Sigma 1 receptor: A new therapeutic target for pain

European Journal of Pharmacology

Volumn 716, Issue 1-3, 2013, Pages 78-93

  Zamanillo, Daniel ^a   Romero, Luz ^a   Merlos, Manuel ^a   Vela, José Miguel ^a  

^a National Institute of Bioinformatics   (Spain)

Author keywords

Analgesia; Neuropathic; Opioid; Pain; Sensitization; Sigma 1 receptor

Indexed keywords

ANALGESIC AGENT; CALCIUM ION; CHAPERONE; N [2 (3,4 DICHLOROPHENYL)ETHYL] 2 DIMETHYLAMINO N METHYLETHYLAMINE; NEUROSTEROID; OPIATE; OPIATE AGONIST; OPIATE ANTAGONIST; SIGMA 1 OPIATE RECEPTOR; SIGMA 1 OPIATE RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ADJUVANT THERAPY; ANALGESIA; CALCIUM SIGNALING; CELLULAR DISTRIBUTION; CENTRAL NERVOUS SYSTEM SENSITIZATION; COMBINATION CHEMOTHERAPY; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG TARGETING; HUMAN; HYPERALGESIA; MOLECULAR DYNAMICS; MONOTHERAPY; NERVE CELL PLASTICITY; NEUROMODULATION; NEUROPATHIC PAIN; NONHUMAN; PRIORITY JOURNAL; PROTEIN FUNCTION; RECEPTOR BLOCKING; REVIEW;

ANALGESIA; NEUROPATHIC; OPIOID; PAIN; SENSITIZATION; SIGMA 1 RECEPTOR;

ANALGESICS; ANIMALS; HUMANS; MOLECULAR TARGETED THERAPY; NOCICEPTION; PAIN; RECEPTORS, SIGMA;

EID: 84892543669     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2013.01.068     Document Type: Review

References (153)

1. Abadias, M., Escriche, M., Vaqué, A., Sust, M., Encina, G., 2000. Safety, tolerability and pharmacokinetics of single and multiple doses of a novel sigma-1 receptor antagonist in three randomized phase I studies. Br. J. Clin. Pharmacol. 75, 103-117.
2. Alonso, G., Phan, V., Guillemain, I., Saunier, M., Legrand, A., Anoal, M., Maurice, T., 2000. Immunocytochemical localization of the sigma(1) receptor in the adult rat central nervous system. Neuroscience 97, 155-170.
3. Aydar, E., Palmer, C.P., Djamgoz, M.B., 2004. Sigma receptors and cancer: possible involvement of ion channels. Cancer Res. 64, 5029-5035.
4. Aydar, E., Palmer, C.P., Klyachko, V.A., Jackson, M.B., 2002. The sigma receptor as a ligand-regulated auxiliary potassium channel subunit. Neuron 34, 399-410.
5. Bergeron, R., De Montigny, C., Debonnel, G., 1996. Potentiation of neuronal NMDA response induced by dehydroepiandrosterone and its suppression by progesterone: effects mediated via sigma receptors. J. Neurosci. 16, 1193-1202.
6. Bergeron, R., De Montigny, C., Debonnel, G., 1997. Effect of short-term and longterm 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.
7. Bermack, J.E., Debonnel, G., 2005. The role of sigma receptors in depression. J. Pharmacol. Sci. 97, 317-336.
8. Bermack, J.E., Haddjeri, N., Debonnel, G., 2004. Effects of the potential antidepressant OPC-14523 [1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5- methoxy-3,4-dihydro-2-quinolino ne monomethanesulfonate] a combined sigma and 5-HT1A ligand: modulation of neuronal activity in the dorsal raphe nucleus. J. Pharmacol. Exp. Ther. 310, 578-583.
9. Bhuiyan, M.S., Fukunaga, K., 2011. Targeting sigma-1 receptor signaling by endogenous ligands for cardioprotection. Expert Opin. Ther. Targets 15, 145-155.
10. Brent, P.J., Haynes, H., Jarvie, P.E., Mudge, L., Sim, A.T., Dunkley, P.R., 1995. Phosphorylation of synapsin I and dynamin in rat forebrain synaptosomes: modulation by sigma (sigma) ligands. Neurosci. Lett. 191, 71-74.
11. Bridges, D., Thompson, S.W., Rice, A.S., 2001. Mechanisms of neuropathic pain. Br. J. Anaesth. 87, 12-26.
12. Bura, A.S., Guegan, T., Zamanillo, D., Vela, J.M., Maldonado, R., 2012. Operant self-administration of a sigma ligand improves nociceptive and emotional manifestations of neuropathic pain. Eur. J. Pain, http://dx.doi.org/10.1002/j. 1532-2149.2012.00251.x.
13. Cahill, M.A., 2007. Progesterone receptor membrane component 1: an integrative review. J. Steroid Biochem. Mol. Biol. 105, 16-36.
14. Caudle, R.M., Perez, F.M., Valle-Pinero, A.Y., Iadarola, M.J., 2005. Spinal cord NR1 serine phosphorylation and NR2B subunit suppression following peripheral inflammation. Mol. Pain 1, 25.
15. Cendán, C.M., Pujalte, J.M., Portillo-Salido, E., Baeyens, J.M., 2005a. Antinociceptive effects of haloperidol and its metabolites in the formalin test in mice. Psychopharmacology (Berl) 182, 485-493.
16. Cendán, C.M., Pujalte, J.M., Portillo-Salido, E., Montoliu, L., Baeyens, J.M., 2005b. Formalin-induced pain is reduced in sigma(1) receptor knockout mice. Eur. J. Pharmacol. 511, 73-74.
17. Chaki, S., Okuyama, S., Ogawa, S., Tomisawa, K., 1998. Regulation of NMDA-induced [3H]dopamine release from rat hippocampal slices through sigma-1 binding sites. Neurochem. Int. 33, 29-34.
18. Chen, H.S., Lipton, S.A., 2006. The chemical biology of clinically tolerated NMDA receptor antagonists. J. Neurochem. 97, 1611-1626.
19. Cheng, Z.X., Lan, D.M., Wu, P.Y., Zhu, Y.H., Dong, Y., Ma, L., Zheng, P., 2008. Neurosteroid dehydroepiandrosterone sulphate inhibits persistent sodium currents in rat medial prefrontal cortex via activation of sigma-1 receptors. Exp. Neurol. 210, 128-136.
20. Chien, C.C., Pasternak, G.W., 1993. Functional antagonism of morphine analgesia by (+)-pentazocine: evidence for an anti-opioid sigma 1 system. Eur. J. Pharmacol. 250, R7-R8.
21. Chien, C.C., Pasternak, G.W., 1994. Selective antagonism of opioid analgesia by a sigma system. J. Pharmacol. Exp. Ther. 271, 1583-1590.
22. Chien, C.C., Pasternak, G.W., 1995a. (-)-Pentazocine analgesia in mice: interactions with a sigma receptor system. Eur. J. Pharmacol. 294, 303-308.
23. Chien, C.C., Pasternak, G.W., 1995b. Sigma antagonists potentiate opioid analgesia in rats. Neurosci. Lett. 190, 137-139.
24. Cobos, E.J., Baeyens, J.M., Del Pozo, E., 2005. Phenytoin differentially modulates the affinity of agonist and antagonist ligands for sigma 1 receptors of guinea pig brain. Synapse 55, 192-195.
25. Cobos, E.J., Del Pozo, E., Baeyens, J.M., 2007. Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells. J. Neurochem. 102, 812-825.
26. Cobos, E.J., Entrena, J.M., Nieto, F.R., Cendán, C.M., Del Pozo, E., 2008. Pharmacology and therapeutic potential of sigma(1) receptor ligands. Curr. Neuropharmacol. 6, 344-366.
27. Coderre, T.J., Kumar, N., Lefebvre, C.D., Yu, J.S., 2005. Evidence that gabapentin reduces neuropathic pain by inhibiting the spinal release of glutamate. J. Neurochem. 94, 1131-1139.
28. Colclough, G., McLarney, J.T., Sloan, P.A., McCoun, K.T., Rose, G.L., Grider, J.S., Steyn, P., 2008. Epidural haloperidol enhances epidural morphine analgesia: three case reports. J. Opioid. Manag. 4, 163-166.
29. Dableh, L.J., Henry, J.L., 2011. Progesterone prevents development of neuropathic pain in a rat model: timing and duration of treatment are critical. J. Pain Res. 4, 91-101.
30. Daw, J.L., Cohen-Cole, S.A., 1981. Haloperidol analgesia. South. Med. J. 74, 364-365.
31. de la Puente, B., Nadal, X., Portillo-Salido, E., Sánchez-Arroyos, R., Ovalle, S., Palacios, G., Muro, A., Romero, L., Entrena, J.M., Baeyens, J.M., López-García, J.A., Maldonado, R., Zamanillo, D., Vela, J.M., 2009. Sigma-1 receptors regulate activity-induced spinal sensitization and neuropathic pain after peripheral nerve injury. Pain 145, 294-303.
32. Díaz, J.L., Zamanillo, D., Corbera, J., Baeyens, J.M., Maldonado, R., Pericàs, M.A., Vela, J.M., Torrens, A., 2009. Selective sigma-1 (sigma1) receptor antagonists: emerging target for the treatment of neuropathic pain. Cent. Nerv. Syst. Agents Med. Chem. 9, 172-183.
33. Díaz, J.L., Cuberes, R., Berrocal, J., Contijoch, M., Christmann, U., Fernández, A., Port, A., Holenz, J., Buschmann, H., Laggner, C., Serafini, M.T., Burgueño, J., Zamanillo, D., Merlos, M., Vela, J.M., Almansa, C., 2012. Synthesis and biological evaluation of the 1-arylpyrazole class of s(1) receptor antagonists: identification of 4-{2-[5-methyl-1- (naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J. Med. Chem. 55, 8211-8224.
34. Dickenson, A.H., Chapman, V., Green, G.M., 1997. The pharmacology of excitatory and inhibitory amino acid-mediated events in the transmission and modulation of pain in the spinal cord. Gen. Pharmacol. 28, 633-638.
35. Dickenson, A.H., Sullivan, A.F., 1987. Evidence for a role of the NMDA receptor in the frequency dependent potentiation of deep rat dorsal horn nociceptive neurones following C fibre stimulation. Neuropharmacology 26, 1235-1238.
36. Eide, P.K., 2000. Wind-up and the NMDA receptor complex from a clinical perspective. Eur. J. Pain 4, 5-15.
37. Entrena, J.M., Cobos, E.J., Nieto, F.R., Cendán, C.M., Baeyens, J.M., Del Pozo, E., 2009a. Antagonism by haloperidol and its metabolites of mechanical hypersensitivity induced by intraplantar capsaicin in mice: role of sigma-1 receptors. Psychopharmacology (Berl) 205, 21-33.
38. Entrena, J.M., Cobos, E.J., Nieto, F.R., Cendán, C.M., Gris, G., Del Pozo, E., Zamanillo, D., Baeyens, J.M., 2009b. 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.
39. Gao, X., Kim, H.K., Chung, J.M., Chung, K., 2005. Enhancement of NMDA receptor phosphorylation of the spinal dorsal horn and nucleus gracilis neurons in neuropathic rats. Pain 116, 62-72.
40. Gear, R.W., Lee, J.S., Miaskowski, C., Gordon, N.C., Paul, S.M., Levine, J.D., 2006. Neuroleptics antagonize nalbuphine antianalgesia. J. Pain 7, 187-191.
41. Guertin, P., 2008. Can the spinal cord learn and remember? ScientificWorldJournal 8, 757-761.
42. Guitart, X., Codony, X., Monroy, X., 2004. Sigma receptors: biology and therapeutic potential. Psychopharmacology (Berl) 174, 301-319.
43. Ha, Y., Dun, Y., Thangaraju, M., Duplantier, J., Dong, Z., Liu, K., Ganapathy, V., Smith, S.B., 2011. Sigma receptor 1modulates endoplasmic reticulumstress in retinal neurons. Invest. Ophthalmol. Vis. Sci. 52, 527-540.
44. Hanner, M., Moebius, F.F., Flandorfer, A., Knaus, H.G., Striessnig, J., Kempner, E., Glossmann, H., 1996. Purification, molecular cloning, and expression of the mammalian sigma1-binding site. Proc. Nat. Acad. Sci. U.S.A. 93, 8072-8077.
45. Harada, Y., Hara, H., Sukamoto, T., 1994. Receptor binding profiles of KB-5492, a novel anti-ulcer agent, at sigma receptors in guinea-pig brain. Eur. J. Pharmacol. 256, 321-328.
46. ++ mobilization by N-methyl-D-aspartate in primary culture of rat frontal cortical neurons. J. Pharmacol. Exp. Ther. 275, 207-214.
47. Hayashi, T., Maurice, T., Su, T.P., 2000. Ca(2+) signaling via sigma(1)-receptors: novel regulatory mechanism affecting intracellular Ca(2+) concentration. J. Pharmacol. Exp. Ther. 293, 788-798.
48. Hayashi, T., Su, T., 2005a. The sigma receptor: evolution of the concept in neuropsychopharmacology. Curr. Neuropharmacol. 3, 267-280.
49. Hayashi, T., Su, T.P., 2001. Regulating ankyrin dynamics: roles of sigma-1 receptors. Proc. Nat. Acad. Sci. U.S.A. 98, 491-496.
50. Hayashi, T., Su, T.P., 2004. Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs 18, 269-284.
51. Hayashi, T., Su, T.P., 2005b. 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.
52. Hayashi, T., Su, T.P., 2007. Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca(2+) signaling and cell survival. Cell 131, 596-610.
53. Hayashi, T., Su, T.P., 2010. Cholesterol at the endoplasmic reticulum: roles of the sigma-1 receptor chaperone and implications thereof in human diseases. Subcell. Biochem. 51, 381-398.
54. Hayashi, T., Tsai, S.Y., Mori, T., Fujimoto, M., Su, T.P., 2011. Targeting ligand-operated chaperone sigma-1 receptors in the treatment of neuropsychiatric disorders. Expert Opin. Ther. Targets 15, 557-577.
55. Hellewell, S.B., Bruce, A., Feinstein, G., Orringer, J., Williams, W., Bowen, W.D., 1994. 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.
56. Herrero, J.F., Laird, J.M., López-García, J.A., 2000. Wind-up of spinal cord neurones and pain sensation: much ado about something? Prog. Neurobiol. 61, 169-203.
57. Hiramatsu, M., Hoshino, T., 2004. Involvement of kappa-opioid receptors and sigma receptors in memory function demonstrated using an antisense strategy. Brain Res. 1030, 247-255.
58. Hiramatsu, M., Hoshino, T., Kameyama, T., Nabeshima, T., 2002. Involvement of kappa-opioid and sigma receptors in short-term memory in mice. Eur. J. Pharmacol. 453, 91-98.
59. Junien, J.L., Roman, F.J., Brunelle, G., Pascaud, X., 1991. JO1784, a novel sigma ligand, potentiates [3H]acetylcholine release from rat hippocampal slices. Eur. J. Pharmacol. 200, 343-345.
60. Kest, B., Mogil, J.S., Sternberg, W.F., Pechnick, R.N., Liebeskind, J.C., 1995a. 1,3-Di-o-tolylguanidine (DTG) differentially affects acute and tonic formalin pain: antagonism by rimcazole. Pharmacol. Biochem. Behav. 52, 175-178.
61. Kest, B., Mogil, J.S., Sternberg, W.F., Pechnick, R.N., Liebeskind, J.C., 1995b. Antinociception following 1,3,-di-o-tolylguanidine, a selective sigma receptor ligand. Pharmacol. Biochem. Behav. 50, 587-592.
62. Kibaly, C., Meyer, L., Patte-Mensah, C., Mensah-Nyagan, A.G., 2008. Biochemical and functional evidence for the control of pain mechanisms by dehydroepiandrosterone endogenously synthesized in the spinal cord. FASEB J. 22, 93-104.
63. Kim, F.J., Kovalyshyn, I., Burgman, M., Neilan, C., Chien, C.C., Pasternak, G.W., 2010. Sigma 1 receptor modulation of G-protein-coupled receptor signaling: potentiation of opioid transduction independent from receptor binding. Mol. Pharmacol. 77, 695-703.
64. Kim, H.W., Kwon, Y.B., Roh, D.H., Yoon, S.Y., Han, H.J., Kim, K.W., Beitz, A.J., Lee, J.H., 2006. 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.
65. Kim, H.W., Roh, D.H., Yoon, S.Y., Seo, H.S., Kwon, Y.B., Han, H.J., Kim, K.W., Beitz, A.J., Lee, J.H., 2008. Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKC- and PKA-dependent phosphorylation of the NR1 subunit in mice. Br. J. Pharmacol. 154, 1125-1134.
66. King, M., Pan, Y.X., Mei, J., Chang, A., Xu, J., Pasternak, G.W., 1997. Enhanced kappa-opioid receptor-mediated analgesia by antisense targeting the sigma1 receptor. Eur. J. Pharmacol. 331, R5-R6.
67. Kitaichi, K., Chabot, J.G., Moebius, F.F., Flandorfer, A., Glossmann, H., Quirion, R., 2000. Expression of the purported sigma(1) (sigma(1)) receptor in the mammalian brain and its possible relevance in deficits induced by antagonism of the NMDA receptor complex as revealed using an antisense strategy. J. Chem. Neuroanat. 20, 375-387.
68. Kobayashi, T., Matsuno, K., Nakata, K., Mita, S., 1996. Enhancement of acetylcholine release by SA4503, a novel sigma 1 receptor agonist, in the rat brain. J. Pharmacol. Exp. Ther. 279, 106-113.
69. Kwon, Y.B., Jeong, Y.C., Kwon, J.K., Son, J.S., Kim, K.W., 2009. The antinociceptive effect of sigma-1 receptor antagonist, BD1047, in a capsaicin induced headache model in rats. Korean J. Physiol. Pharmacol. 13, 425-429.
70. Langa, F., Codony, X., Tovar, V., Lavado, A., Giménez, E., Cozar, P., Cantero, M., Dordal, A., Hernández, E., Pérez, R., Monroy, X., Zamanillo, D., Guitart, X., Montoliu, L., 2003. Generation and phenotypic analysis of sigma receptor type I (sigma 1) knockout mice. Eur. J. Neurosci. 18, 2188-2196.
71. Losel, R.M., Besong, D., Peluso, J.J., Wehling, M., 2008. Progesterone receptor membrane component 1-many tasks for a versatile protein. Steroids 73, 929-934.
72. + channels in rat neurohypophysial terminals requires neither G-protein nor ATP. J. Physiol. 526 (Pt 3), 527-539.
73. Majewska, M.D., 1990. Steroid regulation of the GABAA receptor: ligand binding, chloride transport and behaviour. Ciba Found. Symp. 153, 83-97.
74. Majewska, M.D., Mienville, J.M., Vicini, S., 1988. Neurosteroid pregnenolone sulfate antagonizes electrophysiological responses to GABA in neurons. Neurosci. Lett. 90, 279-284.
75. Mancuso, R., Oliván, S., Rando, A., Casas, C., Osta, R., Navarro, X., 2012. Sigma-1R agonist improves motor function and motoneuron survival in ALS mice. Neurotherapeutics 9, 814-826.
76. Marrazzo, A., Parenti, C., Scavo, V., Ronsisvalle, S., Scoto, G.M., Ronsisvalle, G., 2006. In vivo evaluation of (+)-MR200 as a new selective sigma ligand modulating MOP, DOP and KOP supraspinal analgesia. Life Sci. 78, 2449-2453.
77. Martina, M., Turcotte, M.E., Halman, S., Bergeron, R., 2007. The sigma-1 receptor modulates NMDA receptor synaptic transmission and plasticity via SK channels in rat hippocampus. J. Physiol. 578, 143-157.
78. Matsumoto, R.R., Bowen, W.D., Tom, M.A., Vo, V.N., Truong, D.D., De Costa, B.R., 1995. Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur. J. Pharmacol. 280, 301-310.
79. Matsuno, K., Matsunaga, K., Senda, T., Mita, S., 1993. Increase in extracellular acetylcholine level by sigma ligands in rat frontal cortex. J. Pharmacol. Exp. Ther. 265, 851-859.
80. Maurice, T., Su, T.P., 2009. The pharmacology of sigma-1 receptors. Pharmacol. Ther. 124, 195-206.
81. Megalizzi, V., Decaestecker, C., Debeir, O., Spiegl-Kreinecker, S., Berger, W., Lefranc, F., Kast, R.E., Kiss, R., 2009. 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.
82. Mei, J., Pasternak, G.W., 2002. Sigma1 receptor modulation of opioid analgesia in the mouse. J. Pharmacol. Exp. Ther. 300, 1070-1074.
83. Mei, J., Pasternak, G.W., 2007. Modulation of brainstem opiate analgesia in the rat by sigma 1 receptors: a microinjection study. J. Pharmacol. Exp. Ther. 322, 1278-1285.
84. Mensah-Nyagan, A.G., Kibaly, C., Schaeffer, V., Venard, C., Meyer, L., Patte-Mensah, C., 2008. Endogenous steroid production in the spinal cord and potential involvement in neuropathic pain modulation. J. Steroid Biochem. Mol. Biol. 109, 286-293.
85. Meunier, J., Hayashi, T., 2010. 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.
86. Moebius, F.F., Bermoser, K., Reiter, R.J., Hanner, M., Glossmann, H., 1996. Yeast sterol C8-C7 isomerase: identification and characterization of a high-affinity binding site for enzyme inhibitors. Biochemistry 35, 16871-16878.
87. Moebius, F.F., Reiter, R.J., Hanner, M., Glossmann, H., 1997a. 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.
88. Moebius, F.F., Striessnig, J., Glossmann, H., 1997b. The mysteries of sigma receptors: new family members reveal a role in cholesterol synthesis. Trends Pharmacol. Sci. 18, 67-70.
89. Monnet, F.P., De Costa, B.R., Bowen, W.D., 1996. Differentiation of sigma ligand-activated receptor subtypes that modulate NMDA-evoked [3H]-noradrenaline release in rat hippocampal slices. Br. J. Pharmacol. 119, 65-72.
90. Monnet, F.P., Debonnel, G., Junien, J.L., De Montigny, C., 1990. N-methyl-D-aspartate-induced neuronal activation is selectively modulated by sigma receptors. Eur. J. Pharmacol. 179, 441-445.
91. Monnet, F.P., Mahe, V., Robel, P., Baulieu, E.E., 1995. Neurosteroids, via sigma receptors, modulate the [3H]norepinephrine release evoked by N-methyl-D-aspartate in the rat hippocampus. Proc. Nat. Acad. Sci. U.S.A. 92, 3774-3778.
92. Monnet, F.P., Maurice, T., 2006. 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.
93. Monnet, F.P., Morin-Surun, M.P., Leger, J., Combettes, L., 2003. Protein kinase C-dependent potentiation of intracellular calcium influx by sigma1 receptor agonists in rat hippocampal neurons. J. Pharmacol. Exp. Ther. 307, 705-712.
94. Morin-Surun, M.P., Collin, T., Denavit-Saubié, M., Baulieu, E.E., Monnet, F.P., 1999. Intracellular sigma1 receptor modulates phospholipase C and protein kinase C activities in the brainstem. Proc. Nat. Acad. Sci. U.S.A. 96, 8196-8199.
95. Mtchedlishvili, Z., Kapur, J., 2003. A presynaptic action of the neurosteroid pregnenolone sulfate on GABAergic synaptic transmission. Mol. Pharmacol. 64, 857-864.
96. Murakami, K., Fellous, A., Baulieu, E.E., Robel, P., 2000. Pregnenolone binds to microtubule-associated protein 2 and stimulates microtubule assembly. Proc. Nat. Acad. Sci. U.S.A. 97, 3579-3584.
97. Navarro, G., Moreno, E., Aymerich, M., Marcellino, D., McCormick, P.J., Mallol, J., Cortés, A., Casadó, V., Canela, E.I., Ortiz, J., Fuxe, K., Lluís, C., Ferré, S., Franco, R., 2010. Direct involvement of sigma-1 receptors in the dopamine D1 receptor-mediated effects of cocaine. Proc. Nat. Acad. Sci. U.S.A. 107, 18676-18681.
98. Nieto, F.R., Cendán, C.M., Sánchez-Fernández, C., Cobos, E.J., Entrena, J.M., Tejada, M.A., Zamanillo, D., Vela, J.M., Baeyens, J.M., 2012. Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice. J. Pain 13, 1107-1121.
99. Novakova, M., Ela, C., Barg, J., Vogel, Z., Hasin, Y., Eilam, Y., 1995. Inotropic action of sigma receptor ligands in isolated cardiac myocytes from adult rats. Eur. J. Pharmacol. 286, 19-30.
100. Novakova, M., Ela, C., Bowen, W.D., Hasin, Y., Eilam, Y., 1998. Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes. Eur. J. Pharmacol. 353, 315-327.
101. Ohsawa, M., Carlsson, A., Asato, M., Koizumi, T., Nakanishi, Y., Fransson, R., Sandstrom, A., Hallberg, M., Nyberg, F., Kamei, J., 2011a. The dipeptide Phe-Phe amide attenuates signs of hyperalgesia, allodynia and nociception in diabetic mice using a mechanism involving the sigma receptor system. Mol. Pain 7, 85.
102. Ohsawa, M., Carlsson, A., Asato, M., Koizumi, T., Nakanishi, Y., Fransson, R., Sandstrom, A., Hallberg, M., Nyberg, F., Kamei, J., 2011b. The effect of substance P1-7 amide on nociceptive threshold in diabetic mice. Peptides 32, 93-98.
103. Ohsawa, M., Hayashi, S.S., Kamei, J., 2010. Effect of acute topical application of (+)-pentazocine on the mechanical allodynia in diabetic mice. Eur. J. Pharmacol. 641, 49-53.
104. Ossipov, M.H., Lai, J., Malan Jr., T.P., Porreca, F., 2000. Spinal and supraspinal mechanisms of neuropathic pain. Ann. N.Y. Acad. Sci. 909, 12-24.
105. Palacios, G., Muro, A., Verdú, E., Pumarola, M., Vela, J.M., 2004. Immunohistochemical localization of the sigma1 receptor in Schwann cells of rat sciatic nerve. Brain Res. 1007, 65-70.
106. Pan, Y.X., Mei, J., Xu, J., Wan, B.L., Zuckerman, A., Pasternak, G.W., 1998. Cloning and characterization of a mouse sigma1 receptor. J. Neurochem. 70, 2279-2285.
107. Pasternak, G.W., Carroll-Buatti, M., Spiegel, K., 1981. The binding and analgesic properties of a sigma opiate, SKF 10,047. J. Pharmacol. Exp. Ther. 219, 192-198.
108. Patte-Mensah, C., Mensah-Nyagan, A.G., 2008. Peripheral neuropathy and neurosteroid formation in the central nervous system. Brain Res. Rev. 57, 454-459.
109. Peeters, M., Romieu, P., Maurice, T., Su, T.P., Maloteaux, J.M., Hermans, E., 2004. Involvement of the sigma 1 receptor in the modulation of dopaminergic transmission by amantadine. Eur. J. Neurosci. 19, 2212-2220.
110. Penas, C., Pascual-Font, A., Mancuso, R., Forés, J., Casas, C., Navarro, X., 2011. 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.
111. Piergentili, A., Amantini, C., Del Bello, F., Giannella, M., Mattioli, L., Palmery, M., Perfumi, M., Pigini, M., Santoni, G., Tucci, P., Zotti, M., Quaglia, W., 2010. Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. J. Med. Chem. 53, 1261-1269.
112. Plassart-Schiess, E., Baulieu, E.E., 2001. Neurosteroids: recent findings. Brain Res. Rev. 37, 133-140.
113. Prezzavento, O., Parenti, C., Marrazzo, A., Ronsisvalle, S., Vittorio, F., Arico, G., Scoto, G.M., Ronsisvalle, G., 2008. A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82, 549-553.
114. Roh, D.H., Choi, S.R., Yoon, S.Y., Kang, S.Y., Moon, J.Y., Kwon, S.G., Han, H.J., Beitz, A.J., Lee, J.H., 2011. Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylation. Br. J. Pharmacol. 163, 1707-1720.
115. Roh, D.H., Kim, H.W., Yoon, S.Y., Seo, H.S., Kwon, Y.B., Kim, K.W., Han, H.J., Beitz, A.J., Lee, J.H., 2008a. Intrathecal administration of sigma-1 receptor agonists facilitates nociception: involvement of a protein kinase C-dependent pathway. J. Neurosci. Res. 86, 3644-3654.
116. Roh, D.H., Kim, H.W., Yoon, S.Y., Seo, H.S., Kwon, Y.B., Kim, K.W., Han, H.J., Beitz, A.J., Na, H.S., Lee, J.H., 2008b. 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.
117. Roh, D.H., Yoon, S.Y., Seo, H.S., Kang, S.Y., Moon, J.Y., Song, S., Beitz, A.J., Lee, J.H., 2010. Sigma-1 receptor-induced increase in murine spinal NR1 phosphorylation is mediated by the PKCalpha and epsilon, but not the PKCzeta, isoforms. Neurosci. Lett. 477, 95-99.
118. Rohe, H.J., Ahmed, I.S., Twist, K.E., Craven, R.J., 2009. PGRMC1 (progesterone receptor membrane component 1): a targetable protein with multiple functions in steroid signaling, P450 activation and drug binding. Pharmacol. Ther. 121, 14-19.
119. Romero, L., Zamanillo, D., Nadal, X., Sánchez-Arroyos, R., Rivera-Arconada, I., Dordal, A., Montero, A., Muro, A., Bura, A., Segalés, C., Laloya, M., Hernández, E., Portillo-Salido, E., Escriche, M., Codony, X., Encina, G., Burgueño, J., Merlos, M., Baeyens, J., Giraldo, J., López-García, J., Maldonado, R., Plata-Salamán, C., Vela, J.M., 2012. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br. J. Pharmacol 166, 2289-2306.
120. Ronsisvalle, G., Marrazzo, A., Prezzavento, O., Pasquinucci, L., Falcucci, B., Di Toro, R.D., Spampinato, S., 2000. Substituted 1-phenyl-2-cyclopropylmethylamines with high affinity and selectivity for sigma sites. Bioorg. Med. Chem. 8, 1503-1513.
121. Ronsisvalle, G., Prezzavento, O., Marrazzo, A., Vittorio, F., Bousquet, E., Di Toro, R., Spampinato, S., 2001. 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.
122. Rossi, G.C., Pasternak, G.W., Bodnar, R.J., 1993. Synergistic brainstem interactions for morphine analgesia. Brain Res. 624, 171-180.
123. Rossi, G.C., Pasternak, G.W., Bodnar, R.J., 1994. Mu and delta opioid synergy between the periaqueductal gray and the rostro-ventral medulla. Brain Res. 665, 85-93.
124. Rygh, L.J., Tjølsen, A., Hole, K., Svendsen, F., 2002. Cellular memory in spinal nociceptive circuitry. Scand. J. Psychol. 43, 153-159.
125. Sandkuhler, J., 2000. Learning and memory in pain pathways. Pain 88, 113-118.
126. Senda, T., Matsuno, K., Okamoto, K., Kobayashi, T., Nakata, K., Mita, S., 1996. Ameliorating effect of SA4503, a novel sigma 1 receptor agonist, on memory impairments induced by cholinergic dysfunction in rats. Eur. J. Pharmacol. 315, 1-10.
127. Smith, S.S., 1991. Progesterone administration attenuates excitatory amino acid responses of cerebellar Purkinje cells. Neuroscience 42, 309-320.
128. Soliman, A.C., Yu, J.S., Coderre, T.J., 2005. mGlu and NMDA receptor contributions to capsaicin-induced thermal and mechanical hypersensitivity. Neuropharmacology 48, 325-332.
129. Son, J.S., Kwon, Y.B., 2010. 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.
130. Spruce, B.A., Campbell, L.A., McTavish, N., Cooper, M.A., Appleyard, M.V., O'Neill, M., Howie, J., Samson, J., Watt, S., Murray, K., McLean, D., Leslie, N.R., Safrany, S.T., Ferguson, M.J., Peters, J.A., Prescott, A.R., Box, G., Hayes, A., Nutley, B., Raynaud, F., Downes, C.P., Lambert, J.J., Thompson, A.M., Eccles, S., 2004. 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.
131. Su, T.P., Hayashi, T., 2003. 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.
132. Su, T.P., Hayashi, T., Maurice, T., Buch, S., Ruoho, A.E., 2010. The sigma-1 receptor chaperone as an inter-organelle signaling modulator. Trends Pharmacol. Sci. 31, 557-566.
133. Suzuki, R., Matthews, E.A., Dickenson, A.H., 2001. Comparison of the effects of MK-801, ketamine and memantine on responses of spinal dorsal horn neurones in a rat model of mononeuropathy. Pain 91, 101-109.
134. Takebayashi, M., Hayashi, T., Su, T.P., 2002. Nerve growth factor-induced neurite sprouting in PC12 cells involves sigma-1 receptors: implications for antidepressants. J. Pharmacol. Exp. Ther. 303, 1227-1237.
135. Tsai, S.Y., Hayashi, T., Mori, T., Su, T.P., 2009a. Sigma-1 receptor chaperones and diseases. Cent. Nerv. Syst. Agents Med. Chem. 9, 184-189.
136. Tsai, S.Y., Hayashi, T., Harvey, B.K., Wang, Y., Wu, W.W., Shen, R.F., Zhang, Y., Becker, K.G., Hoffer, B.J., Su, T.P., 2009b. Sigma-1 receptors regulate hippocampal dendritic spine formation via a free radical-sensitive mechanism involving Rac1xGTP pathway. Proc. Nat. Acad. Sci. U.S.A. 106, 22468-22473.
137. Turk, D.C., Wilson, H.D., Cahana, A., 2011. Treatment of chronic non-cancer pain. Lancet 377, 2226-2235.
138. Ueda, H., Inoue, M., Yoshida, A., Mizuno, K., Yamamoto, H., Maruo, J., Matsuno, K., Mita, S., 2001. Metabotropic neurosteroid/sigma-receptor involved in stimulation of nociceptor endings of mice. J. Pharmacol. Exp. Ther. 298, 703-710.
139. Vela, J.M., Abadias, M., Escriche, M., Sust, M., Farrán, R., Encabo, M., Vidal, A., Romero, L., Zamanillo, D., Encina, G., Plata, C.R., 2010. Characterization of a New Selective Sigma-1 Receptor Antagonist (S1RA) that Inhibits Neuropathic Pain and Potentiates Opioid Analgesia - From Rodents to Human. BENZON SYMPOSIUM Copenhagen, October 4-7.
140. Walker, J.M., Bowen, W.D., Goldstein, S.R., Roberts, A.H., Patrick, S.L., Hohmann, A. G., DeCosta, B., 1992. Autoradiographic distribution of [3H](+)-pentazocine and [3H]1,3-di-o-tolylguanidine (DTG) binding sites in guinea pig brain: a comparative study. Brain Res. 581, 33-38.
141. Wolfe Jr., S.A., Culp, S.G., De Souza, E.B., 1989. Sigma-receptors in endocrine organs: identification, characterization, and autoradiographic localization in rat pituitary, adrenal, testis, and ovary. Endocrinology 124, 1160-1172.
142. Wolfe Jr., S.A., Ha, B.K., Whitlock, B.B., Saini, P., 1997. Differential localization of three distinct binding sites for sigma receptor ligands in rat spleen. J. Neuroimmunol. 72, 45-58.
143. Woolf, C.J., Mannion, R.J., 1999. Neuropathic pain: aetiology, symptoms, mechanisms, and management. Lancet 353, 1959-1964.
144. Woolf, C.J., Thompson, S.W., 1991. The induction and maintenance of central sensitization is dependent on N-methyl-D-aspartic acid receptor activation; implications for the treatment of post-injury pain hypersensitivity states. Pain 44, 293-299.
145. Wu, F.S., Gibbs, T.T., Farb, D.H., 1991. Pregnenolone sulfate: a positive allosteric modulator at the N-methyl-D-aspartate receptor. Mol. Pharmacol. 40, 333-336.
146. Xu, J., Zeng, C., Chu, W., Pan, F., Rothfuss, J.M., Zhang, F., Tu, Z., Zhou, D., Zeng, D., Vangveravong, S., Johnston, F., Spitzer, D., Chang, K.C., Hotchkiss, R.S., Hawkins, W.G., Wheeler, K.T., Mach, R.H., 2011. Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site. Nat. Commun. 2, 380.
147. Yang, S., Bhardwaj, A., Cheng, J., Alkayed, N.J., Hurn, P.D., Kirsch, J.R., 2007. Sigma receptor agonists provide neuroprotection in vitro by preserving bcl-2. Anesth. Analg. 104, 1179-1184.
148. Yang, Z.J., Carter, E.L., Torbey, M.T., Martin, L.J., Koehler, R.C., 2010. 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.
149. Yoon, S.Y., Roh, D.H., Seo, H.S., Kang, S.Y., Han, H.J., Beitz, A.J., Lee, J.H., 2009. Intrathecal injection of the neurosteroid, DHEAS, produces mechanical allodynia in mice: involvement of spinal sigma-1 and GABA receptors. Br. J. Pharmacol. 157, 666-673.
150. Yoon, S.Y., Roh, D.H., Seo, H.S., Kang, S.Y., Moon, J.Y., Song, S., Beitz, A.J., Lee, J.H., 2010. An increase in spinal dehydroepiandrosterone sulfate (DHEAS) enhances NMDA-induced pain via phosphorylation of the NR1 subunit in mice: involvement of the sigma-1 receptor. Neuropharmacology 59, 460-467.
151. Zamanillo, D., Portillo-Salido, E., Vela, J.M., Romero, L., 2012. Sigma 1 receptor chaperone: pharmacology and therapeutic perspectives. In: Botana, L.M., Loza, M. (Eds.), Therapeutic Targets. Wiley-VCH, Weinheim, Germany, pp. 225-278.
152. Zambon, A.C., De Costa, B.R., Kanthasamy, A.G., Nguyen, B.Q., Matsumoto, R.R., 1997. Subchronic administration of N-[2-(3,4-dichlorophenyl) ethyl]-N-methyl-2-(dimethylamino) ethylamine (BD1047) alters sigma 1 receptor binding. Eur. J. Pharmacol. 324, 39-47.
153. Zou, X., Lin, Q., Willis, W.D., 2002. Role of protein kinase A in phosphorylation of NMDA receptor 1 subunits in dorsal horn and spinothalamic tract neurons after intradermal injection of capsaicin in rats. Neuroscience 115, 775-786.