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Chemical Compound Review

Gabatril     (3R)-1-[4,4-bis(3- methylthiophen-2-yl)but...

Synonyms: Tiagabina, tiagabine, Tiagabinum, Gabitril (TN), CHEMBL1027, ...
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Disease relevance of tiagabine


Psychiatry related information on tiagabine


High impact information on tiagabine


Chemical compound and disease context of tiagabine


Biological context of tiagabine


Anatomical context of tiagabine

  • We used in vivo microdialysis to determine a suitable dosing regimen for tiagabine (NNC328) to elevate extracellular levels of GABA within the hippocampus [3].
  • When normothermia was maintained both during and after ischemia in a separate group of tiagabine-treated animals, approximately 77% of the CA1 pyramidal cell layer was necrotic at 4 days [3].
  • In the present study the effects of systemically administered tiagabine [30 mg/kg, ip (ED50)] were examined on audiogenic seizure (AGS) severity and neuronal firing in the inferior colliculus (IC) in the freely moving genetically epilepsy-prone rat (GEPR-9) [22].
  • The present study examines the effect of tiagabine (a selective inhibitor of GABA transporter 1, GAT-1), SNAP-5114 (a semi-selective inhibitor of rat GAT-3/mouse GAT4) and NNC 05-2045 (a non-selective GABA uptake inhibitor) in modulating GABA levels in the hippocampus and thalamus [23].
  • Whereas nipecotic acid and beta-alanine suppressed all forms of epileptiform activity albeit at high concentrations (1-5 mM), tiagabine was much more potent in blocking the hippocampal recurrent short discharges and the seizure-like events in the medial entorhinal cortex, but could not block the late recurrent discharges [24].

Associations of tiagabine with other chemical compounds


Gene context of tiagabine


Analytical, diagnostic and therapeutic context of tiagabine

  • One hundred sixty-two patients provided cognitive and quality of life data for the analyses and received the following treatments: placebo (n = 57), 16 mg/d tiagabine (n = 34), 32 mg/d tiagabine (n = 45), or 56 mg/d tiagabine (n = 26) at a fixed-dose for 12 weeks after a 4-week dose titration period [33].
  • Exploratory regressions on these data in children and previous data in adults showed fairly strong relationships between body size and tiagabine clearance and volume of distribution, with body size explaining about 40 to 50% of the variability [12].
  • Tiagabine significantly increased sleep efficiency, tendentially decreased wakefulness and prominently increased both SWS and low-frequency activity in the EEG within non-REM sleep [34].
  • This 12-week, multicenter, double-blind study randomized patients to receive either tiagabine or placebo [13].
  • MEASUREMENTS AND RESULTS: Polysomnography documented a SWS-enhancing effect of tiagabine [35].


  1. Improvement of stiff-person syndrome with tiagabine. Murinson, B.B., Rizzo, M. Neurology (2001) [Pubmed]
  2. Possible drug-induced thrombocytopenia secondary to tiagabine. Willert, C., Englisch, S., Schlesinger, S., Runge, U. Neurology (1999) [Pubmed]
  3. Postischemic inhibition of GABA reuptake by tiagabine slows neuronal death in the gerbil hippocampus. Inglefield, J.R., Perry, J.M., Schwartz, R.D. Hippocampus. (1995) [Pubmed]
  4. Tiagabine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the management of epilepsy. Adkins, J.C., Noble, S. Drugs (1998) [Pubmed]
  5. Tiagabine and the treatment of refractory bipolar disorder. Schaffer, L.C., Schaffer, C.B. The American journal of psychiatry. (1999) [Pubmed]
  6. Tiagabine for posttraumatic stress disorder: a case series of 7 women. Taylor, F.B. The Journal of clinical psychiatry. (2003) [Pubmed]
  7. Tiagabine for the treatment of generalized anxiety disorder: a randomized, open-label, clinical trial with paroxetine as a positive control. Rosenthal, M. The Journal of clinical psychiatry. (2003) [Pubmed]
  8. Effect of tiagabine on sleep in elderly subjects with primary insomnia: a randomized, double-blind, placebo-controlled study. Roth, T., Wright, K.P., Walsh, J. Sleep. (2006) [Pubmed]
  9. Medications development: successes and challenges. Vocci, F., Ling, W. Pharmacol. Ther. (2005) [Pubmed]
  10. Visual field constriction: accumulation of vigabatrin but not tiagabine in the retina. Sills, G.J., Patsalos, P.N., Butler, E., Forrest, G., Ratnaraj, N., Brodie, M.J. Neurology (2001) [Pubmed]
  11. Reflections on the treatment of seizures in the elderly population. Rowan, A.J. Neurology (1998) [Pubmed]
  12. A single-dose study to define tiagabine pharmacokinetics in pediatric patients with complex partial seizures. Gustavson, L.E., Boellner, S.W., Granneman, G.R., Qian, J.X., Guenther, H.J., el-Shourbagy, T., Sommerville, K.W. Neurology (1997) [Pubmed]
  13. The efficacy and tolerability of tiagabine in adult patients with post-traumatic stress disorder. Davidson, J.R., Brady, K., Mellman, T.A., Stein, M.B., Pollack, M.H. Journal of clinical psychopharmacology (2007) [Pubmed]
  14. The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study. Pollack, M.H., Roy-Byrne, P.P., Van Ameringen, M., Snyder, H., Brown, C., Ondrasik, J., Rickels, K. The Journal of clinical psychiatry. (2005) [Pubmed]
  15. Comparison of the preclinical anticonvulsant profiles of tiagabine, lamotrigine, gabapentin and vigabatrin. Dalby, N.O., Nielsen, E.B. Epilepsy Res. (1997) [Pubmed]
  16. Total percentage body weight changes during add-on therapy with tiagabine, carbamazepine and phenytoin. Hogan, R.E., Bertrand, M.E., Deaton, R.L., Sommerville, K.W. Epilepsy Res. (2000) [Pubmed]
  17. The gamma-aminobutyric acid uptake inhibitor, tiagabine, is anticonvulsant in two animal models of reflex epilepsy. Smith, S.E., Parvez, N.S., Chapman, A.G., Meldrum, B.S. Eur. J. Pharmacol. (1995) [Pubmed]
  18. Concurrent use of antiretrovirals and anticonvulsants in human immunodeficiency virus (HIV) seropositive patients. Romanelli, F., Pomeroy, C. Curr. Pharm. Des. (2003) [Pubmed]
  19. Effects of tiagabine, a gamma-aminobutyric acid re-uptake inhibitor, on normal rat bladder function. Pehrson, R., Andersson, K.E. J. Urol. (2002) [Pubmed]
  20. Pharmacodynamic analysis of the interaction between tiagabine and midazolam with an allosteric model that incorporates signal transduction. Jonker, D.M., Vermeij, D.A., Edelbroek, P.M., Voskuyl, R.A., Piotrovsky, V.K., Danhof, M. Epilepsia (2003) [Pubmed]
  21. Effect of the GABA uptake inhibitor tiagabine on sleep and EEG power spectra in the rat. Lancel, M., Faulhaber, J., Deisz, R.A. Br. J. Pharmacol. (1998) [Pubmed]
  22. Blockade of GABA uptake with tiagabine inhibits audiogenic seizures and reduces neuronal firing in the inferior colliculus of the genetically epilepsy-prone rat. Faingold, C.L., Randall, M.E., Anderson, C.A. Exp. Neurol. (1994) [Pubmed]
  23. GABA-level increasing and anticonvulsant effects of three different GABA uptake inhibitors. Dalby, N.O. Neuropharmacology (2000) [Pubmed]
  24. Effects of gamma-aminobutyric acid (GABA) agonists and GABA uptake inhibitors on pharmacosensitive and pharmacoresistant epileptiform activity in vitro. Pfeiffer, M., Draguhn, A., Meierkord, H., Heinemann, U. Br. J. Pharmacol. (1996) [Pubmed]
  25. The clinical pharmacokinetics of the newer antiepileptic drugs. Focus on topiramate, zonisamide and tiagabine. Perucca, E., Bialer, M. Clinical pharmacokinetics. (1996) [Pubmed]
  26. Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. Dhar, T.G., Borden, L.A., Tyagarajan, S., Smith, K.E., Branchek, T.A., Weinshank, R.L., Gluchowski, C. J. Med. Chem. (1994) [Pubmed]
  27. Do antiepileptic drugs play a role in sudden unexpected death in epilepsy? Walczak, T. Drug safety : an international journal of medical toxicology and drug experience. (2003) [Pubmed]
  28. Lack of pharmacokinetic interaction between tiagabine and erythromycin. Thomsen, M.S., Groes, L., Agersø, H., Kruse, T. Journal of clinical pharmacology. (1998) [Pubmed]
  29. GABA-B receptor activation in the rat globus pallidus potently suppresses pentylenetetrazol-induced tonic seizures. Chen, L., Chan, Y.S., Yung, W.H. J. Biomed. Sci. (2004) [Pubmed]
  30. Behavioural correlates of an altered balance between synaptic and extrasynaptic GABAAergic inhibition in a mouse model. Sinkkonen, S.T., Vekovischeva, O.Y., Möykkynen, T., Ogris, W., Sieghart, W., Wisden, W., Korpi, E.R. Eur. J. Neurosci. (2004) [Pubmed]
  31. Correlation between anticonvulsant activity and inhibitory action on glial gamma-aminobutyric acid uptake of the highly selective mouse gamma-aminobutyric acid transporter 1 inhibitor 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and its N-alkylated analogs. White, H.S., Sarup, A., Bolvig, T., Kristensen, A.S., Petersen, G., Nelson, N., Pickering, D.S., Larsson, O.M., Frølund, B., Krogsgaard-Larsen, P., Schousboe, A. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  32. Tiagabine: a novel antiepileptic drug. Luer, M.S., Rhoney, D.H. The Annals of pharmacotherapy. (1998) [Pubmed]
  33. Cognitive and quality of life effects of differing dosages of tiagabine in epilepsy. Dodrill, C.B., Arnett, J.L., Sommerville, K.W., Shu, V. Neurology (1997) [Pubmed]
  34. The GABA uptake inhibitor tiagabine promotes slow wave sleep in normal elderly subjects. Mathias, S., Wetter, T.C., Steiger, A., Lancel, M. Neurobiol. Aging (2001) [Pubmed]
  35. Tiagabine is associated with sustained attention during sleep restriction: evidence for the value of slow-wave sleep enhancement? Walsh, J.K., Randazzo, A.C., Stone, K., Eisenstein, R., Feren, S.D., Kajy, S., Dickey, P., Roehrs, T., Roth, T., Schweitzer, P.K. Sleep. (2006) [Pubmed]
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