酮色林可阻断猪血管平滑肌细胞的α1-肾上腺素能受体。
Ketanserin blocks alpha 1-adrenoceptors of porcine vascular smooth muscle cells.
作者信息
Nishimura J, Kanaide H, Shogakiuchi Y, Nakamura M
出版信息
Eur J Pharmacol. 1987 Jan 13;133(2):235-8. doi: 10.1016/0014-2999(87)90155-5.
The effect of ketanserin on alpha-adrenoceptors was studied in membrane preparations of the porcine aorta using [3H]prazosin and [3H]yohimbine binding assays to identify alpha 1- and alpha 2-adrenoceptors. Ketanserin bound to alpha-adrenoceptors and the Ki value of ketanserin for alpha 1-adrenoceptors was 8.3 nM, a value practically equal to that of phentolamine (Ki = 7.2 nM). The Ki value of ketanserin for alpha 2-adrenoceptors was 3.3 microM. Thus, at the doses prescribed clinically, ketanserin blocks alpha 1- but not alpha 2-adrenoceptors of porcine vascular smooth muscle.
使用[3H]哌唑嗪和[3H]育亨宾结合试验来鉴定α1和α2肾上腺素能受体，在猪主动脉膜制剂中研究了酮色林对α肾上腺素能受体的作用。酮色林与α肾上腺素能受体结合，其对α1肾上腺素能受体的Ki值为8.3 nM，该值实际上与酚妥拉明的Ki值（7.2 nM）相等。酮色林对α2肾上腺素能受体的Ki值为3.3 μM。因此，在临床规定的剂量下，酮色林阻断猪血管平滑肌的α1肾上腺素能受体而非α2肾上腺素能受体。
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