Johansson L H, Persson H, Rosengren E
Eur J Pharmacol. 1986 Oct 14;130(1-2):97-103. doi: 10.1016/0014-2999(86)90187-1.
We studied the effect of two catechol and two resorcinol series of beta-adrenoceptor agonists on isolated papillary (beta 1-adrenoceptors) and soleus (beta 2-adrenoceptors) muscles preparations from the guinea-pig. One of the catechol and one of the resorcinol series were substituted by branched alkyl groups on the amino nitrogen, and the other two series were substituted by cycloalkyl groups. It was found that: the catechol derivatives were more potent than their corresponding resorcinol derivatives on both the papillary and the soleus muscle preparations, the resorcinol derivatives were more selective for the soleus muscle than their corresponding catechol derivatives, the substitution on the amino nitrogen gave compounds that were highly selective for the soleus muscle, both in the catechol and the resorcinol series. Greatest selectivity was obtained with a tertiary butyl group. the branched alkyl substitution on the amino nitrogen favoured selectivity for the soleus muscle more than cycloalkyl substitution did.
我们研究了两类儿茶酚系列和两类间苯二酚系列的β-肾上腺素能受体激动剂对豚鼠离体乳头肌（β1-肾上腺素能受体）和比目鱼肌（β2-肾上腺素能受体）标本的作用。儿茶酚系列中的一类和间苯二酚系列中的一类在氨基氮上被支链烷基取代，另外两类被环烷基取代。结果发现：在乳头肌和比目鱼肌标本上，儿茶酚衍生物比相应的间苯二酚衍生物活性更强；间苯二酚衍生物比对相应的儿茶酚衍生物对比目鱼肌更具选择性；在氨基氮上进行取代得到的化合物，在儿茶酚系列和间苯二酚系列中，对比目鱼肌都具有高度选择性。叔丁基取代时选择性最高。氨基氮上的支链烷基取代比对环烷基取代更有利于对比目鱼肌的选择性。
