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大鼠肠系膜动脉床中节后兴奋性α-肾上腺素能受体亚型的研究。

A study on the postjunctional excitatory alpha-adrenoreceptor subtypes in the mesenteric arterial bed of the rat.

作者信息

Pipili E

出版信息

J Auton Pharmacol. 1986 Jun;6(2):125-32. doi: 10.1111/j.1474-8673.1986.tb00639.x.

Abstract

The nature of the postsynaptic adrenoreceptor subtypes which mediate vasoconstriction in the mesenteric arterial bed of the rat was investigated using mixed and selective alpha 1, alpha 2 and beta-agonists and antagonists. Phenylephrine (PE) an alpha 1-selective agonist and noradrenaline (NA) a mixed alpha1 and alpha 2-agonist, produced a rise in perfusion pressure (vasoconstriction). The responses to NA remained stable with time whereas responses to PE considerably increased. UK14304 an alpha 2-selective agonist at low doses (10(-8)-10(-7) moles), caused small, slow contractions in most preparations. Repeated administration of these doses or slightly higher ones, densensitized the tissue to this compound but not to NA or PE. Finally, UK14304 given simultaneously with NA or PE, at doses higher than 5 X 10(-7) moles, reduced contractions to the latter compounds and this effect was not altered by 10(-7) M rauwolscine, an alpha 2-selective antagonist. Prazosin, an alpha1-selective antagonist, as expected, reduced contractions to NA considerably at 10(-10)-10(-8) M and abolished contractions to UK14304 at 2 X 10(-9) M. Rauwolscine, at 10(-8) M, potentiated contractions to NA and at 10(-6) M reduced contractions to both NA and PE (when compared to time controls). When propranolol (10(-6) M), a beta-antagonist was included in the perfusion fluid, rauwolscine no longer potentiated responses to NA but reduced them at all concentrations. Under the same conditions rauwolscine affected the responses to PE in a similar direction to that observed in the absence of propranolol. These results suggest that in the rat mesenteric arterial bed: rauwolscine exerts an effect additional to alpha2-adrenoreceptor antagonism.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

运用混合及选择性α1、α2和β激动剂与拮抗剂,对介导大鼠肠系膜动脉床血管收缩的突触后肾上腺素能受体亚型的性质进行了研究。苯肾上腺素(PE)是一种α1选择性激动剂,去甲肾上腺素(NA)是一种混合性α1和α2激动剂,二者均可使灌注压升高(血管收缩)。随着时间推移,对NA的反应保持稳定,而对PE的反应则显著增强。UK14304是一种低剂量(10^(-8)-10^(-7)摩尔)的α2选择性激动剂,在大多数标本中可引起轻微、缓慢的收缩。重复给予这些剂量或稍高剂量,会使组织对该化合物产生脱敏,但对NA或PE无影响。最后,UK14304与NA或PE同时给予,剂量高于5×10^(-7)摩尔时,会降低对后两种化合物的收缩反应,且这种作用不会被α2选择性拮抗剂10^(-7)M萝芙木碱改变。哌唑嗪是一种α1选择性拮抗剂,正如预期的那样,在10^(-10)-10^(-8)M时可显著降低对NA的收缩反应,并在2×10^(-9)M时消除对UK14304的收缩反应。萝芙木碱在10^(-8)M时可增强对NA的收缩反应,在10^(-6)M时可降低对NA和PE的收缩反应(与时间对照相比)。当灌注液中加入β拮抗剂普萘洛尔(10^(-6)M)时,萝芙木碱不再增强对NA的反应,而是在所有浓度下均使其降低。在相同条件下,萝芙木碱对PE反应的影响方向与未加普萘洛尔时观察到的相似。这些结果表明,在大鼠肠系膜动脉床中:萝芙木碱除了具有α2肾上腺素能受体拮抗作用外,还发挥其他作用。(摘要截短于250字)

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