Pharmacology of sigma (σ) receptor ligands from a behavioral perspective

Current Pharmaceutical Design

Volumn 18, Issue 7, 2012, Pages 863-874

  Skuza, Grazyna ^a  

^a INSTITUTE OF PHARMACOLOGY   (Poland)

Author keywords

1 and 2 receptor ligands; Anxiety; Behavioral effect; Cocaine; Dopamine (DA) agonists; Forced swim test (FST); Learning and memory; Olfactory bulbectomy (OB); Phencyclidine (PCP); Prepuls inhibition (PPI)

Indexed keywords

1 PHENYLCYCLOHEXANECARBOXYLIC ACID 2 MORPHOLINOETHYL ESTER; 2 [4 METHOXY 3 (2 PHENYLETHOXY)PHENYL] N,N DIPROPYLETHYLAMINE; 2 AMINO 4 METHYL 5 PHOSPHONO 3 PENTENOIC ACID; 4 (4 FLUOROPHENYL) 1,2,3,6 TETRAHYDRO 1 [4 (1,2,4 TRIAZOL 1 YL)BUTYL]PYRIDINE; 4 PHOSPHONOMETHYLPIPECOLIC ACID; 6 [6 (4 HYDROXY 1 PIPERIDINYL)HEXYLOXY] 3 METHYLFLAVONE; ALPHA (4 FLUOROPHENYL) 4 (5 FLUORO 2 PYRIMIDINYL) 1 PIPERAZINEBUTANOL; BD 1063; CLORGYLINE; CUTAMESINE; DIZOCILPINE; ELIPRODIL; FLUVOXAMINE; HALOPERIDOL; IGMESINE; MS 377; N [2 (3,4 DICHLOROPHENYL)ETHYL] 2 DIMETHYLAMINO N METHYLETHYLAMINE; N ALLYLNORMETAZOCINE; NALOXONE; OPC 14523; OPIATE AGONIST; OPIATE ANTAGONIST; PANAMESINE; PENTAZOCINE; PRECLAMOL; RIMCAZOLE; SERTRALINE; SIGMA OPIATE RECEPTOR; SIRAMESINE; SM 21; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANTIDEPRESSANT ACTIVITY; BEHAVIOR; CENTRAL NERVOUS SYSTEM FUNCTION; DRUG ACTIVITY; DRUG EFFECT; DRUG MECHANISM; FORCED SWIMMING TEST; HUMAN; LEARNING; MEMORY; MENTAL DISEASE; NEUROTRANSMISSION; NONHUMAN; PREPULSE INHIBITION; PRIORITY JOURNAL; REVIEW; SCHIZOPHRENIA;

ANIMALS; BEHAVIOR; BEHAVIOR, ANIMAL; CENTRAL NERVOUS SYSTEM AGENTS; HUMANS; LIGANDS; RECEPTORS, SIGMA;

EID: 84857131980     PISSN: 13816128     EISSN: 18734286     Source Type: Journal    
DOI: 10.2174/138161212799436458     Document Type: Review

References (147)

1. Gundlach AL, Largent BL, Snyder SH. Phencyclidine and sigma opiate receptors in brain: biochemical and autoradiographical differentiation. Eur J Pharmacol 1985; 113: 465-6.
2. Walker JM, Bowen WD, Walker FO, Matsumoto RR, De Costa B, Rice KC. Sigma receptors: biology and function. Pharmacol Rev 1990; 2: 355-402.
3. 3H]SKF 10,047 binding to sigma1 receptors in mouse forebrain. J Neurosci Res 1996; 46: 734-43.
4. Cobos EJ, Entrena JM, Nieto FR, Cendan CM, Del Pozo E. Pharmacology of therapeutic potential of sigma 1 receptor ligands. Curr Neuropharmacol 2008; 6: 344-66.
5. Martin WR, Eades CG, Thompson JA, Huppler RE, Gilbert PE. The effects of morphine-and nalorphine-like drugs in the nondependent and morphine-dependent chronic spinal dog. J Pharmacol Exp Ther 1976; 197: 517-32.
6. Hayashi T, Su TP. Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs 2004; 18: 269-84.
7. 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 2008; 12: 45-58.
8. Maurice T, Su TP. The pharmacology of sigma1 receptors. Pharmacol Ther 2009; 124: 195-206.
9. Quirion R, Bowen WD, Itzhak Y, et al. A proposal on the classification of sigma binding sites. Trends Pharmacol Sci 1992; 13: 85-6.
10. Hanner M, Moebius FF, Flandorfer A, et al. Purification, molecular cloning, and expression of the mammalian sigma1-binding site. Proc Natl Acad Sci USA 1996; 15: 8072-7.
11. Hayashi T, Su T-P. Sigma-1 receptor chaperones at the ERmitochondrion interface regulate Ca2+ signaling and cell survival. Cell 2007; 131: 596-610.
12. Bouchard P, Quirion R. [3H]1,3-di(2-tolyl)guanidine and [3H](+)pentazocine binding sites in the rat brain: autoradiographic visualization of the putative sigma1 and sigma2 receptor subtypes. Neuroscience 1997; 76: 467-77.
13. Crawford KW, Bowen WD. Sigma-2 receptor agonists activate a novel apoptotic pathway and potentiate antineoplastic drugs in breast tumor cell lines. Cancer Res 2002; 62: 313-22.
14. Walker JM, Bowen WD, Patrick SL, et al. A comparison of (-)-deoxybenzomorphans devoid of opiate activity with their dextrorotatory phenolic counterparts suggests role of sigma 2 receptors in motor function. Eur J Pharmacol 1993; 1: 61-8.
15. 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 1995; 280: 301-10.
16. Sánchez C, Arnt J, Costall B, et al. The selective σ2 ligand Lu 28-179 has potent anxiolytic-like effects in rodents. J Pharmacol Exp Ther 1997; 283: 1323-32.
17. Couture S, Debonnel G. Modulation of the neuronal response to Nmethyl-D-aspartate by selective sigma2 ligands. Synapse 1998; 29: 62-71.
18. Mach RH, Wu L, West T, Whirrett BR, Childers SR. The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors. Life Sci 1999; 64: PL131-7.
19. Matsumoto RR, Mack AL. (+/-)-SM 21 attenuates the convulsive and locomotor stimulatory effects of cocaine in mice. Eur J Pharmacol 2001; 417: R1-2.
20. Rao TS, Mick SJ, Cler JA, et al. Effects of sigma ligands on mouse cerebellar cyclic guanosine monophosphate (cGMP) levels in vivo: further evidence for a functional modulation of N-methyl-Daspartate (NMDA) receptor complex-mediated events by sigma ligands. Brain Res 1991; 561: 43-50.
21. Kobayashi T, Matsuno K, Nakata K, Mita S. Enhancement of acetylcholine release by SA4503, a novel sigma 1 receptor agonist, in the rat brain. J Pharmacol Exp Ther 1996; 279:106-13.
22. Patrick SL, Walker JM, Perkel JM, Lockwood M, Patrick RL. Increases in rat striatal extracellular dopamine and vacuous chewing produced by two sigma receptor ligands. Eur J Pharmacol 1993; 231: 243-9.
23. 3H]noradrenaline release in the rat hippocampus: G-protein dependency. Naunyn Schmiedebergs Arch Pharmacol 1992; 346: 32-9.
24. Garcés-Ramírez L, Green JL, Hiranita T, et al. Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis. Biol Psychiatry 2011; 69: 208-17.
25. Sánchez-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 1999; 378: 31-7.
26. Kobayashi T, Matsuno K, Murai M, Mita S. Sigma 1 receptor subtype is involved in the facilitation of cortical dopaminergic transmission in the rat brain. Neurochem Res 1997; 22: 1105-9.
27. Gronier B, Debonnel G. Involvement of sigma receptors in the modulation of the glutamatergic/NMDA neurotransmission in the dopaminergic systems. Eur J Pharmacol 1999; 368: 183-96.
28. Goldstein SR, Matsumoto RR, Thompson TL, Patrick RL, Bowen WD, Walker JM. Motor effects of two sigma ligands mediated by nigrostriatal dopamine neurons. Synapse 1989; 4: 254-8.
29. Minabe Y, Matsuno K, Ashby CR Jr. Acute and chronic administration of the selective sigma1 receptor agonist SA4503 significantly alters the activity of midbrain dopamine neurons in rats: An in vivo electrophysiological study. Synapse 1999; 33: 129-40.
30. Bermack JE, Debonnel G. Modulation of serotonergic neurotransmission by short-and long-term treatments with sigma ligands. Br J Pharmacol 2001, 134: 691-9.
31. Matsuno K, Matsunaga K, Mita S. Increase of extracellular acetylcholine level in rat frontal cortex induced by (+)Nallylnormetazocine as measured by brain microdialysis. Brain Res 1992; 575: 315-9.
32. Akunne HC, Whetzel SZ, Wiley JN, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology 1997; 36: 51-62.
33. Bastianetto S, Perrault G, Sanger DJ. Pharmacological evidence for the involvement of σ sites in DTG-induced contralateral circling in rats. Neuropharmacology 1995; 34: 107-14.
34. 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 1996; 306: 271-9.
35. Chaki S, Tanaka M, Muramatsu M, Otomo S. NE-100, a novel potent sigma ligand, preferentially binds to sigma 1 binding sites in guinea pig brain. Eur J Pharmacol 1994; 251: R1-2.
36. Stone JM, Arstad E, Erlandsson K, Waterhouse RN, Ell PJ, Pilowsky LS. [123I]TPCNE-a novel SPET tracer for the sigma-1 receptor: first human studies and in vivo haloperidol challenge. Synapse 2006; 60:109-17.
37. Bowen WD, Moses EL, Tolentino PJ, Walker JM. Metabolites of haloperidol display preferntial activity at σ receptors compared to dopamine D-2 receptors. Eur J Pharmacol 1990; 177: 111-8.
38. Bartoszyk GD, Bender HM, Hellmann J, Schnorr C, Seyfried CA. EMD 57445: a selective sigma receptor ligand with the profile of an atypical neuroleptic. CNS Drug Rev 1996; 2: 175-94.
39. Cobos EJ, del Pozo E, Baeyens JM. Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells. J Neurochem 2007; 102: 812-25.
40. Monnet FP, Debonnel G, de Montigny C. In vivo electrophysiological evidence for a selective modulation of N-methyl-Daspartate-induced neuronal activation in rat CA3 dorsal hippocampus by sigma ligands. J Pharmacol Exp Ther 1992; 261: 123-30.
41. Debonnel G, Bergeron R, Monnet FP, de Montigny C. Differential effects of sigma ligands on the N-methyl-D-aspartate response in the CA1 and CA3 regions of the dorsal hippocampus: effect of mossy fiber lesioning. Neuroscience 1996; 71: 977-87.
42. 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 1996, 16: 1193-202.
43. Matsumoto RR, Hewett KL, Pouw B, et al. Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology, 2001; 41: 878-86.
44. Weissman AD, Casanova MF, Kleinman JE, London ED, De Souza EB. Selective loss of cerebral cortical sigma, but not PCP binding sites in schizophrenia. Biol Psychiatry 1991; 29: 41-54.
45. Ishiguro H, Otsuki T, Toru M, et al. Association between polymorphisms in the type 1 sigma receptor gene and schizophrenia. Neurosci Lett 1998; 257: 45-8.
46. Satoh F, Miyatake R, Furukawa A, Suwaki H. Lack of association between sigma receptor gene variants and schizophrenia. Psychiatry Clin Neurosci 2004; 58: 359-63.
47. Skuza G, Rogóz Z. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep 2006; 58: 626-35.
48. Skuza G., Wedzony K. Behavioral pharmacology of sigma-ligands. Pharmacopsychiatry 2004; 37 (Suppl 3): S183-88
49. Maj J, Rogóz Z, Skuza G, Mazela H. Neuropharmacological profile of EMD 57445, a sigma receptor ligand with potential antipsychotic activity. Eur J Pharmacol 1996; 315: 235-43.
50. Tran TT, de Costa B, Matsumoto RR. Microinjection of sigma ligands into cranial nerve nuclei produces vacuous chewing in rats. Psychopharmacology 1998, 137: 191-200.
51. Okumura K, Ujike H, Akiyama K, Kuroda S. BMY-14802 reversed the sigma receptor agonist-induced neck dystonia in rats. J Neural Transm 1996;103: 1153-61.
52. Yamaguchi K, Nabeshima T, Ishikawa K, Yoshida S, Kameyama T. Phencyclidine-induced head-weaving and head-twitch through interaction with 5-HT1 and 5-HT2 receptors in reserpinized rats. Neuropharmacology 1987, 26: 1489-97.
53. Takahata R, Moghaddam B. Activation of glutamate neurotransmission in the prefrontal cortex sustains the motoric and dopaminergic effects of phencyclidine. Neuropsychopharmacology 2003, 28: 1117-24.
54. Wedzony K, Czyrak A, Mackowiak M, Fijal K. The impact of a competitive and a non-competitive NMDA receptor antagonist on dopaminergic neurotransmission in the rat ventral tegmental area and substantia nigra. Naunyn Schmiedebergs Arch Pharmacol 1996, 353: 517-27.
55. Takahashi S, Horikomi K, Kato T. MS-377, a novel selective sigma(1) receptor ligand, reverses phencyclidine-induced release of dopamine and serotonin in rat brain. Eur J Pharmacol 2001, 427: 211-9.
56. Takahashi S, Sonehara K, Takagi K, et al. Pharmacological profile of MS-377, a novel antipsychotic agent with selective affinity for sigma receptors. Psychopharmacology (Berl) 1999; 145: 295-302.
57. Karasawa J, Takahashi S, Takagi K, Horikomi K. Effects of sigma(1) receptor ligand MS-377 on D(2) antagonists-induced behaviors. Pharmacol Biochem Behav 2002, 73: 505-510.
58. Okuyama S, Imagawa Y, Tomisawa K. Behavioral evidence for modulation by sigma ligands of (+)MK-801-induced hyperlocomotion in monoamine-depleted mice. Neuropharmacology 1996; 35: 467-74.
59. Yamada S, Yamauchi K, Hisatomi S, Annoh N, Tanaka M. Effects of sigma(1) receptor ligand, MS-377 on apomorphine-or phencyclidine-induced disruption of prepulse inhibition of acoustic startle in rats. Eur J Pharmacol 2000; 402: 251-4.
60. Skuza G, Fijał K, Rogóz Z, Wedzony K. Effect of sigma (σ) receptor ligands on the dizocilpine-induced prepulse inhibition (PPI) deficit in mice. Pharmacol Rep 2010; 62(Suppl): S63.
61. Berardi F, Abate C, Ferorelli S, Colabufo NA, Perrone R. 1-Cyclohexylpiperazine and 3,3-dimethylpiperidine derivatives as sigma-1 (sigma1) and sigma-2 (sigma2) receptor ligands: a review. Cent Nerv Syst Agents Med Chem. 2009; 3:205-19.
62. Ujike H, Kuroda S, Otsuki S. σ Receptor antagonists block the development of sensitization to cocaine. Eur J Pharmacol 1996; 296, 123-8.
63. Guy W, Manov G, Wilson WH, et al. Psychotropic actions of BW 234U in the treatment of inpatient schizophrenics: a dose-range study. Drug Dev Res 1983; 3: 245-52.
64. Huber MT, Gotthardt U, Schreiber W, Krieg JC. Efficacy and safety of the sigma receptor ligand EMD 57445 (panamesine) in patients with schizophrenia: an open clinical trial. Pharmacopsychiatry 1999; 32: 68-72.
65. Schmidt A, Lebel L, Koe BK, Seeger T, Heym J. Sertraline potently displeaces (+)-[3H]3-PPP binding to σ sites in rat brain. Eur J Pharmacol 1989; 165: 335-6.
66. Itzhak Y, Kassim CO. Clorgyline displays high affinity for sigma binding sites in C57BL/6 mouse brain. Eur J Pharmacol 1990; 176: 107-8.
67. Leonard BE. The potential contribution of sigma receptors to antidepressant actions. In: Antidepressants: New Pharmacological Strategies. Ed. Skolnick P, Humana Press, Totowa, 1997, 159-72.
68. Shirayama Y, Nishikawa T, Umino A, Takahashi K. p-Chlorophenylalanine-reversible reduction of sigma binding sites by chronic imipramine treatment in rat brain. Eur J Pharmacol 1993; 237: 117-26.
69. Bergeron R, Debonnel G, De Montigny C. Modification of the Nmethyl-D-aspartate response by antidepressant sigma receptor ligands. Eur J Pharmacol 1993; 240: 319-23
70. Matsuno K, Kobayashi T, Tanaka MK, Mita S. σ1 Receptor subtype is involved in the relief of behavioral despair in the mouse forced swimming test. Eur J Pharmacol 1996; 312: 267-71.
71. Cryan JF, Mombereau C, Vassout A. The tail suspension test as a model for assessing antidepressant activity: review of pharmacological and genetic studies in mice. Neurosci Biobehav Rev 2005;29: 571-625.
72. 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 1998; 61: 247-53.
73. 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. 2001; 298: 1269-79.
74. Sánchez C, Meier E. Behavioural profile of SSRIs in animal models of depression, anxiety and aggression. Are they all alike? Psychopharmacology 1997; 129: 197-205.
75. 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 inthe rat. Int J Neuropsychopharmacol 2002; 5: 53-62.
76. Borsini F, Meli A. Is the forced swimming test a suitable model for revealing antidepressant activity? Psychopharmacology (Berl.) 1988; 94: 147-60.
77. Skuza G. Potential antidepressant activity of sigma ligands. Pol J Pharmacol 2003; 55: 923-34.
78. Bermack JE, Debonnel G. The role of sigma receptors in depression. J Pharmacol Sci 2005; 97: 317-36
79. Fishback JA, Robson MJ, Xu YT, Matsumoto RR. Sigma receptors: potential targets for a new class of antidepressant drug. Pharmacol Ther 2010; 127: 271-82.
80. Skuza G, Rogóz Z. Antidepressant-like effect of PRE-084, a selective sigma1 receptor agonist, in Albino Swiss and C57BL/6J mice. Pharmacol Rep 2009; 61:1179-83.
81. Reddy DS, Kaur G, Kulkarni SK. Sigma (σ1) receptor mediated antideprssant-like effects of neurosteroids in the Porsolt forced swim test. NeuroReport 1998; 9: 3069-73.
82. Tottori K, Miwa T, Uwahodo Y, et al. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology 2001; 41: 976-88.
83. Roman FJ, Pascaud X, Martin B, Vauché D, Junien JL. JO 1784, a potent and selective ligand for rat and mouse brain sigma-sites. J Pharm Pharmacol 1990; 42:439-40
84. Su TP, Wu XZ, Cone EJ, et al. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J Pharmacol Exp Ther 1991; 259: 543-50.
85. RB. Screen of receptor and uptake-site activity of hypericin component of St. John's wort reveals sigma receptor binding. Life Sci 1998; 62: 265-70.
86. Perfumi M, Panocka I, Ciccocioppo R, Vitali D, Froldi R, Massi M. Effects of a methanolic extract and a hyperforin-enriched CO2 extract of Hypericum perforatum on alcohol intake in rats. Alcohol Alcohol 2001; 36: 199-206.
87. Phan VL, Urani A, Romieu P, Maurice T. Strain differences in sigma(1) receptor-mediated behaviours are related to neurosteroid levels. Eur J Neurosci 2002; 15: 1523-34.
88. 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 1999; 81: 125-55.
89. Maurice T. Neurosteroids and sigma1 receptors, biochemical and behavioral relevance. Pharmacopsychiatry 2004; 37(Suppl 3): S171-82.
90. Monnet FP, Maurice T. The sigma1 protein as a target for the nongenomic effects of neuro(active)steroids: molecular, physiological, and behavioral aspects. J Pharmacol Sci 2006; 100: 93-118.
91. Phan VL, Miyamoto Y, Nabeshima T, Maurice T. Age-related expression of σ1 receptors and antidepressant efficacy of a selective agonist in the senescence-accelerated (SAM) mouse. J Neurosci Res 2005; 79: 561-72.
92. 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. 2002;134: 239-47.
93. Sabino V, Cottone P, Parylak SL, Steardo L, Zorrilla EP. Sigma-1 receptor knockout mice display a depressive-like phenotype. Behav Brain Res 2009; 198: 472-76.
94. Villard V, Meunier J, Chevallier N, Maurice T. Pharmacological interaction with the sigma1 (σ1)-receptor in the acute behavioral effects of antidepressants. J Pharmacol Sci 2011; 115: 279-92.
95. Dimitriou EC, Dimitriou CE. Buspirone augmentation of antidepressant therapy. J Clin Psychopharmacol 1998; 18: 465-9.
96. Shelton RC, Papakostas GI. Augmentation of antidepressants with atypical antipsychotics for treatment-resistant major depressive disorder. Acta Psychiatr Scand 2008; 117: 253-9.
97. [L. 5-HT1A receptor antagonists as putative adjuvants to antidepressants: preclinical and clinical evidence. IDrugs 1999; 2: 121-8.
98. Blier P, Bergeron R, de Montigny C. Selective activation of postsynaptic 5-HT1A receptors induces rapid antidepressant response. Neuropsychopharmacology 1997; 16: 333-8.
99. Rogóz Z, Skuza G, Maj J, Danysz W. Synergistic effects of uncompetitive NMDA receptor antagonists and antidepressant drugs in the forced swimming test in rats. Neuropharmacology 2002; 42: 1024-30.
100. Rogóz Z. Effects of co-treatment with mirtazapine and low doses of risperidone on immobility time in the forced swimming test in mice. Pharmacol Rep 2010; 62: 1191-6.
101. Kinney GG, Taber MT, Gribkoff VK. The augmentation hypothesis for improvement of antidepressant therapy: is pindolol a suitable candidate for testing the ability of 5HT1A receptor antagonists to enhance SSRI efficacy and onset latency? Mol Neurobiol 2000; 21: 137-52.
102. Millan MJ. The role of monoamines in the actions of established and "novel" antidepressant agents: a critical review. Eur J Pharmacol 2004; 500: 371-84.
103. Skuza G, Rogóz Z. Antidepressant-like effect of combined treatment with selective sigma receptor agonists and a 5-HT1A receptor agonist in the forced swimming test in rats. Pharmacol Rep 2007; 59: 773-7.
104. Rogóz Z, Skuza G. Mechanism of synergistic action following cotreatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep 2006; 58: 493-500.
105. 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 2007; 21: 85-92.
106. Dhir A, Kulkarni SK. Involvement of sigma-1 receptor modulation in the antidepressant action of venlafaxine. Neurosci Lett 2007; 420: 204-8.
107. Skuza G, Rogóz Z. The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. J Physiol Pharmacol 2006; 57, 217-29.
108. Skuza G, Sadaj W, Kabzinski M. Anti-immobility effect of the combined treatment with antidepressant drugs and memantine in the forced swim test in mice. The role of sigma(σ)1 receptors. 8th IBRO World Congress of Neuroscience, Florence, Italy, July 14-18, 2011, Abstracts, A501.
109. Peeters M, Romieu P, Maurice T, Su TP, Maloteaux JM, Hermans E. Involvement ofthe sigma 1 receptor in the modulation of dopaminergic transmission by amantadine. Eur J Neurosci 2004;19: 2212-20.
110. Skolnick P. Antidepressants for the new millennium. Eur J Pharmacol 1999; 375: 31-40.
111. Trullas R, Skolnick P. Functional antagonists of the NMDA receptor complex exhibit antidepressant action. Eur J Pharmacol 1990; 185: 1-10.
112. Nestler EJ, Barrot M, DiLeone RJ, Eisch AJ, Gold SJ, Monteggia LM. Neurobiology of depression. Neuron 2002; 34: 13-25.
113. Duman RS. Pathophysiology of depression: the concept of synaptic plasticity. Eur Psychiatry 2002; 17 Suppl 3: 306-10.
114. Siuciak JA, Lewis DR, Wiegand SJ, Lindsay RM. Antidepressantlike effect of brain-derived neurotrophic factor (BDNF). Pharmacol Biochem Behav 1997; 56:131-7
115. Yagasaki Y, Numakawa T, Kumamaru E, Hayashi T, Su TP, Kunugi H. Chronic antidepressants potentiate via sigma-1 receptors the brain-derived neurotrophic factor-induced signaling for glutamate release. J Biol Chem 2006; 281: 12941-9.
116. Racagni G, Popoli M. Cellular and molecular mechanisms in the long-term action of antidepressants. Dialogues Clin Neurosci 2008; 10: 385-400.
117. Martinowich K, Manji H, Lu B. New insights into BDNF function in depression and anxiety. Nat Neurosci 2007; 10: 1089-93.
118. Nishimura T, Ishima T, Iyo M, Hashimoto K. Potentiation of nerve growth factor-induced neurite outgrowth by fluvoxamine: role of sigma-1 receptors, IP3 receptors and cellular signaling pathways. PLoS One 2008; 3: e2558.
119. 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 2002; 303: 1227-37.
120. Kikuchi-Utsumi K, Nakaki T. Chronic treatment with a selective ligand for the sigma-1 receptor chaperone, SA4503, up-regulates BDNF protein levels in the rat hippocampus. Neurosci Lett 2008; 440: 19-22.
121. 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 2004; 53: 90-103.
122. th IBRO World Congress of Neuroscience, Florence, Italy, July 14-18, 2011, Abstracts, A503.
123. Wang D, Noda Y, Tsunekawa H, et al. Role of N-methyl-Daspartate receptors in antidepressant-like effects of sigma1 receptor agonist 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA-4503) in olfactory bulbectomized rats. J Pharmacol Exp Ther 2007; 322:1305-14.
124. 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 2002; 5:53-62.
125. Stahl SM. Antidepressant treatment of psychotic major depression: potential role of the sigma receptor. CNS Spectr 2005; 10: 319-23.
126. Goodman WK, Price LH, Rasmussen SA, Delgado PL, Heninger GR, Charney DS. Efficacy of fluvoxamine in obsessive-compulsive disorder: a double-blind comparison with placebo. Arch Gen Psychiatry 1989; 46: 36-44.
127. Lauterbach EC. Dextromethorphan as a potential rapid-acting antidepressant. Med Hypotheses 2011; 76: 717-19.
128. Kamei H, Kameyama T, Nabeshima T. (+)-SKF-10,047 and dextromethorphan ameliorate conditioned fear stress via dopaminergic systems linked to phenytoin-regulated sigma 1 sites. Eur J Pharmacol. 1996; 309: 149-58.
129. Noda Y, Kamei H, Kamei Y, Nagai T, Nishida M, Nabeshima T. Neurosteroids ameliorate conditioned fear stress: an association with sigma receptors. Neuropsychopharmacology 2000; 23:276-84.
130. Egashira N, Harada S, Okuno R, et al. Involvement of the sigma1 receptor in inhibiting activity of fluvoxamine on marble-burying behavior: comparison with paroxetine. Eur J Pharmacol 2007; 563: 149-54.
131. Gue M, Junien JL, Del Rio C, Bueno L. Neuropeptide Y and sigma ligand (JO 1784) suppress stress-induced colonic motor disturbances in rats through sigma and cholecystokinin receptors. J Pharmacol Exp Ther 1992; 261: 850-5.
132. Volz HP, Stoll KD. Clinical trials with sigma ligands. Pharmacopsychiatry 2004; 37: Suppl 3, S214-20.
133. Matsumoto RR, McCracken KA, Pouw B, Zhang Y, Bowen WD. Involvement of sigma receptors in the behavioral effects of cocaine: evidence from novel ligands andantisense oligodeoxynucleotides. Neuropharmacology 2002; 42: 1043-55.
134. Witkin JM, Terry P, Menkel M, et al. Effects of the selective sigma receptor ligand, 6-[6-(4-hydroxypiperidinyl)hexyloxy]-3-methylflavone (NPC 16377), on behavioral and toxic effects of cocaine. J Pharmacol Exp Ther 1993; 266: 473-82.
135. Senda T, Matsuno K, Okamoto K, Kobayashi T, Nakata K, Mita S. Ameliorating effects of SA4503, a novel σ1 receptor agonist, on memory impairments induced by cholinergic dysfunction in rats. Eur J Pharmacol 1996; 315: 1-10.
136. Matsuno K, Senda T, Matsunaga K, Mita S. Ameliorating effects of σ receptor ligands on the impairment of passive avoidance task in mice: involvement in the central acetylcholinergic system. Eur J Pharmacol 1994; 261:43-51.
137. Maurice T, Hiramatsu M, Itoh J, Kameyama T, Hasegawa T, Nabeshima T. Behavioral evidence for a modulating role of σ ligands in memory processes. I. Attenuation of dizocilpine (MK-801)-induced amnesia. Brain Res 1994; 647: 44-56.
138. Maurice T, Privat A. SA4503, a novel cognitive enhancer with σ1 receptor agonist properties, facilitates NMDA receptor-dependent learning in mice. Eur J Pharmacol 1997; 328: 9-18.
139. Zou L-B, Yamada K, Nabeshima T. σ Receptor ligands (+)SKF 10,047 and SA4503 improve dizocilpine-induced spatial memory deficits in rats. Eur J Pharmacol 1998; 355: 1-10.
140. 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 1999; 260: 5-8.
141. Hashimoto K, Fujita Y, Iyo M. Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of fluvoxamine: role of sigma1 receptors. Neuropsychopharmacology 2007; 32: 514-21.
142. 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)-1H-indoles. J Med Chem 1995; 38: 1998-2008.
143. Sanchez C, Papp M. The selective sigma2 ligand Lu 28-179 has an antidepressant-like profile in the rat chronic mild stress model of depression. Behavioural Pharmacology. 2000;11:117-24.
144. Vilner BJ, Bowen WD. Sigma receptor-active neuroleptics are cytotoxic to C6 glioma cells in culture. Eur J Pharmacol 1993; 244: 199-201.
145. Vilner BJ, de Costa BR, Bowen WD. Cytotoxic effect of sigma ligands: sigma receptor alterations in cellular morphology and viability. J Neurosci 1995; 15: 117-34.
146. Ostenfeld MS, Høyer-Hansen M, Bastholm L, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008; 4: 487-99.
147. Parry MJ, Alakoskela JM, Khandelia H, et al. High-affinity small molecule-phospholipid complex formation: binding of siramesine to phosphatidic acid. J Am Chem Soc 2008;130:12953-60.