產品屬性：
產品名稱 | Alpidem |
規格 | 1 mg、5 mg、10 mg、25 mg |
貨號 | EY-01Y16975 |
Cas No.: 82626-01-5
別名: N/A
化學名: N/A
分子式: C21H23Cl2N3O
分子量: 404.3
溶解度: Chloroform: slightly soluble,Methanol: slightly soluble
儲存條件: -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
Alpidem is an anxiolytic agent.1 It selectively binds to α1β2γ2 subunit-containing GABAA receptors over α5β2γ2 subunit-containing GABAA receptors in HEK293 cells (IC50s = 0.017 and ≥10 μM, respectively, for the recombinant rat receptors).2 Alpidem also binds to the GABAA/benzodiazepine receptor complex and translocator protein 18 kDa (TSPO) with IC50 values of 0.028 and 0.0079 μM, respectively.3 It reduces marble burying in mice, indicating anxiolytic activity, with a minimum effective dose (MED) of 10 mg/kg.4 Unlike the benzodiazepine alprazolam, alpidem does not induce sedation in mice when administered at doses up to 2 mg/kg.5 Formulations containing alpidem have previously been used in the treatment of generalized anxiety disorder.1.Skolnick, P.Anxioselective anxiolytics: On a quest for the holy grailTrends Pharamacol. Sci.33(11)611-620(2012)
2.Faure-Halley, C., Graham, D., Arbilla, S., et al.Expression and properties of recombinant α1β2γ2 and α5β2γ2 forms of the rat GABAA receptorEur. J. Pharmacol.246(3)283-287(1993)
3.Trapani, G., Franco, M.C., Ricciardi, L., et al.Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral typeJ. Med. Chem.40(19)3109-3118(1997)
4.Zivkovic, B., Morel, E., Joly, D., et al.Pharmacological and behavioral profile of alpidem as an anxiolyticPharmacopsychiatry23(Suppl. 3)108-113(1990)
5.Hasco?t, M., and Bourin, M.Anticonflict effect of alpidem as compared with the benzodiazepine alprazolam in ratsPharmacol. Biochem. Behav.56(2)317-324(1997)
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