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将5-羟色胺1A受体激动剂微量注射到麻醉大鼠的中缝隐核后产生的升压效应。

Pressor effects following microinjection of 5-HT1A receptor agonists into the raphe obscurus of the anaesthetized rat.

作者信息

Dreteler G H, Wouters W, Saxena P R, Ramage A G

机构信息

Academic Department of Pharmacology, Royal Free Hospital School of Medicine, Hampstead, London.

出版信息

Br J Pharmacol. 1991 Feb;102(2):317-22. doi: 10.1111/j.1476-5381.1991.tb12172.x.

Abstract
  1. The effects of electrical stimulation and microinjections (90 nl) of the 5-HT1A receptor agonists, flesinoxan and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), and glutamate into the raphe obscurus on blood pressure, heart rate and phrenic nerve activity (central inspiratory drive) were investigated in rats anaesthetized with alpha-chloralose. 2. Electrical stimulation of the raphe obscurus caused a rise in blood pressure which was associated with bradycardia, while glutamate (2.7 nmol) caused only a rise in blood pressure. 3. Flesinoxan (1.3 nmol) and 8-OH-DPAT (0.7 nmol) increased blood pressure by 9 +/- 1 and 14 +/- 2 mmHg, respectively and did not affect heart rate. For both agonists the effect on blood pressure was shown to be dose-dependent; again no effect on the heart rate was observed over the dose-ranges chosen. 4. Microinjections of the non-selective 5-HT1A receptor antagonists, (+/-)-pindolol (2.7 nmol) or methiothepin (5.2 nmol), into the raphe obscurus prevented the increase in blood pressure caused by microinjection of flesinoxan. However, (+/-)-pindolol caused a sustained rise in blood pressure of 15 +/- 1 mmHg while methiothepin caused a transient rise in blood pressure. Neither drugs affected heart rate. The ability of methiothepin to attenuate the pressor effect of flesinoxan was found to be partially reversed after 30 min. 5. It is suggested that activation of 5-HT1A receptors within the raphe obscurus can cause sympatho-excitation.
摘要
  1. 研究了在α-氯醛糖麻醉的大鼠中,向中缝隐核电刺激以及微量注射(90纳升)5-HT1A受体激动剂氟司必林和8-羟基-2-(二正丙基氨基)四氢萘(8-OH-DPAT)和谷氨酸对血压、心率及膈神经活动(中枢吸气驱动)的影响。2. 中缝隐核的电刺激导致血压升高并伴有心动过缓,而谷氨酸(2.7纳摩尔)仅引起血压升高。3. 氟司必林(1.3纳摩尔)和8-OH-DPAT(0.7纳摩尔)分别使血压升高9±1和14±2毫米汞柱,且不影响心率。两种激动剂对血压的作用均呈剂量依赖性;在所选择的剂量范围内,对心率均无影响。4. 向中缝隐核微量注射非选择性5-HT1A受体拮抗剂(±)-吲哚洛尔(2.7纳摩尔)或甲硫噻平(5.2纳摩尔)可阻止氟司必林微量注射引起的血压升高。然而,(±)-吲哚洛尔使血压持续升高15±1毫米汞柱,而甲硫噻平使血压短暂升高。两种药物均不影响心率。发现30分钟后甲硫噻平减弱氟司必林升压作用的能力部分逆转。5. 提示中缝隐核内5-HT1A受体的激活可引起交感兴奋。

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