Atipamezole hydrochloride

An α2A-adrenergic receptor antagonist

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货号: ajci16454
CAS: 104075-48-1
别名: 阿替美唑盐酸盐; MPV-1248 hydrochloride
分子式: C14H16N2.HCl
分子量: 248.75
纯度: >98%
溶解度: ≥ 24.9mg/mL in EtOH with ultrasonic
储存: Desiccate at 4°C
库存: 现货

Background

Atipamezole hydrochloride is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.

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[1].

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[1].

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.