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Tiagabine-d6(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tiagabine-d6(hydrochloride)图片
规格:98%
分子量:418
包装与价格:
包装价格(元)
500ug电议
1mg电议
5mg电议

产品介绍
An internal standard for the quantification of tiagabine
货号:ajcx23612
CAS:1217808-68-8
分子式:C20H19D6NO2S2.HCl
分子量:418
溶解度:DMSO: soluble,Methanol: soluble,Water: soluble
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Tiagabine-d6is intended for use as an internal standard for the quantification of tiagabine by GC- or LC-MS. Tiagabine is an inhibitor of GABA transporter 1 (GAT-1; IC50= 49 nM for GAT-1 expressed in CHO cells).1It inhibits seizures induced by DMCM in mice (ED50= 1.2 mg/kg, i.p.).2Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin to delay pain responses in mice in the hot plate test.3,4Formulations containing tiagabine have been used as adjunctive therapies in the treatment of partial seizures.


1.Nakada, K., Yoshikawa, M., Ide, S., et al.Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: Identification of an efficient lead for potent inhibitors of GABA transportsBioorg. Med. Chem.21(17)4938-4950(2013) 2.Andersen, K.E., Braestrup, C., GrØnwald, F.C., et al.The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidateJ. Med. Chem.36(12)1716-1725(1993) 3.Giardina, W.J., Decker, M.W., Porsolt, R.D., et al.An evaluation of the GABA uptake blocker tiagabine in animal models of neuropathic and nociceptive painDrug Dev. Res.44(2-3)106-113(1998) 4.?uszczki, J.J., Ko?acz, A., Wojda, E., et al.Synergistic interaction of gabapentin with tiagabine in the hot-plate test in mice: An isobolographic analysisPharmacol. Rep.61(3)459-467(2009)