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Effects of arterial pressure on drinking and urinary responses to intracerebroventricular angiotensin II.动脉血压对脑室内注射血管紧张素II引起的饮水和排尿反应的影响。
Am J Physiol. 1993 Jan;264(1 Pt 2):R211-7. doi: 10.1152/ajpregu.1993.264.1.R211.
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Block of voltage-dependent sodium currents by the substance P receptor antagonist (+/-)-CP-96,345 in neurones cultured from rat cortex.P物质受体拮抗剂(±)-CP-96,345对大鼠皮层培养神经元中电压依赖性钠电流的阻断作用
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In vivo and in vitro pharmacology of SR 48,968, a non-peptide tachykinin NK2 receptor antagonist.非肽类速激肽NK2受体拮抗剂SR 48,968的体内外药理学研究
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Tachykinin receptors and tachykinin receptor antagonists.速激肽受体与速激肽受体拮抗剂
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The mechanism of central pressor actions of tachykinin NK-3 receptor in the paraventricular nucleus of the hypothalamus in rats.
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Distribution of the substance P receptor (NK-1 receptor) in the central nervous system.
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中枢给予速激肽对大鼠心血管及行为的影响:用选择性拮抗剂对受体进行特性描述

Cardiovascular and behavioural effects of centrally administered tachykinins in the rat: characterization of receptors with selective antagonists.

作者信息

Picard P, Regoli D, Couture R

机构信息

Department of Physiology, Faculty of Medicine, Université de Montréal, Québec, Canada.

出版信息

Br J Pharmacol. 1994 May;112(1):240-9. doi: 10.1111/j.1476-5381.1994.tb13058.x.

DOI:10.1111/j.1476-5381.1994.tb13058.x
PMID:7518304
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1910324/
Abstract
  1. The effects of intracerebroventricular (i.c.v.) injection of selective and potent NK1 (RP 67580), NK2 (SR 48968) and NK3 (R 486, [Trp7, beta-Ala8]NKA(4-10)) receptor antagonists were assessed on the cardiovascular and behavioural responses elicited by the i.c.v. injection of substance P (SP), neurokinin A (NKA) or [MePhe7]neurokinin B ([MePhe7]NKB) in the conscious freely moving rat. 2. SP, NKA and [MePhe7]NKB (5-650 pmol) evoked dose-dependent increases in mean arterial blood pressure (MAP) and heart rate (HR) with the rank order of potency SP > NKA > [MePhe7]NKB. The cardiovascular responses were accompanied by excessive face washing, grooming and wet dog shakes. 3. The cardiovascular effects and face washing behaviour induced by SP (25 pmol) were significantly reduced by the pre-injection (i.c.v., 5 min earlier) of RP 67580 (6.5 nmol). However, this antagonist failed to affect the central effects of 25 pmol NKA or [MePhe7]NKB. 4. The cardiovascular and behavioural responses (except for wet dog shakes) elicited by NKA (25 pmol) were significantly reduced by 6.5 nmol SR 48968. However, the latter antagonist had no effect on the SP or [MePhe7]NKB-mediated responses. 5. Both cardiovascular and behavioural effects produced by either SP or NKA (25 pmol) were completely abolished when rats were pretreated with a combination of RP 67580 (6.5 nmol) and SR 48968 (6.5 nmol), yet this combination of antagonists failed to modify the central effects of [MePhe7]NKB. 6. R 486 (6.5 nmol) inhibited the cardiovascular effects as well as wet dog shakes produced by [MePhe7]NKB, but it was inactive against the responses induced by either SP or NKA. 7. None of the tachykinin receptor antagonists or agonists caused motor impairment or respiratory distress. All antagonists blocked in a reversible manner and were devoid of intrinsic activity except R486 (6.5 nmol) which produced a transient increase of MAP and HR.8. These results suggest that the central effects of SP, NKA and [MePhe7]NKB are primarily mediated by central NK1, NK2 and NK3 receptors, respectively. However, a minor activation of NK2 receptors bySP and NK1 receptors by NKA was seen during blockade of both receptors. This study therefore supports the existence of functional NK1, NK2 and NK3 receptors in the adult rat brain.
摘要
  1. 研究评估了脑室内(i.c.v.)注射选择性强效NK1(RP 67580)、NK2(SR 48968)和NK3(R 486,[Trp7,β - Ala8]NKA(4 - 10))受体拮抗剂对清醒自由活动大鼠脑室内注射P物质(SP)、神经激肽A(NKA)或[MePhe7]神经激肽B([MePhe7]NKB)所引发的心血管和行为反应的影响。2. SP、NKA和[MePhe7]NKB(5 - 650 pmol)引起平均动脉血压(MAP)和心率(HR)呈剂量依赖性升高,其效力顺序为SP > NKA > [MePhe7]NKB。心血管反应伴有过度洗脸、梳理毛发和像湿狗一样抖动。3. RP 67580(6.5 nmol)预先注射(脑室内,提前5分钟)可显著降低SP(25 pmol)诱导的心血管效应和洗脸行为。然而,该拮抗剂未能影响25 pmol NKA或[MePhe7]NKB的中枢效应。4. SR 48968(6.5 nmol)可显著降低NKA(25 pmol)引发的心血管和行为反应(除像湿狗一样抖动外)。然而,后一种拮抗剂对SP或[MePhe7]NKB介导的反应无影响。5. 当大鼠用RP 67580(6.5 nmol)和SR 48968(6.5 nmol)联合预处理时,SP或NKA(25 pmol)产生的心血管和行为效应均完全被消除,但这种拮抗剂组合未能改变[MePhe7]NKB的中枢效应。6. R 486(6.5 nmol)抑制[MePhe7]NKB产生的心血管效应以及像湿狗一样抖动,但对SP或NKA诱导的反应无活性。7. 速激肽受体拮抗剂或激动剂均未引起运动障碍或呼吸窘迫。所有拮抗剂均以可逆方式阻断且无内在活性,除R486(6.5 nmol)可使MAP和HR短暂升高。8. 这些结果表明,SP、NKA和[MePhe7]NKB的中枢效应分别主要由中枢NK1、NK2和NK3受体介导。然而,在两种受体被阻断期间,观察到SP对NK2受体有轻微激活作用,NKA对NK1受体有轻微激活作用。因此本研究支持成年大鼠脑中存在功能性NK1、NK2和NK3受体。