Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization

British Journal of Pharmacology

Volumn 166, Issue 8, 2012, Pages 2289-2306

  Romero, L ^a   Zamanillo, D ^a   Nadal, X ^b   Sanchez Arroyos R ^a   Rivera Arconada, I ^c   Dordal, A ^a   Montero, A ^a   Muro, A ^a   Bura, A ^b   Segales C ^a   Laloya, M ^a   Hernandez E ^a   Portillo Salido, E ^a   Escriche, M ^a   Codony, X ^a   Encina, G ^a   Burgueno J ^a   Merlos, M ^a   Baeyens, J ^d   Giraldo, J ^e   Lopez Garcia J A ^c   Maldonado, R ^b   Plata Salaman C R ^a   Vela, J M ^a   more..

^a ESTEVE   (Spain)

^b UNIVERSITAT POMPEU FABRA   (Spain)

^c UNIVERSITY OF ALCALÁ   (Spain)

^d UNIVERSITY OF GRANADA   (Spain)

^e UNIVERSITAT AUTÒNOMA DE BARCELONA   (Spain)

Author keywords

central sensitization; neuropathic pain; S1RA (E 52862) 1 receptor

Indexed keywords

4 [2 [[5 METHYL 1 (2 NAPHTHALENE) 1H PYRAZOL 3 YL]OXY]ETHYL]MORPHOLINE; E 52862; OPIATE ANTAGONIST; PREGABALIN; S 1RA; SIGMA 1 OPIATE RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIALLODYNIC EFFECT; ANTIHYPERALGESIC EFFECT; ANTINOCICEPTION; ARTICLE; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; CORRELATION ANALYSIS; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG RESPONSE; DRUG TISSUE LEVEL; DRUG TOLERANCE; ELECTROPHYSIOLOGY; EX VIVO STUDY; IN VITRO STUDY; IN VIVO STUDY; MALE; MECHANICAL STIMULATION; MOUSE; NEUROPATHIC PAIN; NEWBORN; NOCICEPTION; NOCICEPTIVE PAIN; NONHUMAN; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; REPEATED DRUG DOSE; SCIATIC NERVE INJURY; SENSITIZATION; SINGLE DRUG DOSE; THERMAL STIMULATION;

ANALGESICS; ANIMALS; BEHAVIOR, ANIMAL; CAPSAICIN; ELECTRIC STIMULATION; FORMALDEHYDE; GENE EXPRESSION REGULATION; MALE; MICE; MORPHOLINES; NEURALGIA; PAIN MEASUREMENT; PYRAZOLES; RECEPTORS, SIGMA;

EID: 84864447546     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.01942.x     Document Type: Article

References (41)

1. Alonso G, Phan V, Guillemain I, Saunier M, Legrand A, Anoal M, et al,. (2000). Imunocytochemical localization of the sigma 1 receptor in the adult rat central nervous system. Neuroscience 97: 155-170. (Pubitemid 30195885)
2. 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. (Pubitemid 26140876)
3. Black JW, Leff P, (1983). Operational models of pharmacological agonism. Proc R Soc Lond B Biol Sci 220: 141-162. (Pubitemid 14217337)
4. Cendán CM, Pujalte JM, Portillo-Salido E, Baeyens JM, (2005a). Antinociceptive effects of haloperidol and its metabolites in the formalin test in mice. Psychopharmacology (Berl) 182: 485-493. (Pubitemid 41464629)
5. Cendán CM, Pujalte JM, Portillo-Salido E, Montoliu L, Baeyens JM, (2005b). Formalin-induced pain is reduced in sigma(1) receptor knockout mice. Eur J Pharmacol 511: 73-74. (Pubitemid 40380646)
6. Cheng ZX, Lan DM, Wu PY, Zhu YH, Dong Y, Ma L, et al,. (2008). Neurosteroid dehydroepiandrosterone sulphate inhibits persistent sodium currents in rat medial prefrontal cortex via activation of sigma-1 receptors. Exp Neurol 210: 128-136. (Pubitemid 351258075)
7. Chien CC, Pasternak GW, (1994). Selective antagonism of opioid analgesia by a sigma system. J Pharmacol Exp Ther 271: 1583-1590. (Pubitemid 24382674)
8. Cobos EJ, Baeyens JM, 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. (Pubitemid 40194721)
9. Cobos EJ, del Pozo E, Baeyens JM, (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. (Pubitemid 47057276)
10. Cobos EJ, Entrena JM, Nieto FR, Cendán CM, Del Pozo E, (2008). Pharmacology and therapeutic potential of sigma(1) receptor ligands. Curr Neuropharmacol 6: 344-366.
11. DeHaven-Hudkins DL, Fleissner LC, Ford-Rice FY, (1992). Characterization of the binding of [3H](+)pentazocine to Ï recognition sites in guinea pig brain. Eur J Pharmacol 227: 371-378.
12. Dickenson AH, Sullivan AF, (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. (Pubitemid 17123438)
13. Drews E, Zimmer A, (2009). Central sensitization needs sigma receptors. Pain 145: 269-270.
14. Entrena JM, Cobos EJ, Nieto FR, Cendán CM, Baeyens JM, 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.
15. Entrena JM, Cobos EJ, Nieto FR, Cendán CM, Gris G, Del Pozo E, et al,. (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.
16. Hayashi T, Kagaya A, Takebayashi M, Shimizu M, Uchitomi Y, Motohashi N, et al,. (1995). Modulation by sigma ligands of intracellular free Ca++ mobilization by N-methyl-D-aspartate in primary culture of rat frontal cortical neurons. J Pharmacol Exp Ther 275: 207-214.
17. Hayashi T, Maurice T, Su TP, (2000). Ca(2+) signaling via sigma(1)-receptors: novel regulatory mechanism affecting intracellular Ca(2+) concentration. J Pharmacol Exp Ther 293: 788-798. (Pubitemid 30417843)
18. Herrera Y, Katnik C, Rodriguez JD, Hall AA, Willing A, Pennypacker KR, et al,. (2008). Sigma-1 receptor modulation of acid-sensing ion channel a (ASIC1a) and ASIC1a-induced Ca2+ influx in rat cortical neurons. J Pharmacol Exp Ther 327: 491-502.
19. Herrero JF, Laird JM, Lõpez-García JA, (2000). Wind-up of spinal cord neurones and pain sensation: much ado about something? Prog Neurobiol 61: 169-203. (Pubitemid 30110477)
20. Kawasaki Y, Kohno T, Zhuang ZY, Brenner GJ, Wang H, Van Der Meer C, et al,. (2004). 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. (Pubitemid 39280810)
21. Kim FJ, Kovalyshyn I, Burgman M, Neilan C, Chien CC, Pasternak GW, (2010). Sigma 1 receptor modulation of G-protein-coupled receptor signaling: potentiation of opioid transduction independent from receptor binding. Mol Pharmacol 77: 695-703.
22. Kim HW, Kwon YB, Roh DH, Yoon SY, Han HJ, Kim KW, et al,. (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.
23. Kim HW, Roh DH, Yoon SY, Seo HS, Kwon YB, Han HJ, et al,. (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.
24. Laggner C, Cuberes MR, Holenz J, Berrocal-Romero J, Contijoch-Llobet MM, (2006). Sigma receptor inhibitors. Patent no WO-2006/021462 A1.
25. Latremoliere A, Woolf CJ, (2009). Central sensitization: a generator of pain hypersensitivity by central neural plasticity. J Pain 10: 895-926.
26. Martina M, Turcotte ME, 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. (Pubitemid 44971116)
27. Maurice T, Su TP, (2009). The pharmacology of sigma-1 receptors. Pharmacol Ther 124: 195-206.
28. McGrath J, Drummond G, McLachlan E, Kilkenny C, Wainwright C, (2010). Guidelines for reporting experiments involving animals: the ARRIVE guidelines. Br J Pharmacol 160: 1573-1576.
29. Mei J, Pasternak GW, (2002). Sigma1 receptor modulation of opioid analgesia in the mouse. J Pharmacol Exp Ther 300: 1070-1074. (Pubitemid 34165014)
30. Monnet FP, Debonnel G, Junien JL, De Montigny C, (1990). N-methyl-D-aspartate-induced neuronal activation is selectively modulated by sigma receptors. Eur J Pharmacol 179: 441-445. (Pubitemid 20137514)
31. de la Puente B, Nadal X, Portillo-Salido E, Sánchez-Arroyos R, Ovalle S, Palacios G, et al,. (2009). Sigma-1 receptors regulate activity-induced spinal sensitization and neuropathic pain after peripheral nerve injury. Pain 145: 294-303.
32. Roh DH, Kim HW, Yoon SY, Seo HS, Kwon YB, Kim KW, et al,. (2008). 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.
33. Roh DH, Yoon SY, Seo HS, Kang SY, Moon JY, Song S, et al,. (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.
34. Ronsisvalle G, Marrazzo A, Prezzavento O, Cagnotto A, Mennini T, Parenti C, et al,. (2001). Opioid and sigma receptor studies. New developments in the design of selective sigma ligands. Pure Appl Chem 73: 1499-1509.
35. Son JS, Kwon YB, (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.
36. Su TP, 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. (Pubitemid 37139064)
37. Su TP, Hayashi T, Maurice T, Buch S, Ruoho AE, (2010). The sigma-1 receptor chaperone as an inter-organelle signaling modulator. Trends Pharmacol Sci 31: 557-566.
38. Tsai SY, Hayashi T, Mori T, Su TP, (2009). Sigma-1 receptor chaperones and diseases. Cent Nerv Syst Agents Med Chem 9: 184-189.
39. Ultenius C, Linderoth B, Meyerson BA, Wallin J, (2006). Spinal NMDA receptor phosphorylation correlates with the presence of neuropathic signs following peripheral nerve injury in the rat. Neurosci Lett 399: 85-90.
40. Woolf CJ, Thompson SW, (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.
41. Zhang H, Cuevas J, (2002). Sigma receptors inhibit high-voltage-activated calcium channels in rat sympathetic and parasympathetic neurons. J Neurophysiol 87: 2867-2879. (Pubitemid 34670667)