育亨宾立体异构体与大鼠肝脏及人血小板中α-肾上腺素能受体的结合。
Binding of yohimbine stereoisomers to alpha-adrenoceptors in rat liver and human platelets.
作者信息
Ferry N, Goodhardt M, Hanoune J, Sevenet T
出版信息
Br J Pharmacol. 1983 Feb;78(2):359-64. doi: 10.1111/j.1476-5381.1983.tb09401.x.
Abstract
1--Displacement of tritiated prazosin binding to rat liver plasma membranes and tritiated yohimbine human platelet membranes shows that (+)-yohimbine, alloyohimbine and alpha-yohimbine (rauwolscine) are selective alpha 2-adrenoceptor antagonists (KD alpha 1/KD alpha 2:635, 46.6 and 112 respectively) whereas corynanthine is more alpha 1-selective (KD alpha 1/KD alpha 2:0.036). 2--11-Methoxy derivatives of alpha-yohimbine and epi-alpha-yohimbine are very weak alpha-adrenoceptor blockers. 3--It is concluded that the aromatic A ring, the Nb atom, and the carboxymethyl moiety are important for the binding of yohimbine to the alpha-adrenoceptor, the carboxymethyl group being important for the alpha 1/alpha 2 specificity of the molecule.
摘要
- 氚标记的哌唑嗪与大鼠肝细胞膜结合以及氚标记的育亨宾与人血小板膜结合的置换实验表明，（+）-育亨宾、别育亨宾和α-育亨宾（萝芙辛）是选择性α2-肾上腺素能受体拮抗剂（KDα1/KDα2分别为635、46.6和112），而柯楠因对α1受体的选择性更高（KDα1/KDα2为0.036）。2. α-育亨宾和表-α-育亨宾的11-甲氧基衍生物是非常弱的α-肾上腺素能受体阻滞剂。3. 得出的结论是，芳香A环、Nb原子和羧甲基部分对于育亨宾与α-肾上腺素能受体的结合很重要，羧甲基基团对于分子的α1/α2特异性很重要。
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