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Chemical Compound Review

Pregablin     (3S)-3-(aminomethyl)-5- methyl-hexanoic acid

Synonyms: Lyrica, Pregabalin, TOS-BB-0910, CHEMBL1059, Lyrica (TN), ...
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Disease relevance of Lyrica


Psychiatry related information on Lyrica


High impact information on Lyrica


Chemical compound and disease context of Lyrica


Biological context of Lyrica


Anatomical context of Lyrica


Associations of Lyrica with other chemical compounds


Gene context of Lyrica

  • We investigated whether the newer antiepileptic drug, pregabalin (PGB), could exert effects on KATP channels in differentiated hippocampal neuron-derived H19-7 cells [30].
  • Pregabalin produced a limited, significant decrement on CFF and CTT and a significant effect on the LARS [22].
  • RESULTS: Pregabalin showed no significant effects on the objective psychometrics-CRT, BRT, RVIP, STM-compared with placebo [22].
  • The alpha 2 delta-1, alpha 2 delta-2, and alpha 2 delta-3 subunits of voltage-gated Ca(2+) channels, presumed sites of gabapentin and pregabalin action, were detected with immunoblots of human neocortical synaptosomes [31].
  • Pregabalin is a synthetic amino acid compound effective in clinical trials for the treatment of post-herpetic neuralgia, diabetic peripheral neuropathy, generalized anxiety disorder and adjunctive therapy for partial seizures of epilepsy [32].

Analytical, diagnostic and therapeutic context of Lyrica


  1. Pregabalin-withdrawal encephalopathy and splenial edema: a link to high-altitude illness? Oaklander, A.L., Buchbinder, B.R. Ann. Neurol. (2005) [Pubmed]
  2. Pregabalin-withdrawal encephalopathy and splenial edema. Prilipko, O., Delavelle, J., Seeck, M. Ann. Neurol. (2006) [Pubmed]
  3. Pregabalin for the treatment of fibromyalgia syndrome: results of a randomized, double-blind, placebo-controlled trial. Crofford, L.J., Rowbotham, M.C., Mease, P.J., Russell, I.J., Dworkin, R.H., Corbin, A.E., Young, J.P., LaMoreaux, L.K., Martin, S.A., Sharma, U. Arthritis Rheum. (2005) [Pubmed]
  4. Oral treatment with PD-0200347, an alpha2delta ligand, reduces the development of experimental osteoarthritis by inhibiting metalloproteinases and inducible nitric oxide synthase gene expression and synthesis in cartilage chondrocytes. Boileau, C., Martel-Pelletier, J., Brunet, J., Tardif, G., Schrier, D., Flory, C., El-Kattan, A., Boily, M., Pelletier, J.P. Arthritis Rheum. (2005) [Pubmed]
  5. Pregabalin: in the treatment of painful diabetic peripheral neuropathy. Frampton, J.E., Scott, L.J. Drugs (2004) [Pubmed]
  6. Pregabalin for treatment of generalized anxiety disorder: a 4-week, multicenter, double-blind, placebo-controlled trial of pregabalin and alprazolam. Rickels, K., Pollack, M.H., Feltner, D.E., Lydiard, R.B., Zimbroff, D.L., Bielski, R.J., Tobias, K., Brock, J.D., Zornberg, G.L., Pande, A.C. Arch. Gen. Psychiatry (2005) [Pubmed]
  7. Pregabalin in generalized anxiety disorder: a placebo-controlled trial. Pande, A.C., Crockatt, J.G., Feltner, D.E., Janney, C.A., Smith, W.T., Weisler, R., Londborg, P.D., Bielski, R.J., Zimbroff, D.L., Davidson, J.R., Liu-Dumaw, M. The American journal of psychiatry. (2003) [Pubmed]
  8. Efficacy of the novel anxiolytic pregabalin in social anxiety disorder: a placebo-controlled, multicenter study. Pande, A.C., Feltner, D.E., Jefferson, J.W., Davidson, J.R., Pollack, M., Stein, M.B., Lydiard, R.B., Futterer, R., Robinson, P., Slomkowski, M., DuBoff, E., Phelps, M., Janney, C.A., Werth, J.L. Journal of clinical psychopharmacology. (2004) [Pubmed]
  9. A double-blind study in healthy volunteers to assess the effects on sleep of pregabalin compared with alprazolam and placebo. Hindmarch, I., Dawson, J., Stanley, N. Sleep. (2005) [Pubmed]
  10. Effect of a second-generation alpha2delta ligand (pregabalin) on visceral sensation in hypersensitive patients with irritable bowel syndrome. Houghton, L.A., Fell, C., Whorwell, P.J., Jones, I., Sudworth, D.P., Gale, J.D. Gut (2007) [Pubmed]
  11. Synthesis of both enantiomers of a P-chirogenic 1,2-bisphospholanoethane ligand via convergent routes and application to rhodium-catalyzed asymmetric hydrogenation of CI-1008 (pregabalin). Hoge, G. J. Am. Chem. Soc. (2003) [Pubmed]
  12. Pharmacology meets vesicular trafficking at a central nervous system synapse: pregabalin effects on synaptic vesicle cycling in hippocampal neurons. Holz, R.W. Mol. Pharmacol. (2006) [Pubmed]
  13. Efficacy and safety of pregabalin in the treatment of generalized anxiety disorder: a 6-week, multicenter, randomized, double-blind, placebo-controlled comparison of pregabalin and venlafaxine. Montgomery, S.A., Tobias, K., Zornberg, G.L., Kasper, S., Pande, A.C. The Journal of clinical psychiatry. (2006) [Pubmed]
  14. Genotype-dependence of gabapentin and pregabalin sensitivity: the pharmacogenetic mediation of analgesia is specific to the type of pain being inhibited. Chesler, E.J., Ritchie, J., Kokayeff, A., Lariviere, W.R., Wilson, S.G., Mogil, J.S. Pain (2003) [Pubmed]
  15. Antinociceptive effect of pregabalin in septic shock-induced rectal hypersensitivity in rats. Eutamene, H., Coelho, A.M., Theodorou, V., Toulouse, M., Chovet, M., Doherty, A., Fioramonti, J., Bueno, L. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  16. Pregabalin: A novel gamma-aminobutyric acid analogue in the treatment of neuropathic pain, partial-onset seizures, and anxiety disorders. Tassone, D.M., Boyce, E., Guyer, J., Nuzum, D. Clinical therapeutics (2007) [Pubmed]
  17. Effects of oral pregabalin and aprepitant on pain and central sensitization in the electrical hyperalgesia model in human volunteers. Chizh, B.A., Göhring, M., Tröster, A., Quartey, G.K., Schmelz, M., Koppert, W. British journal of anaesthesia (2007) [Pubmed]
  18. Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein. Belliotti, T.R., Capiris, T., Ekhato, I.V., Kinsora, J.J., Field, M.J., Heffner, T.G., Meltzer, L.T., Schwarz, J.B., Taylor, C.P., Thorpe, A.J., Vartanian, M.G., Wise, L.D., Zhi-Su, T., Weber, M.L., Wustrow, D.J. J. Med. Chem. (2005) [Pubmed]
  19. Novel cyclopropyl beta-amino acid analogues of pregabalin and gabapentin that target the alpha2-delta protein. Schwarz, J.B., Gibbons, S.E., Graham, S.R., Colbry, N.L., Guzzo, P.R., Le, V.D., Vartanian, M.G., Kinsora, J.J., Lotarski, S.M., Li, Z., Dickerson, M.R., Su, T.Z., Weber, M.L., El-Kattan, A., Thorpe, A.J., Donevan, S.D., Taylor, C.P., Wustrow, D.J. J. Med. Chem. (2005) [Pubmed]
  20. Pregabalin pharmacology and its relevance to clinical practice. Ben-Menachem, E. Epilepsia (2004) [Pubmed]
  21. Pregabalin enhances nonrapid eye movement sleep. Kubota, T., Fang, J., Meltzer, L.T., Krueger, J.M. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  22. A double-blind, placebo- and positive-internal-controlled (alprazolam) investigation of the cognitive and psychomotor profile of pregabalin in healthy volunteers. Hindmarch, I., Trick, L., Ridout, F. Psychopharmacology (Berl.) (2005) [Pubmed]
  23. Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Micheva, K.D., Taylor, C.P., Smith, S.J. Mol. Pharmacol. (2006) [Pubmed]
  24. Pregabalin exerts oppositional effects on different inhibitory circuits in human motor cortex: a double-blind, placebo-controlled transcranial magnetic stimulation study. Lang, N., Sueske, E., Hasan, A., Paulus, W., Tergau, F. Epilepsia (2006) [Pubmed]
  25. Two cases of painful gynecomastia and lower extremity pain in association with pregabalin therapy. Málaga, I., Sanmarti, F.X. Epilepsia (2006) [Pubmed]
  26. Stereospecific effect of pregabalin on ectopic afferent discharges and neuropathic pain induced by sciatic nerve ligation in rats. Chen, S.R., Xu, Z., Pan, H.L. Anesthesiology (2001) [Pubmed]
  27. Modern antiepileptic drugs: guidelines and beyond. Hitiris, N., Brodie, M.J. Curr. Opin. Neurol. (2006) [Pubmed]
  28. Pregabalin and gabapentin reduce release of substance P and CGRP from rat spinal tissues only after inflammation or activation of protein kinase C. Fehrenbacher, J.C., Taylor, C.P., Vasko, M.R. Pain (2003) [Pubmed]
  29. Anticonvulsants for neuropathic pain syndromes: mechanisms of action and place in therapy. Tremont-Lukats, I.W., Megeff, C., Backonja, M.M. Drugs (2000) [Pubmed]
  30. The opening effect of pregabalin on ATP-sensitive potassium channels in differentiated hippocampal neuron-derived H19-7 cells. Huang, C.W., Huang, C.C., Wu, S.N. Epilepsia (2006) [Pubmed]
  31. Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex. Fink, K., Dooley, D.J., Meder, W.P., Suman-Chauhan, N., Duffy, S., Clusmann, H., Göthert, M. Neuropharmacology (2002) [Pubmed]
  32. Calcium channel alpha2-delta type 1 subunit is the major binding protein for pregabalin in neocortex, hippocampus, amygdala, and spinal cord: an ex vivo autoradiographic study in alpha2-delta type 1 genetically modified mice. Bian, F., Li, Z., Offord, J., Davis, M.D., McCormick, J., Taylor, C.P., Walker, L.C. Brain Res. (2006) [Pubmed]
  33. Pregabalin: in the treatment of postherpetic neuralgia. Frampton, J.E., Foster, R.H. Drugs (2005) [Pubmed]
  34. A randomized, double-blind, placebo-controlled, fixed-dose, multicenter study of pregabalin in patients with generalized anxiety disorder. Feltner, D.E., Crockatt, J.G., Dubovsky, S.J., Cohn, C.K., Shrivastava, R.K., Targum, S.D., Liu-Dumaw, M., Carter, C.M., Pande, A.C. Journal of clinical psychopharmacology. (2003) [Pubmed]
  35. Pharmacologic treatment considerations in co-occurring bipolar and anxiety disorders. Keck, P.E., Strawn, J.R., McElroy, S.L. The Journal of clinical psychiatry. (2006) [Pubmed]
  36. Pregabalin as adjunctive therapy for partial seizures. Brodie, M.J. Epilepsia (2004) [Pubmed]
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