进一步证明经典α1A-和克隆α1c-肾上腺素受体是同一亚型

Carmen Pimoule, Salomon Z. Langer, David Graham
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引用次数: 12

摘要

我们比较了在用烷基化剂、10μM氯乙基可乐定或10nM SZL-49(1-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-4-(2-二环[2.2.2]辛-2,5-二烯-Z-羰基)-哌嗪)预处理后,表达克隆的α1b、α1c和α1d肾上腺素受体的细胞系的膜制剂中[3H]哌唑嗪结合位点的失活。克隆的α1b肾上腺素能受体表现出与大鼠肝脏经典α1b肾上腺素能受体相似的失活特征,因为氯乙基可乐定与SZL-49相比产生了显著程度的失活。克隆的大鼠颌下腺α1c肾上腺素能受体和经典的α1A肾上腺素能受体之间的相似之处还在于,这两种亚型对SZL-49高度敏感,但对氯乙基可乐定相对不敏感。克隆的α1d肾上腺素受体表现出独特的特征,氯乙基可乐定和SZL-49都对该亚型产生了显著的失活。克隆的α1c和经典的α1A肾上腺素受体之间烷基化失活谱的相似性支持了最近的提议,即这两种α1-肾上腺素受体实际上对应于相同的亚型。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Further evidence that the classical α1A- and cloned α1c-adrenoceptors are the same subtype

We compared the inactivation of [3H]prazosin binding sites in membrane preparations of cell-lines expressing the cloned α1b, α1c and α1d-adrenoceptors after pretreatment with the alkylating agents, 10 μM chlorethylclonidine or 10 nM SZL-49 (1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-bicyclo[2.2.2]octa-2,5-diene-Z-carbonyl)-piperazine). The cloned α1b-adrenoceptor exhibited a similar inactivation profile to that of the classical α1B-adrenoceptor of rat liver in that chlorethylclonidine in contrast to SZL-49 produced a marked degree of inactivation. A similarity between the cloned α1c-adrenoceptor and the classical α1A-adrenoceptor of rat submaxillary gland was also noted in that both subtypes were highly sensitive to SZL-49 but relatively insensitive to chlorethylclonidine. The cloned α1d-adrenoceptor displayed a unique profile in that both chlorethylclonidine and SZL-49 produced a marked inactivation of this subtype. The similarity of the alkylation-inactivation profiles between the cloned α1c and classical α1A-adrenoceptors support the recent proposal that these two α1-adrenoceptors in fact correspond to the same subtype.

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