產(chǎn)品目錄

規(guī)格	500 μg 1 mg 5 mg
CAS	1217808-68-8
別名	N/A
化學(xué)名	N/A
分子式	C20H19D6NO2S2.HCl
分子量	418
溶解度	DMSO: soluble,Methanol: soluble,Water: soluble
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Tiagabine-d6 is 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).1 It inhibits seizures induced by DMCM in mice (ED50 = 1.2 mg/kg, i.p.).2 Tiagabine 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.3,4 Formulations 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)

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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