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Atipamezole

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Chemical Structure| 104054-27-5 同义名 : MPV 1248;Antisedan
CAS号 : 104054-27-5
货号 : A316493
分子式 : C14H16N2
纯度 : 95%
分子量 : 212.29
MDL号 : MFCD00864502
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(141.32 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 11 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
靶点

  • α-adrenergic receptor
描述 Atipamezole is an alpha2-adrenoceptor antagonist with an imidazole structure. It rapidly reverses sedation/anesthesia induced by alpha2-adrenoceptor agonists. In animals with sustained nociception, atipamezole increased pain-related responses by blocking the noradrenergic feedback inhibition of pain[3]. Atipamezole has inhibition to CYP2C9 mediated diclofenac hydroxylation in human and animal liver microsomes with IC50 values of 1.50-5.20 μM[4]. Animals receiving atipamezole (1 mg/kg, s.c.) without rehabilitation exhibited a significant motor improvement in the ladder rung walk test, but not the forelimb reaching test[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
NCT01435213 Healthy Phase 1 Completed - Finland ... 展开 >> University of Turku, Clinical Research Services Turku CRST Turku, Finland, 20520 University of Turku, Turku PET Centre Turku, Finland, 20520 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.71mL

0.94mL

0.47mL

23.55mL

4.71mL

2.36mL

47.11mL

9.42mL

4.71mL
参考文献

[1]Pertovaara A, Haapalinna A, et al. Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.

[2]Sirvio J, Riekkinen P Jr, et al. The effects of alpha-2 adrenoceptor antagonist, atipamezole, on spatial learning in scopolamine-treated and aged rats. J Neural Transm Park Dis Dement Sect. 1992;4(2):99-106.

[3]Pertovaara A, Haapalinna A, Sirviö J, Virtanen R. Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.

[4]Li Z, Zhang Y, Gao Y, Xiang Y, Zhang W, Lu C, Zhuang X. Atipamezole is a promising non-discriminative inhibitor against pan-CYP450 including diclofenac 4'-hydroxylation: A comparison with ABT for drug ADME optimization and mechanism study. Eur J Pharm Sci. 2019 Mar 15;130:156-165.

[5]Beltran EJ, Papadopoulos CM, Tsai SY, Kartje GL, Wolf WA. Long-term motor improvement after stroke is enhanced by short-term treatment with the alpha-2 antagonist, atipamezole. Brain Res. 2010 Jul 30;1346:174-82.