice T, Romieu P. Involvement of the sigma1 receptor in the appetitive effects of cocaine. Pharmacopsychiatry 37 (Suppl 3):S198-S207 (2004).
158. Maurice T, Su TP, Parish DW, Nabeshima T, Privat A. PRE-084, a sigma selective PCP derivative, attenuates MK-801-induced impairment of learning in mice. Pharmacol Biochem Behav 49:859-869 (1994).
159. Maurice T, Su TP. The pharmacology of sigma-1 receptors. Pharmacol Ther 124:195- 206 (2009).
160. Maurice T, Urani A, Phan VL, Romieu P. The interaction between neuroactive steroids and the sigma1 receptor function: Behavioral consequences and therapeutic opportunities. Brain Res Brain Res Rev 37:116-132, (2001).
161. Maurice T. Neurosteroids and sigma1 receptors, biochemical and behavioral relevance. Pharmacopsychiatry 37 (Suppl 3):S171-S182 (2004).
162. McCann DJ,Weissman AD, Su TP. Sigma-1 and sigma-2 sites in rat brain: comparison of regional, ontogenetic, and subcellular patterns. Synapse 17:182-189 (1994).
163. McCracken KA, Bowen WD, de Costa BR, Matsumoto RR. Two novel sigma receptor ligands, BD1047 and LR172, attenuate cocaine-induced toxicity and locomotor activity. Eur J Pharmacol 370:225-232, (1999).
164. McCracken KA, Bowen WD, Matsumoto RR. Novel sigma receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur J Pharmacol 365:35-38, (1999).
165. Megalizzi V, Decaestecker C, Debeir O, Spiegl-Kreinecker S, BergerW, Lefranc F, Kast RE, Kiss R. Screening of anti-glioma effects induced by sigma-1 receptor ligands: potential new use for old anti-psychiatric medicines. Eur J Cancer 45:2893-2905 (2009).
166. Megalizzi V, Mathieu V, Mijatovic T, Gailly P, Debeir O, De Neve N, Van Damme M, Bontempi G, Haibe-Kains B, Decaestecker C, Kondo Y, Kiss R, Lefranc F. 4-IBP, a sigma1 receptor agonist, decreases the migration of human cancer cells, including glioblastoma cells, in vitro and sensitizes them in vitro and in vivo to cytotoxic insults of proapoptotic and proautophagic drugs. Neoplasia 9:358-369 (2007).
167. Mei J, Pasternak GW. Sigma1 receptor modulation of opioid analgesia in the mouse. J Pharmacol Exp Ther 300:1070-1074 (2002).
168. Meunier J, Hayashi T. Sigma-1 receptors regulate Bcl-2 expression by reactive oxygen species-dependent transcriptional regulation of nuclear factor kappaB. J Pharmacol Exp Ther 332:388-397 (2010).
169. Meunier J, Ieni J, Maurice T. The anti-amnesic and neuroprotective effects of donepezil against amyloid beta25-35 peptide-induced toxicity in mice involve an interaction with the sigma1 receptor. Br J Pharmacol 149:998-1012 (2006).
170. Meurs A, Clinckers R, Ebinger G, Michotte Y, Smolders I. Sigma 1 receptor-mediated increase in hippocampal extracellular dopamine contributes to the mechanism of the anticonvulsant action of neuropeptide Y. Eur J Neurosci 26:3079-3092 (2007).
171. Meyer DA, Carta M, Partridge LD, Covey DF, Valenzuela CF. Neurosteroids enhance spontaneous glutamate release in hippocampal neurons. Possible role of metabotropic sigma1-like receptors. J Biol Chem 277:28725-28732 (2002).
172. Mizuno T, Yotsuyanagi S, Kondo Y, Komatsu K, Ishiura Y, Nakamura Y, Nagasaka Y, Yokoyama O, Namiki M. Dehydroepiandrosterone alleviates copulatory disorder induced by social stress in male rats. J Sex Med 3:612-618 (2006).
173. Modell S, Naber D, Holzbach R. Efficacy and safety of an opiate sigma-receptor antagonist (SL 82. 0715) in schizophrenic patients with negative symptoms: an open dose-range study. Pharmacopsychiatry 29:63-66 (1996).
174. Moebius FF, Bermoser K, Reiter RJ, Hanner M, Glossmann H. Yeast sterol C8-C7 isomerase: identification and characterization of a high-affinity binding site for enzyme inhibitors. Biochemistry 35:16871-16878 (1996).
175. Moebius FF, Reiter RJ, Hanner M, Glossmann H. High affinity of sigma 1-binding sites for sterol isomerization inhibitors: Evidence for a pharmacological relationship with the yeast sterol C8-C7 isomerase. Br J Pharmacol 121:1-6, (1997).
176. Moebius FF, Striessnig J, Glossmann H. The mysteries of sigma receptors: new family members reveal a role in cholesterol synthesis. Trends Pharmacol Sci 18:67-70, (1997).
177. Moller HJ, Volz HP, Reimann IW, Stoll KD. Opipramol for the treatment of generalized anxiety disorder: A placebo-controlled trial including an alprazolam-treated group. J Clin Psychopharmacol 21:59-65 (2001).
178. Moller HJ, Volz HP, Stoll KD. Psychopharmacotherapy of sornatoform disorders: Effects of Opipramol on symptoms of somatization, anxiety, and depression. Acta Neuropsychiatrica 15:217-226 (2003).
179. Monnet FP, Blier P, Debonnel G, De Montigny C. Modulation by sigma ligands of N-methyl-D-aspartate-induced [3H]noradrenaline release in the rat hippocampus: G-protein dependency. Naunyn Schmiedebergs Arch Pharmacol 346:32-39, (1992).
180. Monnet FP, de Costa BR, Bowen WD. Differentiation of sigma ligand-activated receptor subtypes that modulate NMDA-evoked [3H]-noradrenaline release in rat hippocampal slices. Br J Pharmacol 119:65-72 (1996).
181. Monnet FP, Debonnel G, De Montigny C. In vivo electrophysiological evidence for a selective modulation of N-methyl-D-aspartate-induced neuronal activation in rat CA3 dorsal hippocampus by sigma ligands. J Pharmacol Exp Ther 261:123-130, (1992).
182. Monnet FP, Debonnel G, Fournier A, De Montigny C. Neuropeptide Y potentiates the Nmethyl- D-aspartate response in the CA3 dorsal hippocampus. II. Involvement of a subtype of sigma receptor. J Pharmacol Exp Ther 263:1219-1225, (1992).
183. Monnet FP, Debonnel G, Junien JL, De Montigny C. N-methyl-D-aspartate-induced neuronal activation is selectively modulated by sigma receptors. Eur J Pharmacol 179:441-445 (1990).
184. Monnet FP, Mahe V, Robel P, Baulieu EE. Neurosteroids, via sigma receptors, modulate the [3H]norepinephrine release evoked by N-methyl-D-aspartate in the rat hippocampus. Proc Natl Acad Sci USA 92:3774-3778 (1995).
185. Monnet FP, Maurice T. The sigma1 protein as a target for the non-genomic effects of neuro (active)steroids: Molecular, physiological, and behavioral aspects. J Pharmacol Sci 100:93-118 (2006).
186. Moriguchi S, Yamamoto Y, Ikuno T, Fukunaga K. Sigma-1 receptor stimulation by dehydroepiandrosterone ameliorates cognitive impairment through activation of CaM kinase II, protein kinase C and extracellular signal-regulated kinase in olfactory bulbectomized mice. J Neurochem 117: 879-891 (2011).
187. Mtchedlishvili Z, Kapur J. A presynaptic action of the neurosteroid pregnenolone sulfate on GABAergic synaptic transmission. Mol Pharmacol 64:857-864 (2003).
188. Muller MJ, Grunder G,Wetzel H, Muller-Siecheneder F, Marx-Dannigkeit P, Benkert O. Antipsychotic effects and tolerability of the sigma ligand EMD 57445 (panamesine) and its metabolites in acute schizophrenia: An open clinical trial. Psychiatry Res 89:275-280 (1999).
189. Muller WE, Siebert B. [Opipramol in comparison to other drugs-new pharmacologic data]. Fortschr Neurol Psychiatry 66 (Suppl 1):S9-S12 (1998).
190. Musacchio JM, Klein M, Paturzo JJ. Effects of dextromethorphan site ligands and allosteric modifiers on the binding of (+)-[3H]3- (-3-hydroxyphenyl)-N- (1-propyl) piperidine. Mol Pharmacol 35:1-5 (1989).
191. Nahas RI, Lever JR, Lever SZ. Synthesis and structure-activity relationships of N- (3- phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors. Bioorg Med Chem 16:755-761 (2008).
192. Narayanan S, Mesangeau C, Poupaert JH, McCurdy CR. Sigma receptors and cocaine abuse. Curr Top Med Chem 11:1128-1150 (2011).
193. Narita N, Hashimoto K, Tomitaka S, Minabe Y. Interactions of selective serotonin reuptake inhibitors with subtypes of sigma receptors in rat brain. Eur J Pharmacol 307:117-119 (1996).
194. Navarro G, Moreno E, Aymerich M, Marcellino D, McCormick PJ, Mallol J, Cortes A, Casado V, Canela EI, Ortiz J, Fuxe K, Lluis C, Ferre S, Franco R. Direct involvement of sigma-1 receptors in the dopamine D1 receptor-mediated effects of cocaine. Proc Natl Acad Sci USA 107:18676-18681 (2010).
195. Neff CD, Abkevich V, Packer JC, Chen Y, Potter J, Riley R, Davenport C, DeGrado WJ, Jammulapati S, Bhathena A, Choi WS, Kroeger PE, Metzger RE, Gutin A, Skolnick MH, Shattuck D, Katz DA. Evidence for HTR1A and LHPP as interacting genetic risk factors in major depression. Mol Psychiatry 14:621-630 (2009).
196. Neznamov GG, Siuniakov SA, Chumakov DV, Bochkarev VK, Seredenin SB. [Clinical study of the selective anxiolytic agent afobazol]. Eksp Klin Farmakol 64:15-19 (2001).
197. Nguyen EC, McCracken KA, Liu Y, Pouw B, Matsumoto RR. Involvement of sigma (sigma) receptors in the acute actions of methamphetamine: Receptor binding and behavioral studies. Neuropharmacology 49:638-645 (2005).
198. Nobile M, Lagostena L. A discriminant block among K+ channel types by phenytoin in neuroblastoma cells. Br J Pharmacol 124:1698-1702 (1998).
199. Noda Y, Kamei H, Kamei Y, Nagai T, Nishida M, Nabeshima T. Neurosteroids ameliorate conditioned fear stress: an association with sigma receptors. Neuropsychopharmacology 23:276-284 (2000).
200. Novakova M, Bruderova V, Sulova Z, Kopacek J, Lacinova L, Kvetnansky R, Vasku A, Kaplan P, Krizanova O, Jurkovicova D. Modulation of expression of the sigma receptors in the heart of rat and mouse in normal and pathological conditions. Gen Physiol Biophys 26:110-117 (2007).
201. Novakova M, Ela C, Barg J, Vogel Z, Hasin Y, Eilam Y. Inotropic action of sigma receptor ligands in isolated cardiac myocytes from adult rats. Eur J Pharmacol 286:19- 30 (1995).
202. Ogawa S, Okuyama S, Araki H, Otomo S. Effect of NE-100, a novel sigma receptor ligand, on phencyclidine-induced cognitive dysfunction. Eur J Pharmacol 263:9-15 (1994).
203. Ogawa S, Okuyama S, Tsuchida K, Araki H, Otomo S. The sigma-selective ligand NE- 100 attenuates the effect of phencyclidine in a rat diving model. Gen Pharmacol 26:177- 182 (1995).
204. Ohmori O, Shinkai T, Suzuki T, Okano C, Kojima H, Terao T, Nakamura J. Polymorphisms of the sigma (1) receptor gene in schizophrenia: An association study. Am J Med Genet 96:118-122 (2000).
205. Ohsawa M, Hayashi SS, Kamei J. Effect of acute topical application of+-pentazocine on the mechanical allodynia in diabetic mice. Eur J Pharmacol 641:49-53 (2010).
206. Okuyama S, Imagawa Y, Ogawa S, Araki H, Ajima A, Tanaka M, Muramatsu M, Nakazato A, Yamaguchi K, Yoshida M. NE-100, a novel sigma receptor ligand: In vivo tests. Life Sci 53:L285-L290 (1993).
207. Okuyama S, Imagawa Y, Sakagawa T, Nakazato A, Yamaguchi K, Katoh M, Yamada S, Araki H, Otomo S. NE-100, a novel sigma receptor ligand: Effect on phencyclidineinduced behaviors in rats, dogs and monkeys. Life Sci 55:L133-L138 (1994).
208. Okuyama S, Ogawa S, Nakazato A, Tomizawa K. Effect of NE-100, a novel sigma receptor ligand, on phencyclidine-induced delayed cognitive dysfunction in rats. Neurosci Lett 189:60-62 (1995).
209. Pal K, Pore S, Sinha S, Janardhanan R, Mukhopadhyay D, Banerjee R. Structure-activity study to develop cationic lipid-conjugated haloperidol derivatives as a new class of anticancer therapeutics. J Med Chem 54:2378-2390 (2011).
210. Palacios G, Muro A, Verdu E, Pumarola M, Vela JM. Immunohistochemical localization of the sigma1 receptor in Schwann cells of rat sciatic nerve. Brain Res 1007:65-70 (2004).
211. Pande AC, Geneve J, Scherrer B, Smith F, Leadbetter RA, de Meynard C. A placebocontrolled trial of igmesine in the treatment of major depression. Eur Neuropsychopharmacol 9 (Suppl 5):138 (1999).
212. Peeters M, Romieu P, Maurice T, Su TP, Maloteaux JM, Hermans E. Involvement of the sigma 1 receptor in the modulation of dopaminergic transmission by amantadine. Eur J Neurosci 19:2212-2220 (2004).
213. Penas C, Pascual-Font A, Mancuso R, Fores J, Casas C, Navarro X. Sigma receptor agonist 2- (4-morpholinethyl)1 phenylcyclohexanecarboxylate (PRE084) increases GDNF and BIP expression and promotes neuroprotection after root avulsion injury. J Neurotrauma 28:831-840 (2011).
214. Perregaard J, Moltzen EK, Meier E, Sanchez C. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3- (Omega-aminoalkyl)-1Hindoles. J Med Chem 38:1998-2008 (1995).
215. Poncelet M, Santucci V, Paul R, Gueudet C, Lavastre S, Guitard J, Steinberg R, Terranova JP, Breliere JC, Soubrie P. Neuropharmacological profile of a novel and selective ligand of the sigma site: SR 31742A. Neuropharmacology 32:605-615 (1993).
216. Quirion R, Bowen WD, Itzhak Y, Junien JL, Musacchio JM, Rothman RB, Su TP, Tam SW, Taylor DP. A proposal for the classification of sigma binding sites. Trends Pharmacol Sci 13:85-86 (1992).
217. Ramachandran S, Chu UB, Mavlyutov TA, Pal A, Pyne S, Ruoho AE. The sigma1 receptor interacts with N-alkyl amines and endogenous sphingolipids. Eur J Pharmacol 609:19-26 (2009).
218. Reddy DS, Kaur G, Kulkarni SK. Sigma (sigma1) receptor mediated anti-depressant-like effects of neurosteroids in the Porsolt forced swim test. Neuroreport 9:3069-3073 (1998).
219. Ritsner MS, Gibel A, Shleifer T, Boguslavsky I, Zayed A, Maayan R,Weizman A, Lerner V. Pregnenolone and dehydroepiandrosterone as an adjunctive treatment in schizophrenia and schizoaffective disorder: An 8-week, double-blind, randomized, controlled, 2- center, parallel-group trial. J Clin Psychiatry 71:1351-1362 (2010).
220. Ritsner MS. Pregnenolone, dehydroepiandrosterone, and schizophrenia: Alterations and clinical trials. CNS Neurosci Ther 16:32-44 (2010).
221. Robichaud M, Debonnel G. Modulation of the firing activity of female dorsal raphe nucleus serotonergic neurons by neuroactive steroids. J Endocrinol 182:11-21 (2004).
222. Rodvelt KR, Lever SZ, Lever JR, Blount LR, Fan KH, Miller DK. SA 4503 attenuates cocaine-induced hyperactivity and enhances methamphetamine substitution for a cocaine discriminative stimulus. Pharmacol Biochem Behav 97:676-682 (2011).
223. Rodvelt KR, Miller DK. Could sigma receptor ligands be a treatment for methamphetamine addiction? Curr Drug Abuse Rev 3:156-162 (2010).
224. Rogers C, Lemaire S. Role of the sigma receptor in the inhibition of [3H]-noradrenaline uptake in brain synaptosomes and adrenal chromaffin cells. Br J Pharmacol 103:1917- 1922 (1991).
225. Rogoz Z, Skuza G. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep 58:493-500 (2006).
226. Roh DH, Kim HW, Yoon SY, Seo HS, Kwon YB, Kim KW, Han HJ, Beitz AJ, Na HS, Lee JH. Intrathecal injection of the sigma (1) receptor antagonist BD1047 blocks both mechanical allodynia and increases in spinal NR1 expression during the induction phase of rodent neuropathic pain. Anesthesiology 109:879-889 (2008).
227. Roman FJ, Pascaud X, Duffy O, Vauche D, Martin B, Junien JL. Neuropeptide Y and peptide YY interact with rat brain sigma and PCP binding sites. Eur J Pharmacol 174:301-302 (1989).
228. Romieu P, Martin-Fardon R, Bowen WD, Maurice T. Sigma 1 receptor-related neuroactive steroids modulate cocaine-induced reward. J Neurosci 23:3572-3576 (2003).
229. Ronsisvalle G, Prezzavento O, Marrazzo A, Vittorio F, Bousquet E, Di Toro R, Spampinato S. Synthesis and binding affinity of cis- (-)- and cis- (+)-N-ethyleneamino- N-nordeoxymetazocine and cis- (-)-N-normetazocine analogues at sigma1, sigma2 and kappa opioid receptors. Eur J Pharm Sci 12:277-284 (2001).
230. Rothman RB, Baumann MH. Monoamine transporters and psychostimulant drugs. Eur J Pharmacol 479:23-40 (2003).
231. Ruscher K, Shamloo M, Rickhag M, Ladunga I, Soriano L, Gisselsson L, Toresson H, Ruslim-Litrus L, Oksenberg D, Urfer R, Johansson BB, Nikolich K, Wieloch T. The sigma-1 receptor enhances brain plasticity and functional recovery after experimental stroke. Brain 134:732-746 (2011).
232. Rush AM, ElliottJr., Phenytoin and carbamazepine: Differential inhibition of sodium currents in small cells from adult rat dorsal root ganglia. Neurosci Lett 226:95-98 (1997).
233. Sabeti J. Ethanol exposure in early adolescence inhibits intrinsic neuronal plasticity via sigma-1 receptor activation in hippocampal CA1 neurons. Alcohol Clin Exp Res 35:885-904 (2011).
234. Sabino V, Cottone P, Zhao Y, Iyer MR, Steardo L Jr, Steardo L, Rice KC, Conti B, Koob GF, Zorrilla EP. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology 34:1482-1493, (2009).
235. Sabino V, Cottone P, Zhao Y, Steardo L, Koob GF, Zorrilla EP. Selective reduction of alcohol drinking in Sardinian alcohol-preferring rats by a sigma-1 receptor antagonist. Psychopharmacology (Berl) 205:327-335, (2009).
236. Samson HH, Tolliver GA, Haraguchi M, Hodge CW. Alcohol self-administration: Role of mesolimbic dopamine. Ann NY Acad Sci 654:242-253 (1992).
237. Sanchez-Arroyos R, Guitart X. Electrophysiological effects of E-5842, a sigma1 receptor ligand and potential atypical antipsychotic, on A9 and A10 dopamine neurons. Eur J Pharmacol 378:31-37 (1999).
238. Satoh F, Miyatake R, Furukawa A, Suwaki H. Lack of association between sigma receptor gene variants and schizophrenia. Psychiatry Clin Neurosci 58:359-363 (2004).
239. Schlyer DJ, Volkow ND, Fowler JS,Wolf AP, Shiue CY, Dewey SL, Bendriem B, Logan J, Raulli R, Hitzemann R. Regional distribution and kinetics of haloperidol binding in human brain: A PET study with [18F]haloperidol. Synapse 11:10-19 (1992).
240. Schwarz S, Pohl P, Zhou GZ. Steroid binding at sigma-"opioid" receptors. Science 246:1635-1638 (1989).
241. Schwarz S, Pohl P. Lack of evidence for in vivo interaction of steroids with haloperidolsensitive sigma (sigma H) binding sites in brain and spleen. Prog Clin Biol Res 328:17- 20 (1990).
242. Seredenin SB, Antipova TA, Voronin MV, Kurchashova SY, Kuimov AN. Interaction of afobazole with sigma1-receptors. Bull Exp Biol Med 148:42-44 (2009).
243. Sharkey J, Glen KA, Wolfe S, Kuhar MJ. Cocaine binding at sigma receptors. Eur J Pharmacol 149:171-174 (1988).
244. Shibuya H, Mori H, Toru M. Sigma receptors in schizophrenic cerebral cortices. Neurochem Res 17:983-990 (1992).
245. Shimazu S, Katsuki H, Takenaka C, Tomita M, Kume T, Kaneko S, Akaike A. sigma receptor ligands attenuate N-methyl-D-aspartate cytotoxicity in dopaminergic neurons of mesencephalic slice cultures. Eur J Pharmacol 388:139-146 (2000).
246. Shin EJ, Nah SY, Kim WK, Ko KH, Jhoo WK, Lim YK, Cha JY, Chen CF, Kim HC. The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: Comparison with the effects of dextromethorphan. Br J Pharmacol 144:908-918 (2005).
247. Skolnick P, Popik P, Trullas R. Glutamate-based antidepressants: 20 years on. Trends Pharmacol Sci 30:563-569 (2009).
248. Skuza G, Rogoz Z. A potential antidepressant activity of SA4503, a selective sigma 1 receptor agonist. Behav Pharmacol 13:537-543 (2002).
249. Skuza G, Rogoz Z. The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. J Physiol Pharmacol 57:217-229 (2006).
250. Smith RL, Canton H, Barrett RJ, Sanders-Bush E. Agonist properties of N, N-dimethyltryptamine at serotonin 5-HT2A and 5-HT2C receptors. Pharmacol Biochem Behav 61:323-330 (1998).
251. Son JS, Kwon YB. Sigma-1 receptor antagonist BD1047 reduces allodynia and spinal ERK phosphorylation following chronic compression of dorsal root ganglion in rats. Korean J Physiol Pharmacol 14:359-364 (2010).
252. Spruce BA, Campbell LA, McTavish N, Cooper MA, Appleyard MV, O'Neill M, Howie J, Samson J,Watt S, Murray K, McLean D, Leslie NR, Safrany ST, Ferguson MJ, Peters JA, Prescott AR, Box G, Hayes A, Nutley B, Raynaud F, Downes CP, Lambert JJ, Thompson AM, Eccles S. Small molecule antagonists of the sigma-1 receptor cause selective release of the death program in tumor and self-reliant cells and inhibit tumor growth in vitro and in vivo. Cancer Res 64:4875-4886 (2004).
253. Stahl SM. Antidepressant treatment of psychotic major depression: Potential role of the sigma receptor. CNS Spectr 10:319-323 (2005).
254. Su TP, Hayashi T, Maurice T, Buch S, Ruoho AE. The sigma-1 receptor chaperone as an inter-organelle signaling modulator. Trends Pharmacol Sci 31:557-566 (2010).
255. Su TP, Hayashi T, Vaupel DB. When the endogenous hallucinogenic trace amine N, Ndimethyltryptamine meets the sigma-1 receptor. Sci Signal 2:pe12 (2009).
256. Su TP, Hayashi T. Understanding the molecular mechanism of sigma-1 receptors: Towards a hypothesis that sigma-1 receptors are intracellular amplifiers for signal transduction. Curr Med Chem 10:2073-2080 (2003).
257. Su TP, London ED, Jaffe JH. Steroid binding at sigma receptors suggests a link between endocrine, nervous, and immune systems. Science 240:219-221 (1988).
258. Su TP. Evidence for sigma opioid receptor: binding of [3H]SKF-10047 to etorphineinaccessible sites in guinea-pig brain. J Pharmacol Exp Ther 223:284-290 (1982).
259. Tagashira H, Bhuiyan S, Shioda N, Hasegawa H, Kanai H, Fukunaga K. Sigma1-receptor stimulation with fluvoxamine ameliorates transverse aortic constriction-induced myocardial hypertrophy and dysfunction in mice. Am J Physiol Heart Circ Physiol 299: H1535-H1545 (2010).
260. Takebayashi M, Hayashi T, Su TP. A perspective on the new mechanism of antidepressants: Neuritogenesis through sigma-1 receptors. Pharmacopsychiatry 37 (Suppl 3): S208-S213, (2004).
261. Takebayashi M, Hayashi T, Su TP. Nerve growth factor-induced neurite sprouting in PC12 cells involves sigma-1 receptors: Implications for antidepressants. J Pharmacol Exp Ther 303:1227-1237 (2002).
262. Takebayashi M, Hayashi T, Su TP. Sigma-1 receptors potentiate epidermal growth factor signaling towards neuritogenesis in PC12 cells: Potential relation to lipid raft reconstitution. Synapse 53:90-103, (2004).
263. Takizawa R, Hashimoto K, Tochigi M, Kawakubo Y, Marumo K, Sasaki T, Fukuda M, Kasai K. Association between sigma-1 receptor gene polymorphism and prefrontal hemodynamic response induced by cognitive activation in schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry 33:491-498 (2009).
264. Tam SW, Mitchell KN. Neuropeptide Yand peptide YY do not bind to brain sigma and phencyclidine binding sites. Eur J Pharmacol 193:121-122 (1991).
265. Tam SW, Steinfels GF, Gilligan PJ, Schmidt WK, Cook L. DuP 734 [1- (cyclopropylmethyl)- 4- (2' (4"-fluorophenyl)-2'-oxoethyl)- piperidine HBr], a sigma and 5-hydroxytryptamine2 receptor antagonist: receptor-binding, electrophysiological and neuropharmacological profiles. J Pharmacol Exp Ther 263:1167-1174 (1992).
266. Tan F, Guio-Aguilar PL, Downes C, Zhang M, O'Donovan L, Callaway JK, Crack PJ. The sigma 1 receptor agonist 4-PPBP elicits ERK1/2 phosphorylation in primary neurons: A possible mechanism of neuroprotective action. Neuropharmacology 59:416-424 (2010).
267. Tchedre KT, Huang RQ, Dibas A, Krishnamoorthy RR, Dillon GH, Yorio T. Sigma-1 receptor regulation of voltage-gated calcium channels involves a direct interaction. Investg. Ophthalmol Vis Sci 49:4993-5002 (2008).
268. Todorovic SM, Lingle CJ. Pharmacological properties of T-type Ca2+ current in adult rat sensory neurons: Effects of anticonvulsant and anesthetic agents. J Neurophysiol 79:240-252 (1998).
269. Tottori K, Miwa T, Uwahodo Y, Yamada S, Nakai M, Oshiro Y, Kikuchi T, Altar CA. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology 41:976-988 (2001).
270. Tsai SY, Hayashi T, Harvey BK, Wang Y, Wu WW, Shen RF, Zhang Y, Becker KG, Hoffer BJ, Su TP. Sigma-1 receptors regulate hippocampal dendritic spine formation via a free radical-sensitive mechanism involving Rac1xGTP pathway. Proc Natl Acad Sci USA 106:22468-22473 (2009).
271. Uchida N, Ujike H, Nakata K, Takaki M, Nomura A, Katsu T, Tanaka Y, Imamura T, Sakai A, Kuroda S. No association between the sigma receptor type 1 gene and schizophrenia: Results of analysis and meta-analysis of case-control studies. BMC Psychiatry 3:13 (2003).
272. Ukai M, Maeda H, Nanya Y, Kameyama T, Matsuno K. Beneficial effects of acute and repeated administrations of sigma receptor agonists on behavioral despair in mice exposed to tail suspension. Pharmacol Biochem Behav 61:247-252 (1998).
273. Urani A, Roman FJ, Phan VL, Su TP, Maurice T. The antidepressant-like effect induced by sigma (1)-receptor agonists and neuroactive steroids in mice submitted to the forced swimming test. J Pharmacol Exp Ther 298:1269-1279 (2001).
274. Urani A, Romieu P, Roman FJ, Maurice T. Enhanced antidepressant effect of sigma (1) (sigma (1)) receptor agonists in beta (25-35)-amyloid peptide-treated mice. Behav Brain Res 134:239-247 (2002).
275. Urani A, Romieu P, Roman FJ, Yamada K, Noda Y, Kamei H, Manh TH, Nagai T, Nabeshima T, Maurice T. Enhanced antidepressant efficacy of sigma1 receptor agonists in rats after chronic intracerebroventricular infusion of beta-amyloid- (1-40) protein. Eur J Pharmacol 486:151-161 (2004).
276. vanWaarde A, Ramakrishnan NK, Rybczynska AA, Elsinga PH, Ishiwata K, Nijholt IM, Luiten PG, Dierckx RA. The cholinergic system, sigma-1 receptors and cognition. Behav Brain Res 221:543-554 (2011).
277. vanWaarde A, Rybczynska AA, Ramakrishnan N, Ishiwata K, Elsinga PH, Dierckx RA. Sigma receptors in oncology: Therapeutic and diagnostic applications of sigma ligands. Curr Pharm Design 16:3519-3537 (2010).
278. VanderMaelen CP, Braselton JP. Effects of a potential antipsychotic, BMY 14802, on firing of central serotonergic and noradrenergic neurons in rats. Eur J Pharmacol 179:357-366 (1990).
279. Vaupel DB. Naltrexone fails to antagonize the sigma effects of PCP and SKF 10,047 in the dog. Eur J Pharmacol 92:269-274 (1983).
280. Vilner BJ, Bowen WD. Modulation of cellular calcium by sigma-2 receptors: Release from intracellular stores in human SK-N-SH neuroblastoma cells. J Pharmacol Exp Ther 292:900-911 (2000).
281. Vilner BJ, John CS, Bowen WD. Sigma-1 and sigma-2 receptors are expressed in a wide variety of human and rodent tumor cell lines. Cancer Res 55:408-413 (1995).
282. Volz HP, Moller HJ, Reimann I, Stoll KD. Opipramol for the treatment of somatoform disorders results from a placebo-controlled trial. Eur Neuropsychopharmacol 10:211- 217 (2000).
283. Volz HP, Stoll KD. Clinical trials with sigma ligands. Pharmacopsychiatry 37 (Suppl 3): S214-S220 (2004).
284. Wachtel SR, White FJ. Electrophysiological effects of BMY 14802, a new potential antipsychotic drug, on midbrain dopamine neurons in the rat: Acute and chronic studies. J Pharmacol Exp Ther 244:410-416 (1988).
285. Walker JM, Bowen WD, Walker FO, Matsumoto RR, De Costa B, Rice KC. Sigma receptors: Biology and function. Pharmacol Rev 42:355-402 (1990).
286. Wang B, Rouzier R, Albarracin CT, Sahin A, Wagner P, Yang Y, Smith TL, Meric- Bernstam F, Marcelo AC, Hortobagyi GN, Pusztai L. Expression of sigma 1 receptor in human breast cancer. Breast Cancer Res Treat 87:205-214 (2004).
287. Wang HH, Chien JW, Chou YC, Liao JF, Chen CF. Anti-amnesic effect of dimemorfan in mice. Br J Pharmacol 138:941-949 (2003).
288. Weissman AD, CasanovaMF, Kleinman JE, London ED, De Souza EB. Selective loss of cerebral cortical sigma, but not PCP binding sites in schizophrenia. Biol Psychiatry 29:41-54 (1991).
289. Wilke RA, Lupardus PJ, Grandy DK, Rubinstein M, Low MJ, Jackson MB. K+ channel modulation in rodent neurohypophysial nerve terminals by sigma receptors and not by dopamine receptors. J Physiol 517 (Pt 2):391-406 (1999).
290. Wilke RA, Mehta RP, Lupardus PJ, Chen Y, Ruoho AE, Jackson MB. Sigma receptor photolabeling and sigma receptor-mediated modulation of potassium channels in tumor cells. J Biol Chem 274:18387-18392 (1999).
291. Wilke RA. Posterior pituitary sigma receptors and drug-induced syndrome of inappropriate antidiuretic hormone release. Ann Intern Med 131:799 (1999).
292. Willuhn I, Wanat MJ, Clark JJ, Phillips PE. Dopamine signaling in the nucleus accumbens of animals self-administering drugs of abuse. Curr Top Behav Neurosci 3:29-71 (2010).
293. Wolfe SA, Jr., Culp SG, De Souza EB. Sigma-receptors in endocrine organs: Identification, characterization, and autoradiographic localization in rat pituitary, adrenal, testis, and ovary. Endocrinology 124:1160-1172 (1989).
294. Wolfe SA Jr, Ha BK, Whitlock BB, Saini P. Differential localization of three distinct binding sites for sigma receptor ligands in rat spleen. J Neuroimmunol 72:45-58 (1997).
295. Yadid G, Sudai E, Maayan R, Gispan I,Weizman A. The role of dehydroepiandrosterone (DHEA) in drug-seeking behavior. Neurosci Biobehav Rev 35:303-314 (2010).
296. Yamada S, Uwahodo Y, Tottori K, et al. Role for s and 5-HT1A receptors in the forced swimming test supports the mechanism of action of OPC-14523. Soc Neurosci Abstr 26:2326 (2000).
297. Yang R, Zhou R, Chen L, CaiW, Tomimoto H, Sokabe M, Chen L. Pregnenolone sulfate enhances survival of adult-generated hippocampal granule cells via sustained presynaptic potentiation. Neuropharmacology 60:529-541 (2011).
298. Yang ZJ, Carter EL, Torbey MT, Martin LJ, Koehler RC. Sigma receptor ligand 4- phenyl-1- (4-phenylbutyl)-piperidine modulates neuronal nitric oxide synthase/postsynaptic density-95 coupling mechanisms and protects against neonatal ischemic degeneration of striatal neurons. Exp Neurol 221:166-174 (2010).
299. Yousef KA, Fowler JS, Volkow ND, Dewey SL, Shea C, Schlyer DJ, Gatley SJ, Logan J, Wolf AP. [18F]Haloperidol binding in baboon brain in vivo. Nucl Med Biol 23:47-52 (1996).
300. Zamanillo D, de la Puente B, Nadal X, Ovalle S, Sanchez R, Portillo E, Romero L, Muro A, Palacios G, Baeyens JM, Lopez-Garcia JA, Buschmann H, Maldonado R, Vela JM. Sigma 1 receptor blocking: A new therapeutic approach for neuropathic pain. 12th World Congress on Pain Glasgow, Aug 17-22, 2008, PH 247.
301. Zamanillo D, Romero L, Burgueno J, Nadal X, Dordal A, Gris G, Vidal A, Laloya M, Segales C, Portillo-Salido E, Baeyens JM, Lopez JA, Maldonado R, Vela JM. A new selective sigma-1 receptor antagonist (S1RA) reduces neuropathic pain behaviors and activity-induced spinal sensitisation. 3rd Int Congress Neuropathic Pain. Eur J Pain Suppl 4 (1):63 (2010).
302. Zhang H, Cuevas J. Sigma receptor activation blocks potassium channels and depresses neuroexcitability in rat intracardiac neurons. J Pharmacol Exp Ther 313:1387-1396 (2005).
303. Zhang H, Cuevas J. Sigma receptors inhibit high-voltage-activated calcium channels in rat sympathetic and parasympathetic neurons. J Neurophysiol 87:2867-2879 (2002).