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福斯高林对兔离体股动脉5-羟色胺1样受体和血管紧张素II诱导的血管收缩及环磷酸腺苷含量的影响。

The effect of forskolin on 5-HT1-like and angiotensin II-induced vasoconstriction and cyclic AMP content of the rabbit isolated femoral artery.

作者信息

Randall V A, MacLennan S J, Martin G R, Wilson V G

机构信息

Department of Physiology and Pharmacology, Medical School, Queen's Medical Centre, Nottingham, UK.

出版信息

Br J Pharmacol. 1996 Jun;118(3):627-34. doi: 10.1111/j.1476-5381.1996.tb15447.x.

Abstract
  1. A characteristic feature of vasoconstrictor 5-HT1-like receptors in vitro is that responses mediated by these receptors are enhanced by other vasoconstrictor agents. In the present study, we have examined the influence of cellular cyclic AMP on vasoconstrictor responses to activation of 5-HT1-like receptors in isolated ring segments of the rabbit femoral artery (RbFA), and determined whether modulation of this second messenger underlies the ability of angiotensin II, an endogenous vasoconstrictor, to enhance 5-HT1-like responses. 2. In the presence of 0.1 microM ketanserin (to antagonize 5-HT2-receptors) and 0.3 microM prazosin (to antagonize alpha 1-adrenoceptors), 5-HT produced a concentration-related contraction, which was significantly augmented by pre-contraction of the vessel with 0.1-0.45 nM ([A30]) angiotensin II. Responses to 5-HT in the presence of angiotensin II were inhibited by the 5-HT1-like/5-HT2 antagonist, metergoline (1 microM). 3. The directly-acting adenylyl cyclase activator, forskolin (1 microM), abolished responses to angiotensin II and caused a rightward shift and concomitant depression of the 5-HT concentration-effect (E/[A]) curve. Higher concentrations of forskolin (> 10 microM) abolished responses to 5-HT and 1 microM sodium nitroprusside abolished responses to 5-HT and angiotensin II (n = 7). 4. In the presence of angiotensin II (0.1-0.45 nM), however, 1 microM forskolin failed to inhibit 5-HT-induced contractions; the E/A curve for 5-HT (in the presence of forskolin and angiotensin II) was not significantly different from that produced in the presence of angiotensin II alone. Similarly, the presence of angiotensin II (0.1-0.45 nM) was also able to overcome partially the inhibitory effect of 1 microM sodium nitroprusside against 5-HT-induced contractions (n = 7). In marked contrast, 5-HT failed to elicit a contraction in the presence of angiotensin II and 10 microM forskolin (n = 5). 5. 5-HT (1 microM) significantly reduced basal cyclic AMP accumulation by 35%, whereas angiotensin II (0.45 nM) was without effect. The combination of angiotensin II and 5-HT failed to alter significantly the reduction in cyclic AMP produced by 5-HT alone. Forskolin (1 microM) increased cyclic AMP levels 7 fold above basal, but neither 1 microM 5-HT nor a combination of 1 microM 5-HT and 0.45 nM angiotensin II produced a significant decrease in cyclic AMP content. 6. Whilst moderate concentrations of forskolin can inhibit the responses to either agent, simultaneous activation of angiotensin II and 5-HT1-like receptors can overcome the inhibitory effect of elevated levels of cyclic AMP. Since the potentiating effect of angiotensin II, in either the presence or absence of forskolin, occurs without significant alteration of cellular cyclic AMP, it seems likely that a cyclic AMP-independent pathway is implicated in the synergistic interaction between angiotensin II and vasoconstrictor 5-HT1-like receptors.
摘要
  1. 血管收缩性5 - HT1样受体在体外的一个特征是,这些受体介导的反应会被其他血管收缩剂增强。在本研究中,我们检测了细胞内环磷酸腺苷(cAMP)对兔股动脉(RbFA)离体环段中5 - HT1样受体激活所引起的血管收缩反应的影响,并确定这种第二信使的调节是否是内源性血管收缩剂血管紧张素II增强5 - HT1样反应能力的基础。2. 在存在0.1微摩尔/升酮色林(以拮抗5 - HT2受体)和0.3微摩尔/升哌唑嗪(以拮抗α1 - 肾上腺素能受体)的情况下,5 - 羟色胺(5 - HT)产生浓度相关的收缩,用0.1 - 0.45纳摩尔([A30])血管紧张素II预收缩血管后,该收缩显著增强。在血管紧张素II存在下对5 - HT的反应被5 - HT1样/5 - HT2拮抗剂麦角新碱(1微摩尔/升)抑制。3. 直接作用的腺苷酸环化酶激活剂福斯可林(1微摩尔/升)消除了对血管紧张素II的反应,并使5 - HT浓度 - 效应(E/[A])曲线向右移动并伴随下降。更高浓度的福斯可林(> 10微摩尔/升)消除了对5 - HT的反应,1微摩尔/升硝普钠消除了对5 - HT和血管紧张素II的反应(n = 7)。4. 然而,在存在血管紧张素II(0.1 - 0.45纳摩尔)的情况下,1微摩尔/升福斯可林未能抑制5 - HT诱导的收缩;5 - HT(在存在福斯可林和血管紧张素II的情况下)的E/A曲线与仅在血管紧张素II存在下产生的曲线无显著差异。同样,血管紧张素II(0.1 - 0.45纳摩尔)的存在也能够部分克服1微摩尔/升硝普钠对5 - HT诱导收缩的抑制作用(n = 7)。明显不同的是,在存在血管紧张素II和10微摩尔/升福斯可林的情况下,5 - HT未能引起收缩(n = 5)。5. 5 - HT(1微摩尔/升)使基础cAMP积累显著降低35%,而血管紧张素II(0.45纳摩尔)无此作用。血管紧张素II和5 - HT的组合未能显著改变仅由5 - HT引起的cAMP减少。福斯可林(1微摩尔/升)使cAMP水平比基础水平升高7倍,但1微摩尔/升5 - HT或1微摩尔/升5 - HT与0.45纳摩尔血管紧张素II的组合均未使cAMP含量显著降低。6. 虽然中等浓度的福斯可林可抑制对任一药物的反应,但血管紧张素II和5 - HT1样受体的同时激活可克服cAMP水平升高的抑制作用。由于无论是否存在福斯可林,血管紧张素II的增强作用在细胞cAMP无显著改变的情况下发生,因此似乎一条不依赖cAMP的途径参与了血管紧张素II与血管收缩性5 - HT1样受体之间的协同相互作用。

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