Pregabalin is a potent and selective ligand for α 2δ- 1 and α 2δ-2 calcium channel subunits

European Journal of Pharmacology

Volumn 667, Issue 1-3, 2011, Pages 80-90

  Li, Zheng ^a   Taylor, Charles P ^a   Weber, Mark ^a   Piechan, Julie ^a   Prior, Faith ^a   Bian, Feng ^a   Cui, Mei ^a   Hoffman, Diane ^b   Donevan, Sean ^a  

^a PFIZER INC   (United States)

^b UBC Scientific Solutions   (United States)

Author keywords

Analgesic; Anticonvulsant; Anxiolytic; Calcium channel 2 subunit; Pregabalin; Receptor autoradiography

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR; ION CHANNEL; PREGABALIN; UNCLASSIFIED DRUG; VOLTAGE GATED CALCIUM CHANNEL; VOLTAGE GATED CALCIUM CHANNEL SUBUNIT ALPHA2DELTA 1; VOLTAGE GATED CALCIUM CHANNEL SUBUNIT ALPHA2DELTA 2;

AMYGDALOID NUCLEUS; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BRAIN CORTEX; BRAIN NERVE CELL; BRAIN REGION; CEREBELLUM; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SPECIFICITY; EMBRYO; EVOKED BRAIN STEM RESPONSE; EVOKED SPINAL CORD RESPONSE; GABAERGIC SYSTEM; HIPPOCAMPUS; HUMAN; HUMAN CELL; HUMAN TISSUE; HYDROGEN BOND; MALE; MOLECULAR DYNAMICS; NONHUMAN; PRIORITY JOURNAL; PROTEIN FUNCTION; RAT; SPINAL CORD DORSAL HORN; SWINE; VOLTAGE CLAMP;

ANIMALS; AUTORADIOGRAPHY; CALCIUM CHANNELS; ELECTROPHYSIOLOGICAL PROCESSES; GAMMA-AMINOBUTYRIC ACID; HIPPOCAMPUS; HUMANS; LIGANDS; MALE; NEOCORTEX; NEURONS; OOCYTES; RATS; RECEPTORS, GABA-A; RECEPTORS, GABA-B; SUBSTRATE SPECIFICITY; XENOPUS;

EID: 79960552387     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.05.054     Document Type: Article

References (30)

1. C.S. Bauer, M. Nieto-Rostro, W. Rahman, A. Tran-Van-Minh, L. Ferron, L. Douglas, I. Kadurin, Y. Sri Ranjan, L. Fernandez-Alacid, N.S. Millar, A.H. Dickenson, R. Lujan, and A.C. Dolphin The increased trafficking of the calcium channel subunit alpha2delta-1 to presynaptic terminals in neuropathic pain is inhibited by the alpha2delta ligand pregabalin J. Neurosci. 29 2009 4076 4088
2. C.S. Bauer, W. Rahman, A. Tran-van-Minh, R. Lujan, A.H. Dickenson, and A.C. Dolphin The anti-allodynic alpha(2)delta ligand pregabalin inhibits the trafficking of the calcium channel alpha(2)delta-1 subunit to presynaptic terminals in vivo Biochem. Soc. Trans. 38 2010 525 528
3. 2- δ protein J Med Chem 48 2005 2294 2307 (Pubitemid 40516424)
4. S. Bertrand, G.Y. Ng, M.G. Purisai, S.E. Wolfe, M.W. Severidt, D. Nouel, R. Robitaille, M.J. Low, G.P. O'Neill, K. Metters, J.C. Lacaille, B.M. Chronwall, and S.J. Morris The anticonvulsant, antihyperalgesic agent gabapentin is an agonist at brain γ-aminobutyric acid type B receptors negatively coupled to voltage-dependent calcium channels J. Pharmacol. Exp. Ther. 298 2001 15 24 (Pubitemid 32574505)
5. B receptors in hippocampal pyramidal cells Synapse 50 2003 95 109 (Pubitemid 37152143)
6. 2-delta type 1 genetically modified mice Brain Res 1075 2006 68 80
7. M.N. Di Guilmi, F.J. Urbano, C.G. Inchauspe, and O.D. Uchitel Pregabalin modulation of neurotransmitter release is mediated by change in intrinsic activation/inactivation properties of cav2.1 calcium channels J. Pharmacol. Exp. Ther. 336 2011 973 982
8. S.D. Donevan, and M.A. Rogawski Multiple actions of arylalkylamine arthropod toxins on the N-methyl-d-aspartate receptor Neuroscience 70 1996 361 375
9. R.H. Dworkin, A.E. Corbin, J.P. Young Jr. , U. Sharma, L. LaMoreaux, H. Bockbrader, E.A. Garofalo, and R.M. Poole Pregabalin for the treatment of postherpetic neuralgia: a randomized, placebo-controlled trial Neurology 60 2003 1274 1283 (Pubitemid 36460982)
10. D.E. Feltner, J.G. Crockatt, S.J. Dubovsky, C.K. Cohn, R.K. Shrivastava, S.D. Targum, M. Liu-Dumaw, C.M. Carter, and A.C. Pande A randomized, double-blind, placebo-controlled, fixed-dose, multicenter study of pregabalin in patients with generalized anxiety disorder J. Clin. Psychopharmacol. 23 2003 240 249 (Pubitemid 36807791)
11. 2- δ-1 subunit of voltage-dependent calcium channels as a molecular target for pain mediating the analgesic actions of pregabalin Proc Natl Acad Sci U S A 103 2006 17537 17542 (Pubitemid 44789004)
12. J.A. French, A.R. Kugler, J.L. Robbins, L.E. Knapp, and E.A. Garofalo Dose-response trial of pregabalin adjunctive therapy in patients with partial seizures Neurology 60 2003 1631 1637 (Pubitemid 36618090)
13. 3H]gabapentin to a novel site in rat brain: autoradiographic studies Eur. J. Pharmacol. 244 1993 303 309 (Pubitemid 23051253)
14. A.A. Jensen, J. Mosbacher, S. Elg, K. Lingenhoehl, T. Lohmann, T.N. Johansen, B. Abrahamsen, J.P. Mattsson, A. Lehmann, B. Bettler, and H. Bräuner-Osborne The anticonvulsant gabapentin (Neurontin) does not act through γ-aminobutyric acid-B receptors Mol. Pharmacol. 61 2002 1377 1384 (Pubitemid 34575748)
15. B receptor agonist Neuropharmacology 41 2001 965 975 (Pubitemid 34024992)
16. Z. Li, S. Donevan, C.P. Taylor, J. Piechan, J. Offord, T.Z. Su, S. Baron, M.G. Vartanian, F. Bian, D.J. Wustrow, T. Belliotti, J. Schwarz, and A. Thorpe High-affinity binding of pregabalin at alpha-2-delta subunits of voltage-gated calcium channel: contribution to anticonvulsant action [abstract no. p866] Epilepsia 46 2005 280
17. S.M. Lotarski, S. Donevan, A. El-Kattan, S. Osgood, J. Poe, C.P. Taylor, and J. Offord Anxiolytic-Like activity of pregabalin in the vogel conflict test in {alpha}2{delta}-1 (R217A) and {alpha}2{delta}-2 (R279A) mouse mutants J. Pharmacol. Exp. Ther. 2011 May 10 [Epub ahead of print]
18. J.J. Lynch III, P. Honore, D.J. Anderson, W.H. Bunnelle, K.H. Mortell, C. Zhong, C.L. Wade, C.Z. Zhu, H. Xu, K.C. Marsh, C.H. Lee, M.F. Jarvis, and M. Gopalakrishnan (L)-Phenylglycine, but not necessarily other alpha2delta subunit voltage-gated calcium channel ligands, attenuates neuropathic pain in rats Pain 125 2006 136 142 (Pubitemid 44498971)
19. G.A. McPherson Analysis of radioligand binding experiments. A collection of computer programs for the IBM PC J Pharmacol Methods 14 1985 213 228 (Pubitemid 15241175)
20. G.Y. Ng, S. Bertrand, R. Sullivan, N. Ethier, J. Wang, J. Yergey, M. Belley, L. Trimble, K. Bateman, L. Alder, A. Smith, R. McKernan, K. Metters, G.P. O'Neill, J.C. Lacaille, and T.E. Hébert γ-Aminobutyric acid type B receptors with specific heterodimer composition and postsynaptic actions in hippocampal neurons are targets of anticonvulsant gabapentin action Mol. Pharmacol. 59 2001 144 152 (Pubitemid 32043096)
21. J. Offord, S. Lotarski, J. Peterson, S. Galvin, B. Strenkowski, H. Hain, and S. Donevan Anticonvulsant activity of pregabalin (Lyrica) requires binding to the α2δ1 subunit of voltage sensitive calcium channels Presented at the American Epilepsy Society - 64th Annual Meeting, San Antonio, TX, December 3-7, 2010 2010 http://www.aesnet.org/go/publications/aes-abstracts/ abstract-search/mode/display/st/offord/sy/2010/sb/All/id/12438 Abstract # 1.238
22. B.W. Peng, J.A. Justice, K. Zhang, J.X. Li, X.H. He, and R.M. Sanchez Gabapentin promotes inhibition by enhancing hyperpolarization-activated cation currents and spontaneous firing in hippocampal CA1 interneurons Neurosci. Lett. 494 2011 19 23
23. J.M. Rho, S.D. Donevan, and M.A. Rogawski Direct Activation of GABAA receptors by barbiturates in cultured rat hippocampal neurons J. Physiol. 497 1996 509 522 (Pubitemid 26418115)
24. S. Straube, S. Derry, R.A. Moore, and H.J. McQuay Pregabalin in fibromyalgia: meta-analysis of efficacy and safety from company clinical trial reports Rheumatology (Oxford) 49 2010 706 715
25. R. Surges, T.M. Freiman, and T.J. Feuerstein Gabapentin increases the hyperpolarization-activated cation current Ih in rat CA1 pyramidal cells Epilepsia 44 2003 150 156 (Pubitemid 36206015)
26. C.P. Taylor Mechanisms of analgesia by gabapentin and pregabalin-calcium channel alpha2-delta [Cavalpha2-delta] ligands Pain 142 2009 13 16
27. C.P. Taylor, and R. Garrido Immunostaining of rat brain, spinal cord, sensory neurons and skeletal muscle for calcium channel alpha2-delta (alpha2-delta) type 1 protein Neuroscience 155 2008 510 521
28. 2-delta) subunit as a target for antiepileptic drug discovery Epilepsy Res 73 2007 137 150 (Pubitemid 46329329)
29. O.D. Uchitel, M.N. Di Guilmi, F.J. Urbano, and C. Gonzalez-Inchauspe Acute modulation of calcium currents and synaptic transmission by gabapentinoids Channels (Austin) 4 2010 490 496
30. 2δ for gabapentin binding Biochem. J. 342 1999 313 320 (Pubitemid 29425352)