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为寻找新的α１受体阻断剂，用［３Ｈ］ＷＢ４１０１配体测定法测定了１８种美西律衍生物。结果表明，其中６种化合物对大鼠脑皮层α１受体有不同程度的亲和力。凡具有手性碳结构的化合物亲和力都较高。化合物Ｍ８５００１的亲和力较妥拉唑林（ｔｏｌａｚｏｌｉｎｅ）高一个数量级并能抑制苯肾上腺素引起的大鼠肛尾肌收缩，其ｐＡ２（６８６）与ｐＫｉ（６５１）相近。结果提示，美西律衍生物对α１受体的亲和力可能与手性碳结构有关，从美西律衍生物中研制新的α１受体阻断剂是有前途的。
In order to find a new α1 receptor blocker, 18 kinds of mexiletine derivatives were determined by [3H] WB4101 ligand assay. The results showed that six of these compounds had different degrees of affinity to α1 receptors in rat cortex. All compounds with a chiral carbon structure have higher affinity. The affinity of compound M-85001 is one order of magnitude higher than that of tolazoline and inhibits phenylephrine-induced contraction of the rostral muscles of rats, with pA2 (686) similar to pKi (651). The results suggest that the affinity of the mexiletine derivatives on the α1-receptor may be related to the chiral carbon structure. It is promising to develop new α1-blockers from mexiletine derivatives.