猪小脑和肾皮质中对α2A-、α2B-和α2C-肾上腺素能受体具有亚型选择性的药物鉴定。
Identification of drugs subtype-selective for alpha 2A-, alpha 2B-, and alpha 2C-adrenoceptors in the pig cerebellum and kidney cortex.
作者信息
Wikberg-Matsson A, Wikberg J E, Uhlén S
机构信息
Department of Ophtalmology, Academic Hospital, Uppsala, Sweden.
出版信息
Eur J Pharmacol. 1995 Sep 25;284(3):271-9. doi: 10.1016/0014-2999(95)00354-n.
The radioligands [3H]MK912 and [3H]RX821002 were used to label alpha2A-, alpha2B-, and alpha2C-adrenoceptors of the pig cerebellum and kidney cortex. By inclusion of the alpha2A-adrenoceptor-selective drug, BRL44408, and using a 'multi-curve' experimental design all the three porcine alpha2-adrenoceptor subtypes could be characterized pharmacologically. The data indicate that the pig alpha2-adrenoceptor subtypes are pharmacologically more related to human alpha2-adrenoceptor subtypes than to the rodent alpha2-adrenoceptors. We suggest a set of drugs that are useful for the delineation of the pig alpha2-adrenoceptor subtypes.
放射性配体[3H]MK912和[3H]RX821002被用于标记猪小脑和肾皮质的α2A-、α2B-和α2C-肾上腺素能受体。通过加入α2A-肾上腺素能受体选择性药物BRL44408，并采用“多曲线”实验设计，所有三种猪α2-肾上腺素能受体亚型都可以从药理学角度进行表征。数据表明，猪α2-肾上腺素能受体亚型在药理学上与人类α2-肾上腺素能受体亚型的关系比与啮齿动物α2-肾上腺素能受体的关系更为密切。我们提出了一组有助于区分猪α2-肾上腺素能受体亚型的药物。
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