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NK1和NK2受体在豚鼠非肾上腺素能、非胆碱能迷走神经刺激引发的肺部反应中的作用。

Involvement of NK1 and NK2 receptors in pulmonary responses elicited by non-adrenergic, non-cholinergic vagal stimulation in guinea-pigs.

作者信息

Savoie C, Tousignant C, Rodger I W, Chan C C

机构信息

Department of Pharmacology, Merck Frosst Centre for Therapeutic Research, Kirkland, Quebec, Canada.

出版信息

J Pharm Pharmacol. 1995 Nov;47(11):914-20. doi: 10.1111/j.2042-7158.1995.tb03270.x.

Abstract

Previous studies from our laboratory using exogenously administered neurokinin (NK) agonists have shown that both NK1- and NK2-receptor subtypes are involved in plasma extravasation in the guinea-pig airways. In the present study, we have extended these observations using antidromic vagal stimulation to stimulate sensory c-fibres as a means of eliciting the release of endogenous tachykinins in propranolol- and atropine-treated guinea-pigs. Antidromic vagal stimulation (5 ms, 30 s) induced frequency-dependent (1-10 Hz) bronchoconstriction that was completely abolished by co-administration of the NK1-selective antagonist CP-99,994 ((2s-methoxy-benzyl)-(2-phenyl-piperidin-3s-yl)-amine), and the NK2-selective antagonist SR-48,968 ((S)-N-methyl-N-[4-(4-acetylamino-4-phenyl piperidino)-2-(3,4-dichlorophenyl) butyl]benzamide), each at a dose sufficient to block NK1 and NK2 receptors, respectively (each at 0.3 mg kg-1, i.v.). In contrast, SR-48,968 when given alone only partially blocked the vagal stimulation-induced bronchospasm, whereas CP-99,994 had no effect. Significant increases (2-3-fold) in plasma extravasation of [125I]fibrinogen in the trachea, main bronchi, distal airways and oesophagus following vagal stimulation (5 Hz, 5 min, 10 V, 5 ms) were observed. Pretreatment with the neutral endopeptidase inhibitor, thiorphan (1 mg kg-1, i.v.), and the angiotensin-converting enzyme inhibitor, enalapril (1 mg kg-1, i.v.), potentiated both vagal stimulation-induced bronchoconstriction and plasma leakage in all tissues examined. This potentiation was due to reduced metabolism of endogenously released tachykinins since enhanced plasma overflow of immunoreactive substance P was observed following vagal stimulation in thiorphan- and enalapril-treated guinea-pigs. CP-99,994 substantially blocked plasma leakage in all parts of the airways and in the oesophagus. In comparison, SR-48,968 had no significant effect in the trachea and the oesophagus but partially inhibited plasma leakage in the main bronchi and distal airways. Co-administration of both CP-99,994 and SR-48,968 abolished the residual plasma leakage in these two regions. These results support the hypothesis that both NK1 and NK2 receptors are involved in tachykinin-induced pulmonary responses in the airways.

摘要

我们实验室之前使用外源性给予神经激肽(NK)激动剂的研究表明,NK1和NK2受体亚型均参与豚鼠气道的血浆外渗。在本研究中,我们通过逆向迷走神经刺激来刺激感觉C纤维,以此作为在普萘洛尔和阿托品处理的豚鼠中引发内源性速激肽释放的一种手段,从而扩展了这些观察结果。逆向迷走神经刺激(5毫秒,30秒)诱导了频率依赖性(1 - 10赫兹)的支气管收缩,当联合给予NK1选择性拮抗剂CP - 99,994((2s - 甲氧基 - 苄基)-(2 - 苯基 - 哌啶 - 3s - 基)-胺)和NK2选择性拮抗剂SR - 48,968((S)-N - 甲基 - N - [4-(4 - 乙酰氨基 - 4 - 苯基哌啶基)-2-(3,4 - 二氯苯基)丁基]苯甲酰胺)时,这种收缩完全被消除,每种拮抗剂的剂量分别足以阻断NK1和NK2受体(均为静脉注射0.3毫克/千克)。相比之下,单独给予SR - 48,968仅部分阻断迷走神经刺激诱导的支气管痉挛,而CP - 99,994则没有作用。在迷走神经刺激(5赫兹,5分钟,10伏,5毫秒)后,观察到气管、主支气管、远端气道和食管中[125I]纤维蛋白原的血浆外渗显著增加(2 - 3倍)。用中性内肽酶抑制剂硫丙苯丙氨酸(静脉注射1毫克/千克)和血管紧张素转换酶抑制剂依那普利(静脉注射1毫克/千克)预处理,增强了在所有检测组织中迷走神经刺激诱导的支气管收缩和血浆渗漏。这种增强是由于内源性释放的速激肽代谢减少,因为在硫丙苯丙氨酸和依那普利处理的豚鼠中,迷走神经刺激后观察到免疫反应性P物质的血浆溢出增加。CP - 99,994基本上阻断了气道所有部位和食管中的血浆渗漏。相比之下,SR - 48,968在气管和食管中没有显著作用,但部分抑制了主支气管和远端气道中的血浆渗漏。联合给予CP - 99,994和SR - 48,968消除了这两个区域残留的血浆渗漏。这些结果支持了NK1和NK2受体均参与速激肽诱导的气道肺部反应这一假说。

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