It might be a big family but the pain remains - Last chance saloon for selective 5-HT receptor ligands?

Current Opinion in Pharmacology

Volumn 11, Issue 1, 2011, Pages 39-44

  Andrews, Nick ^a   O'Neill, Michael F ^b  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b Eolasbio Biosciences   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 [2 [2 (4 METHYL 1 PIPERIDINYL)ETHYL] 1 PYRROLIDINESULFONYL]PHENOL; AS 19; BEFIRADOL; BUSPIRONE; DULOXETINE; E 55888; MILNACIPRAN; MSD 5A; ONDANSETRON; SEROTONIN; SEROTONIN 1 AGONIST; SEROTONIN 1A AGONIST; SEROTONIN 2A AGONIST; SEROTONIN 2A RECEPTOR; SEROTONIN 3 AGONIST; SEROTONIN 3 RECEPTOR; SEROTONIN 7 AGONIST; SEROTONIN 7 ANTAGONIST; SEROTONIN 7 RECEPTOR; SEROTONIN AGONIST; SEROTONIN NORADRENALIN REUPTAKE INHIBITOR; SEROTONIN RECEPTOR; TRICYCLIC ANTIDEPRESSANT AGENT; UNCLASSIFIED DRUG; XALIPRODEN;

ANALGESIC ACTIVITY; ARTICLE; CANCER PAIN; CHRONIC PAIN; DRUG RESEARCH; DRUG SAFETY; NEUROPATHIC PAIN; PAIN; PRIORITY JOURNAL; SENSORY NEUROPATHY; VOLUNTEER;

EID: 79953730259     PISSN: 14714892     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.coph.2011.02.002     Document Type: Review

References (37)

1. N.M. Barnes, and T. Sharp A review of central 5-HT receptors and their function Neuropharmacology 38 1999 1083 1152 (Pubitemid 29292403)
2. I. Tracey, and P.W. Mantyh The cerebral signature for pain perception and its modulation Neuron 55 2007 377 391 (Pubitemid 47161056)
3. A. Sultan, H. Gaskell, S. Derry, and R.A. Moore Duloxetine for painful diabetic neuropathy and fibromyalgia pain: systematic review of randomised trials BMC Neurol 8 2008 29
4. M.P.T. Lunn, R.A.C. Hughes, and P.J. Wiffen Duloxetine for treating painful neuropathy or chronic pain Cochrane Database Syst Rev 2009 10.1002/14651858.CD007115.pub2 Art. No.: CD007115
5. E. Loder Triptan therapy in migraine N Engl J Med 363 2010 63 70
6. D. Levy, M. Jakubowski, and R. Burstein Disruption of communication between peripheral and central trigeminovascular neurons mediates the anti-migraine action of 5HT 1B/1D receptor agonists Proc Natl Acad Sci USA 101 2004 4274 4279 (Pubitemid 38405919)
7. T. Bartsch, Y.E. Knight, and P.J. Goadsby Activation of 5-HT(1B/1D) receptor in the periaqueductal gray inhibits nociception Ann Neurol 56 2004 371 381 (Pubitemid 39166556)
8. K.G. Shields, and P.J. Goadsby Serotonin receptors modulate trigeminovascular responses in ventroposteromedial nucleus of thalamus: a migraine target? Neurobiol Dis 23 2006 491 501 (Pubitemid 44234086)
9. M.J. Millan Descending control of pain Prog Neurobiol 66 2002 355 474 This review provides a one-stop-shop on the subject of descending control of pain and though not solely on 5-HT mechanisms provides the reader with (1) the organisation of descending pathways and their pathophysiological significance; (2) the role of individual transmitters and specific receptor types in the modulation and expression of mechanisms of descending inhibition and facilitation and (3) the advantages and limitations of established and innovative analgesic strategies that act by manipulation of descending controls. (Pubitemid 34606906)
10. M.E. Lynch Antidepressants as analgesics: a review of randomized controlled trials J Psychiatry Neurosci 26 2001 30 36 (Pubitemid 32185177)
11. S.M. Stahl, M.M. Grady, C. Moret, and M. Briley SNRIs: their pharmacology, clinical efficacy, and tolerability in comparison with other classes of antidepressants CNS Spectr 10 2005 732 747 (Pubitemid 41443048)
12. R. Kishore-Kumar, S.C. Schafer, B.A. Lawlor, D.L. Murphy, and M.B. Max Single doses of the serotonin agonists buspirone and m-chlorophenylpiperazine do not relieve neuropathic pain Pain 37 1989 223 227 (Pubitemid 19136151)
13. Clinicaltrials.gov NCT00305188 Evaluation of the Efficacy of Xaliproden (SR 57746A) in Preventing the Neurotoxicity of Oxaliplatin /5FU/LV Chemotherapy.
14. G. Pavlaković, J. Tigges, and T.A. Crozier Effect of buspirone on thermal sensory and pain thresholds in human volunteers BMC Clin Pharmacol 9 2009 12
15. F.C. Colpaert 5-HT(1A) receptor activation: new molecular and neuroadaptive mechanisms of pain relief Curr Opin Investig Drugs 7 2006 40 47 Considering this is the only selective 5-HT receptor ligand currently in clinical trials for chronic pain (excluding migraine and fibromyalgia) this article is extremely provocative and gives the reader an important insight into the compelling reasons for why Pierre Fabre have advanced F 13640 to Phase II trials. (Pubitemid 43115779)
16. V. Granados-Soto, C.F. Argüelles, H.I. Rocha-González, B. Godínez-Chaparro, F.J. Flores-Murrieta, and C.M. Villalón The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats Neuroscience 165 2010 561 568 This paper is an example we feel of the sort of comprehensive pharmacological data sets that are needed to help understand the subtleties of action of the different subtypes of receptor within the 5-HT class. The authors performed dose response curves for each ligand and also antagonism with selective ligands to define specificity of ligand effect.
17. ••] this paper exemplifies the extensive nature of the studies that are needed to delineate the effect of receptor-subtype influence on the complex nature of chronic and noxious pain. (Pubitemid 46994702)
18. J. Stefulj, B. Jernej, L. Cicin-Sain, I. Rinner, and K. Schauenstein mRNA expression of serotonin receptors in cells of the immune tissues of the rat Brain Behav Immun 14 2000 219 224 (Pubitemid 32280876)
19. M. Kubera, M. Maes, G. Kenis, Y.K. Kim, and W. Lasoń Effects of serotonin and serotonergic agonists and antagonists on the production of tumor necrosis factor alpha and interleukin-6 Psychiatry Res 134 2005 251 258 (Pubitemid 40693942)
20. 2A receptors, R-DOI, was able to suppress TNFα induced inflammation with picomolar potency. The authors also state that with the exception of a few natural toxins, no current drugs or small molecule therapeutics demonstrate a comparable potency for any physiological effect.
21. 2A receptor subtype is involved in 5-HT-induced hyperalgesia in acute injury and inflammation in the rat. (Pubitemid 28342744)
22. K. Okamotoa, H. Imbea, Y. Morikawaa, M. Itoha, M. Sekimotob, K. Nemotob, and E. Senbaa 5-HT2A receptor subtype in the peripheral branch of sensory fibers is involved in the potentiation of inflammatory pain in rats Pain 99 2002 133 143
23. 2A receptors in the site of inflammation may be a promising approach to inhibit inflammatory pain.
24. R. Suzuki, and A.H. Dickenson Spinal and supraspinal contributions to central sensitization in peripheral neuropathy Neurosignals 14 2005 175 181 (Pubitemid 41417106)
25. G.J. McCleane, R. Suzuki, and A.H. Dickenson Does a single intravenous injection of the 5HT3 receptor antagonist ondansetron have an analgesic effect in neuropathic pain? A double-blinded, placebo-controlled cross-over study Anesth Analg 97 2003 1474 1478 (Pubitemid 37310150)
26. B. Tuveson, A.S. Leffler, and P. Hansson Ondansetron, a 5HT3-antagonist, does not alter dynamic mechanical allodynia or spontaneous ongoing pain in peripheral neuropathy Clin J Pain 2010 [Epub ahead of print]
27. J.A. Bard, J. Zgombick, N. Adham, P. Vaysse, T.A. Branchek, and R.L. Weinshank Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase J Biol Chem 268 1993 23422 23426 (Pubitemid 23328066)
28. T.W. Lovenberg, B.M. Baron, L. de Lecea, J.D. Miller, R.A. Prosser, M.A. Rea, P.E. Foye, M. Racke, A.L. Slone, and B.W. Siegel A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms Neuron 11 1993 449 458 (Pubitemid 23287072)
29. M. Ruat, E. Traiffort, R. Leurs, J. Tardivel-Lacombe, J. Diaz, J.M. Arrang, and J.C. Schwartz Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation Proc Natl Acad Sci USA 90 1993 8547 8551 (Pubitemid 23277706)
30. Y. Shen, F.J. Monsma Jr., M.A. Metcalf, P.A. Jose, M.W. Hamblin, and D.R. Sibley Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype J Biol Chem 268 1993 18200 18204 (Pubitemid 23260343)
31. P.A. Pierce, G.X. Xie, J.D. Levine, and S.J. Peroutka 5-Hydroxytryptamine receptor subtype messenger RNAs in rat peripheral sensory and sympathetic ganglia: a polymerase chain reaction study Neuroscience 70 1996 553 559
32. P.A. Pierce, G.X. Xie, T. Meuser, and S.J. Peroutka 5-Hydroxytryptamine receptor subtype messenger RNAs in human dorsal root ganglia: a polymerase chain reaction study Neuroscience 81 1997 813 819 (Pubitemid 27402525)
33. S. Doly, J. Fischer, M.J. Brisorgueil, D. Vergé, and M. Conrath Pre- and postsynaptic localization of the 5-HT7 receptor in rat dorsal spinal cord: immunocytochemical evidence J Comp Neurol 490 2005 256 269 (Pubitemid 41140992)
34. 7 receptor agonists as applied to pain behaviour. The authors performed dose responses to 3 agonists and also performed antagonism studies with selective ligands to show specificity of the effects of the agonists on pain behaviours.
35. A antagonist bicuculline.
36. B. Godínez-Chaparro, P. Barragán-Iglesias, G. Castañeda-Corral, H.I. Rocha-González, and V. Granados-Soto Role of peripheral 5-HT(4), 5-HT(6), and 5-HT(7) receptors in development and maintenance of secondary mechanical allodynia and hyperalgesia Pain 152 2011 687 697
37. A. Dogrul, and M. Seyrek Systemic morphine produce antinociception mediated by spinal 5-HT7, but not 5-HT1A and 5-HT2 receptors in the spinal cord Br J Pharmacol 149 2006 498 505 (Pubitemid 44658510)