上海陌孚医药科技有限公司

α2-肾上腺素能受体拮抗剂,Atipamezole hydrochloride是合成的α2-肾上腺素受体拮抗剂, Ki值为1.6 nM。
中文名称 
[优选]Atipamezole hydrochloride
中文别名 
阿替美唑盐酸盐;4-(2-乙基-2-茚满)咪唑盐酸盐;4-(2-乙基-2,3-二氢-1H-茚-2-基)-1H-咪唑盐酸盐;毒死蜱;盐酸阿替美唑;阿替美唑盐酸盐(标准品)
英文名称 
Atipamezole hydrochloride
英文别名 
Atipamezole hydrochloride;4-(2-Ethyl-2-indanyl)imidazole hydrochloride;4-(2-Ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole hydrochloride;1H-Imidazole, 4-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-, monohydrochloride;Atipamezole (hydrochloride);5-(2-Ethyl-2,3-dihydro-1H-indene-2-yl)-1H-imidazolehydrochloride;Antisedan;Atipamezole HCL;MPV1248 hydrochloride;MPV-1248 hydrochloride;Unii-2W4279571x;MPV 1248 hydrochloride;Atipamezole hydrochloride, >=99%;5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-Imidazole hydrochloride;AK387105;2W4279571X;PubChem21910;atipamezole-hydrochloride;DSS
Cas No. 
104075-48-1
分子式 
C14H17ClN2
分子量 
248.75
包装储存 
4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性 
Atipamezole (MPV-1248) hydrochloride is a potent α2-adrenoceptor antagonist with a Ki of 1.6 nM.

性状 
Solid

IC50 & Target[1][2] 
Ki: 1.6 nM

体外研究(In Vitro) 
The affinity of atipamezole for α2-adrenoceptors and its α2/α1 selectivity ratio are considerably higher than yohimbine. Atipamezole is not selective for subtypes of α2-adrenoceptors. It has negligible affinity for 5-HT1, 5-HT2 and I2 bindings sites.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo) 
Atipamezole is well tolerated in rodents. In anesthetized, normotensive rats, the cardiovascular effects of atipamezole (0.01–1 mg/kg, i.v.) are rather modest. Atipamezole is commonly used by veterinarians to awaken animals from sedation or anesthesia. Atipamezole increases sexual activity in rats and monkeys. In animals with sustained nociception, atipamezole increases pain-related responses by blocking the noradrenergic feedback inhibition of pain. Atipamezole at low doses has beneficial effects on alertness, selective attention, planning, learning, and recall in experimental animals, but not necessarily on short-term working memory.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件 
Room temperature or refrigerated transportation.

储存方式 
4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

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