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Presence of functional angiotensin II receptor and angiotensin converting enzyme in the aorta of the snake Bothrops jararaca

机译:蛇Botrops jararaca主动脉中功能性血管紧张素II受体和血管紧张素转化酶的存在

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Aim: Angiotensin II (Ang II) interacts with AT 1 and AT 2 receptors and, in some vertebrates, with an Ang II binding site showing low affinity for AT 1 and AT 2 receptor antagonists. This study was carried out to characterize the Ang II receptor, and the presence of an angiotensin-converting enzyme (ACE) in the aorta of the Bothrops jararaca snake. Main method: Contraction induced by Ang I or II in aortic ring from the snake was evaluated in the absence or in the presence of ACE-blocker or Ang II antagonists. Key findings: Ang II analogs, modified at positions 1 and 5, induced vasoconstriction with differences in their potencies. The relative rank order was: [Asp 1, Val 5] Ang II = [Asp 1, Ile 5] Ang II ? [Asn 1, Val 5] Ang II. ACE-like activity was detected, as well as an Ang II receptor with low affinity for AT 1 and AT 2 selective receptor antagonists (pK B values of 5.62 ± 0.23 and 5.08 ± 0.25). A disulfide reducing agent almost abolished the Ang II effect, while an alpha adrenoceptor antagonist, or removing the endothelium, did not modify the Ang II effect. These results indicate that the B. jararaca aorta has an Ang II receptor pharmacologically distinct from AT 1 and AT 2 receptors, and the vasoconstrictor effect observed is independent of catecholamine or endothelium modulation. ACE and the AT receptor in the aorta of B. jararaca may be part of a tissue renin-angiotensin system. Significance: The data contribute to the knowledge of the renin-angiotensin system in vertebrate species, and provide insight into the understanding of snake Ang II receptor characteristics and diversity.
机译:目的:血管紧张素II(Ang II)与AT 1和AT 2受体相互作用,在某些脊椎动物中,Ang II结合位点对AT 1和AT 2受体拮抗剂的亲和力低。进行这项研究以表征Ang II受体,以及Bothrops jararaca蛇主动脉中血管紧张素转化酶(ACE)的存在。主要方法:在不存在或存在ACE阻滞剂或Ang II拮抗剂的情况下,评估Ang I或II在蛇的主动脉环中引起的收缩。主要发现:在位置1和5修饰的Ang II类似物诱导血管收缩,但其功效不同。相对等级顺序为:[Asp 1,Val 5] Ang II = [Asp 1,Ile 5] Ang II? [Asn 1,Val 5] Ang II。检测到ACE样活性,以及​​对AT 1和AT 2选择性受体拮抗剂具有低亲和力的Ang II受体(pK B值为5.62±0.23和5.08±0.25)。二硫化物还原剂几乎消除了Ang II的作用,而α肾上腺素受体拮抗剂或去除内皮并没有改变Ang II的作用。这些结果表明,jararaca主动脉具有在药理上不同于AT 1和AT 2受体的Ang II受体,并且观察到的血管收缩作用与儿茶酚胺或内皮调节无关。 Jararaca的主动脉中的ACE和AT受体可能是组织肾素-血管紧张素系统的一部分。启示:这些数据有助于了解脊椎动物中的肾素-血管紧张素系统,并有助于深入了解蛇Ang II受体的特性和多样性。

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