生物活性

• 描述Tiagabine Hydrochloride is the hydrochloride form of tiagabine. It is a derivative of piperidine carboxylic acid and has anticonvulsant effect. It is a selective inhibitor of GABA reabsorption. Perfusion of tiagabine (50 microM) for 15 min, evoked large, slow depolarizations with a frequency of 6-8/h which persisted for 4-5 h^[3]. Superfusion of tiagabine significantly prolonged the decay kinetics of both action potential-dependent and -independent (tetrodotoxin-resistant) inhibitory postsynaptic currents (IPSCs) that were mediated by GABA(A) receptors. Furthermore, it decreased the frequency of these IPSCs. In the behaving animal, tiagabine when injected unilaterally into the globus pallidus caused consistent ipsilateral rotation of the rats indicative of increased inhibition of globus pallidus activity^[4]. Moreover, tiagabine offers a significant neuroprotection in global ischemia in gerbils when given 30 min before ischemia but not when given 3 h after ischemia^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01381523	-	-	Completed	-	-
  NCT02727101	Epilepsy	Phase 4	Terminated(slow enrollment)	-	United States, Maryland ... more >> MidAtlantic Epilepsy and Sleep Center Bethesda, Maryland, United States, 20817 Collapse <<
  NCT00404248	Brain and Central Nervous Syst... more >>em Tumors Collapse <<	Phase 1 Phase 2	Completed	-	United States, Alabama ... more >> UAB Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3410 United States, Florida H. Lee Moffitt Cancer Center and Research Institute at University of South Florida Tampa, Florida, United States, 33612-9497 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Comprehensive Cancer Center Winston-Salem, North Carolina, United States, 27157-1096 United States, Ohio Cleveland Clinic Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104-4283 Collapse <<

• 更多
• 参考文献

• [1] Angehagen M, Ben-Menachem E, et al. Novel mechanisms of action of three antiepileptic drugs, vigabatrin, tiagabine, and topiramate. Neurochem Res. 2003 Feb;28(2):333-40.

  [2] Hu RQ, Davies JA. Tigabine hydrochloride, an inhibitor of gamma-aminobutyric acid (GABA) uptake, induces cortical depolarizations in vitro. Brain Res. 1997 Apr 11;753(2):260-8.

  [3] Hu RQ, Davies JA. Tigabine hydrochloride, an inhibitor of gamma-aminobutyric acid (GABA) uptake, induces cortical depolarizations in vitro. Brain Res. 1997 Apr 11;753(2):260-8.

  [4] Chen L, Yung WH. Effects of the GABA-uptake inhibitor tiagabine in rat globus pallidus. Exp Brain Res. 2003 Sep;152(2):263-9.

  [5] Iqbal S, Baziany A, Gordon S, Wright S, Hussain M, Miyashita H, Shuaib A, Hasan Rajput A. Neuroprotective effect of tiagabine in transient forebrain global ischemia: an in vivo microdialysis, behavioral, and histological study. Brain Res. 2002 Aug 16;946(2):162-70.

• 更多

• Collapse