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首页> 外文期刊>Life sciences >ANTAGONISM TO NORADRENALINE-INDUCED LETHALITY IN RATS IS RELATED TO AFFINITY FOR THE ALPHA(1A)-ADRENOCEPTOR SUBTYPE
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ANTAGONISM TO NORADRENALINE-INDUCED LETHALITY IN RATS IS RELATED TO AFFINITY FOR THE ALPHA(1A)-ADRENOCEPTOR SUBTYPE

机译：大鼠去甲肾上腺素诱导的死亡的拮抗作用与α（1A）-肾上腺素受体亚型的亲和力有关

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摘要

The potency of several al-adrenoceptor antagonists in preventing the noradrenaline-induced lethality in conscious rats, their binding affinity for the native alpha(1A)- and alpha(1B)-adrenoceptors, the recombinant animal alpha(1a)-, alpha(1b)- and alpha(1d)-adrenoceptor subtypes, as well as their functional affinity for the alpha 1L-adrenoceptor subtype were evaluated. The potency of the tested compounds as antagonists of noradrenaline-induced lethality was correlated with the affinity for the alpha(1A)- (and alpha(1a)-) adrenoceptor subtype, but not with the affinity for the other subtypes. On the contrary, the hypotensive effects of the compounds, assessed in anesthetized rats, were not clearly related with the affinity for any of the alpha(1)-subtypes. These results suggest that the alpha(1A)-subtype plays a determining role in preventing lethality induced by noradrenaline in the rats, and that this activity is unrelated to the hypotensive effect of the compounds, which cannot be clearly correlated with affinity for a particular alpha(1)-adrenoceptor subtype. [References: 37]
机译：几种al-肾上腺素受体拮抗剂在预防去甲肾上腺素引起的致死性中的效力，它们对天然α（1A）-和alpha（1B）-肾上腺素受体，重组动物alpha（1a）-，alpha（1b）的结合亲和力）和alpha（1d）-肾上腺素受体亚型，以及它们对alpha 1L-肾上腺素受体亚型的功能亲和力进行了评估。被测化合物作为去甲肾上腺素诱导的致死性的拮抗剂的效力与对α（1A）-（和α（1a）-）肾上腺素受体亚型的亲和力相关，但与与其他亚型的亲和力不相关。相反，在麻醉大鼠中评估的化合物的降压作用与与任何α（1）-亚型的亲和力没有明显关系。这些结果表明，α（1A）亚型在预防去甲肾上腺素引起的致死性中起着决定性作用，并且该活性与化合物的降压作用无关，后者与特定α的亲和力不能明确相关（1）肾上腺素受体亚型。 [参考：37]

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