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分离的猫尿道与其他各种分离组织之间突触后α-肾上腺素能受体群体的差异。

Differences in postsynaptic alpha-adrenoceptor populations between isolated cat urethra and various other isolated tissues.

作者信息

Gahlin K, Sparf B

出版信息

Acta Pharmacol Toxicol (Copenh). 1978;43 Suppl 2:48-55. doi: 10.1111/j.1600-0773.1978.tb03219.x.

Abstract

This study was undertaken with the aim of determining whether the postsynaptic alpha-adrenergic receptor population of the cat urethra differed from that of other isolated tissues (rabbit aorta and rat vas deferens) and if so the possibility of selectively affect these receptors. For this purpose the substances 2-methylammonio-1-(spiro[cyclopentane-1,1'-indene]-3'-yl)ethanol (KABI 2023), noradrenaline (NA) and dopamine (DA) were used. KABI 2023 and NA acted as full agonists on all three tissues investigated. DA was a full agonist on the vas deferens but was almost inactive on urethra. The contractile response of urethra to KABI 2023 was of an alpha-adrenergic nature, as it could be blocked with phentolamine. Compared with NA, KABI 2023 showed a 10 times higher selectivity for the receptors of urethra than for those of aorta. Affinity constants (log KB) for phentolamine and haloperidol with use of the various agonists were estimated. The affinity of phentolamine was found to be significantly different when using NA and KABI 2023 as agonists on the urethra but not on the aorta. Corresponding findings were obtained with haloperidol. On the vas deferens a greater difference in log KB values than that on the urethra was found. On the basis of the results, it is suggested that the population of postsynaptic alpha-adrenoceptors in the urethra (cat) differs from that in the aorta (rabbit). On the vas deferens a heterogenicity of postsynaptic receptors seem to exist which makes the interpretation of the results more difficult on this organ. In the presence of phentolamine and haloperidol the maximum responses to NA were potentiated on the aorta and vas deferens, but not on the urethra. Investigations to evaluate this difference are now in progress.

摘要

本研究旨在确定猫尿道的突触后α-肾上腺素能受体群体是否与其他离体组织(兔主动脉和大鼠输精管)不同,若存在差异,则研究选择性影响这些受体的可能性。为此,使用了2-甲基铵-1-(螺[环戊烷-1,1'-茚]-3'-基)乙醇(KABI 2023)、去甲肾上腺素(NA)和多巴胺(DA)。KABI 2023和NA对所有三种研究组织均起完全激动剂作用。DA对输精管是完全激动剂,但对尿道几乎无活性。尿道对KABI 2023的收缩反应具有α-肾上腺素能性质,因为它可被酚妥拉明阻断。与NA相比,KABI 2023对尿道受体的选择性比对主动脉受体的选择性高10倍。估计了酚妥拉明和氟哌啶醇与各种激动剂联合使用时的亲和力常数(log KB)。当使用NA和KABI 2023作为尿道激动剂而非主动脉激动剂时,发现酚妥拉明的亲和力有显著差异。氟哌啶醇也得到了相应的结果。在输精管上发现log KB值的差异比在尿道上更大。根据这些结果,提示猫尿道的突触后α-肾上腺素能受体群体与兔主动脉的不同。输精管上似乎存在突触后受体的异质性,这使得对该器官结果的解释更加困难。在酚妥拉明和氟哌啶醇存在的情况下,主动脉和输精管对NA的最大反应增强,但尿道没有。目前正在进行评估这种差异的研究。

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