Rittenhouse P A, Bakkum E A, Levy A D, Li Q, Yracheta J M, Kunimoto K, van de Kar L D
Department of Pharmacology, Stritch School of Medicine, Loyola University Chicago, Maywood, Ill 60153.
Neuroendocrinology. 1994 Aug;60(2):205-14. doi: 10.1159/000126754.
The aims of the study were to determine; (1) whether activation of serotonin (5-HT) receptors in the brain increases renin secretion, and (2) whether the hypertensive effects of a 5-HT agonist and 5-HT releaser obscure their ability to stimulate renin release. Various drugs that increase serotonergic neuro-transmission can activate the secretion of renin from the kidneys. Many of these drugs can also elevate blood pressure. Changes in blood pressure can alter renin secretion by activating renal baroreceptor mechanisms, so that a decrease in perfusion pressure will increase renin secretion and vice versa. To address the first objective, the 5-HT agonist RU 24969 (0, 10, 100 and 200 micrograms/kg) and the 5-HT releaser p-chloroamphetamine (0, 50, 500 and 1,000 micrograms/kg) were injected intracerebroventricularly (ICV) at doses lower than those that are peripherally effective. ICV injection of RU 24969 dose-dependently increased plasma levels of renin. ICV injection of the 5-HT2A/5-HT2C antagonist LY53857 (50 micrograms/kg) inhibited the renin response to peripherally injected RU 24969 (0, 1, 5 and 10 mg/kg i.p.), suggesting that 5-HT2A/5-HT2C receptors in the brain mediate the effect of peripherally injected RU 24969 on renin secretion. In contrast, ICV injection of p-chloroamphetamine decreased renin secretion. To determine whether hypertensive actions could account for the differences between RU 24969 and p-chloroamphetamine, we measured the effects of both p-chloroamphetamine and RU 24969 on blood pressure and heart rate. ICV injection of p-chloroamphetamine (1,000 micrograms/kg) produced a large rise of 44 mm Hg at 2 min and 25 mm Hg at 5 min after injection, while ICV injection of RU 24969 (200 micrograms/kg) caused a slower and smaller blood pressure elevation of 18 mm Hg at 5 min after injection. To determine whether the hypertensive effects of both RU 24969 and p-chloroamphetamine could mask their effects on renin secretion, rats were pretreated with the alpha 1 antagonist prazosin. Administration of prazosin (1 mg/kg s.c.), which prevents the hypertensive effects of p-chloroamphetamine, exposed a stimulatory effect of ICV-injected p-chloroamphetamine (500 micrograms/kg) on renin secretion and potentiated the effect of RU 24969 (5 mg/kg i.p.) on renin release. In conclusion, these data suggest that both RU 24969 and p-chloroamphetamine increase renin secretion through central 5-HT receptors, and that these effects are partially obscured by their hypertensive actions.
(1)大脑中血清素(5-羟色胺,5-HT)受体的激活是否会增加肾素分泌;(2)5-HT激动剂和5-HT释放剂的高血压作用是否会掩盖它们刺激肾素释放的能力。多种增加血清素能神经传递的药物可激活肾脏肾素的分泌。其中许多药物也可升高血压。血压变化可通过激活肾压力感受器机制改变肾素分泌,因此灌注压降低会增加肾素分泌,反之亦然。为实现第一个目标,将5-HT激动剂RU 24969(0、10、100和200微克/千克)和5-HT释放剂对氯苯丙胺(0、50、500和1000微克/千克)以低于外周有效剂量的剂量进行脑室内(ICV)注射。脑室内注射RU 24969可剂量依赖性地增加血浆肾素水平。脑室内注射5-HT2A/5-HT2C拮抗剂LY53857(50微克/千克)可抑制对腹腔注射(i.p.)外周注射RU 24969(0、1、5和10毫克/千克)的肾素反应,提示大脑中的5-HT2A/5-HT2C受体介导外周注射RU 24969对肾素分泌的作用。相比之下,脑室内注射对氯苯丙胺可降低肾素分泌。为确定高血压作用是否可解释RU 24969和对氯苯丙胺之间的差异,我们测量了对氯苯丙胺和RU 24969对血压和心率的影响。脑室内注射对氯苯丙胺(1000微克/千克)在注射后2分钟使血压大幅升高44毫米汞柱,5分钟时升高25毫米汞柱,而脑室内注射RU 24969(200微克/千克)在注射后5分钟引起较慢且较小的血压升高,为18毫米汞柱。为确定RU 24969和对氯苯丙胺的高血压作用是否会掩盖它们对肾素分泌的影响,用α1拮抗剂哌唑嗪对大鼠进行预处理。给予哌唑嗪(1毫克/千克,皮下注射)可预防对氯苯丙胺的高血压作用,使脑室内注射对氯苯丙胺(500微克/千克)对肾素分泌的刺激作用显现出来,并增强了RU 24969(5毫克/千克,腹腔注射)对肾素释放的作用。总之,这些数据表明,RU 24969和对氯苯丙胺均通过中枢5-HT受体增加肾素分泌,且这些作用部分被它们的高血压作用所掩盖。