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Chemical Compound Review

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

Synonyms: Tiabex, TIAGABINE HCl, CHEMBL1695, Abbott-70569, ABT-569, ...
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Disease relevance of tiagabine

  • Loss of consciousness did not occur reliably after H [1].
  • One patient with unstable angina was excluded from the study because of hypotension and facial flushing after a 6-mg test dose of H [1].
  • After the administration of 5 mg/kg of H or 30 mg/kg of M to the restrained rat, a marked hypothermia was observed which reached a maximum mean depth of 3.1 and 4.5 degrees C below the baseline Tc, respectively [2].

Psychiatry related information on tiagabine


High impact information on tiagabine


Biological context of tiagabine

  • The affinity, capacity, and kinetics of colesevelam HCl binding for GCDC, TDC, and GC were not significantly altered after suspension in water, carbonated water, Coca-Cola(R), Sprite(R), grape juice, orange juice, tomato juice, or Gatorade(R) [8].
  • Although the factor of restraint itself did not alter the rat's Tc, it did dramatically alter the action of M and H on the body temperature of the rat [2].

Anatomical context of tiagabine

  • Injections of 6 and 50 micrograms H into cerebellum and bulbar reticular formation elicited weaker CTA while neocortical, hypothalamic and mesencephalic applications were ineffective [9].

Associations of tiagabine with other chemical compounds


Analytical, diagnostic and therapeutic context of tiagabine

  • An inverse relationship was evident between the degree of dissociation of H from the three salts, at pH 7.3 and their durations of analgesia in vivo [10].


  1. High-dose hydromorphone (Dilaudid) for coronary artery bypass surgery. Welti, R.S., Moldenhauer, C.C., Hug, C.C., Kaplan, J.A., Holbrook, G.W. Anesth. Analg. (1984) [Pubmed]
  2. Restraint alters the effects of morphine and heroin on core temperature in the rat. Martin, G.E., Pryzbylik, A.T., Spector, N.H. Pharmacol. Biochem. Behav. (1977) [Pubmed]
  3. Long-term retention rates of new antiepileptic drugs in adults with chronic epilepsy and learning disability. Simister, R.J., Sander, J.W., Koepp, M.J. Epilepsy & behavior : E&B (2007) [Pubmed]
  4. Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents. Knutsen, L.J., Andersen, K.E., Lau, J., Lundt, B.F., Henry, R.F., Morton, H.E., Naerum, L., Petersen, H., Stephensen, H., Suzdak, P.D., Swedberg, M.D., Thomsen, C., Sørensen, P.O. J. Med. Chem. (1999) [Pubmed]
  5. Intraocular lidocaine in phacoemulsification: an endothelium and blood-aqueous barrier permeability study. Iradier, M.T., Fernandez, C., Bohorquez, P., Moreno, E., del Castillo, J.B., Garcia, J. Ophthalmology (2000) [Pubmed]
  6. Review of controlled trials of gabitril (tiagabine): a clinician's viewpoint. Loiseau, P. Epilepsia (1999) [Pubmed]
  7. The effect of two lipophilic gamma-aminobutyric acid uptake blockers in CA1 of the rat hippocampal slice. Rekling, J.C., Jahnsen, H., Mosfeldt Laursen, A. Br. J. Pharmacol. (1990) [Pubmed]
  8. Bile acid salt binding with colesevelam HCl is not affected by suspension in common beverages. Hanus, M., Zhorov, E. Journal of pharmaceutical sciences. (2006) [Pubmed]
  9. Central mediation of the conditioned taste aversion induced in rats by harmaline. Buresová, O., Bures, J. Psychopharmacology (Berl.) (1984) [Pubmed]
  10. Analgesia duration and physical dependence in mice after a single injection of three heroin salts and morphine sulphate in various vehicles. Brands, B., Hirst, M., Gowdey, C.W., Baskerville, J.C. Archives internationales de pharmacodynamie et de thérapie. (1978) [Pubmed]
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