Doxey J C, Everitt J, Metcalf G
Eur J Pharmacol. 1978 Sep 1;51(1):1-10. doi: 10.1016/0014-2999(78)90055-9.
The autonomic profile of mianserin has been compared with that of yohimbine, phentolamine, phenoxybenzamine and desmethylimipramine. The effects of mianserin on tyramine and noradrenaline pressor responses in the pithed rat were consistent with alpha-adrenoceptor antagonist and uptake blocking properties. In isolated tissue experiments, the selectivity of mianserin for pre- and postsynaptic alpha-adrenoceptors was similar to that of phentolamine. In pitched rats mianserin antagonised the pressor response produced by clonidine and reversed the inhibitory actions of clonidine on cardiac nerve stimulation. In contrast mianserin only caused slight reversal of the inhibitory effects of clonidine on hypogastric nerve stimulation. Uptake blockade itself inhibits hypogastric nerve stimulation and this could counteract any antagonism of the effects of clonidine at the presynaptic alpha-adrenoceptor. The results demonstrate the uptake blocking properties of mianserin and its antagonism at both pre- and postsynaptic alpha-adrenoceptors.
已将米安色林的自主神经特征与育亨宾、酚妥拉明、酚苄明和去甲丙咪嗪的自主神经特征进行了比较。米安色林对脊髓麻醉大鼠体内酪胺和去甲肾上腺素升压反应的影响与α-肾上腺素能受体拮抗剂及摄取阻断特性一致。在离体组织实验中，米安色林对突触前和突触后α-肾上腺素能受体的选择性与酚妥拉明相似。在脊髓麻醉大鼠中，米安色林拮抗可乐定产生的升压反应，并逆转可乐定对心脏神经刺激的抑制作用。相比之下，米安色林仅使可乐定对腹下神经刺激的抑制作用略有逆转。摄取阻断本身会抑制腹下神经刺激，这可能会抵消可乐定在突触前α-肾上腺素能受体处的任何拮抗作用。结果证明了米安色林的摄取阻断特性及其对突触前和突触后α-肾上腺素能受体的拮抗作用。
