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速激肽受体介导体内阿托品抵抗性大鼠十二指肠反射性收缩。

Tachykinin receptors mediate atropine-resistant rat duodenal reflex contractions in vivo.

作者信息

Giuliani S, Tramontana M, Lecci A, Maggi C A

机构信息

Pharmacology Department, Research Laboratories, Menarini Ricerche, Florence, Italy.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1996 Aug-Sep;354(3):327-35. doi: 10.1007/BF00171064.

Abstract

The study aimed to establish the possible role of tachykinins as mediators of atropine-resistant reflex contractions evoked by balloon distension in the proximal duodenum of urethane-anesthetized, guanethidine (34 mumol/kg s.c.)-pretreated rats. Distension of the balloon with a small amount (0.2-0.3 ml) of saline induced the appearance of phasic rhythmic contractions (about 11 mmHg in amplitude) which were promptly suppressed by either atropine (3 mumol/kg i.v.) or hexamethonium (28 mumol/kg i.v.). Despite the continuous i.v. infusion of atropine (2 mumol/h), low-amplitude rhythmic phasic contractions recovered, which were promptly suppressed by hexamethonium, to indicate the involvement of an atropine-resistant excitatory reflex. The amplitude of these atropine-resistant contractions was increased to about 4-5 mmHg by further distension of the balloon (0.4-0.6 ml) : under these conditions, the atropine-resistant contractions undergo a progressive fading. The fading was prevented by i.v. administration of the nitric oxide (NO) synthase inhibitor, L-nitroarginine methyl ester (L-NAME, 55 mumol/h), to provide a suitable baseline (amplitude of contractions was 7-8 mmHg) for studying the effect of tachykinin receptor antagonists. I.v. administration of the selective tachykinin NK2 receptor antagonists, MEN 10,627 (10-100 nmol/kg) and SR 48968 (100-300 nmol/kg) or of the selective NK1 antagonist SR 140333 (100 nmol/kg), at doses which do not affect the duodenal contractions induced by acetylcholine (5.5 mumol/kg i.v.), produced a prompt and long lasting suppression of the atropine-resistant reflex duodenal contractions produced by balloon distension in urethane-anesthetized rats, whilst SR-48965 (300 nmol/kg), the enantiomer of SR-48968 devoid, of NK2 receptor blocking activity, was without effect. I.v. administration of the selective NK1 receptor agonists [Sar9] substance P sulfone and septide or of the NK2 receptor selective agonist, [beta Ala8] neurokinin A(4-10) produced dose-dependent contractions of the duodenum. SR 140333 (100 nmol/kg i.v.) selectively antagonized the duodenal contractions produced by [Sar9] substance P sulfone and septide without affecting those produced by [beta Ala8] neurokinin A(4-10). On the other hand, MEN 10,627 (30-100 nmol/kg i.v.) and SR 48968 (100-300 nmol/kg i.v.) but not SR 48965 (300 nmol/kg i.v.) antagonized, at a comparable extent, duodenal contractions induced by both the selective NK2 and NK1 receptor agonists. We conclude that endogenous tachykinins are involved in mediating atropine-resistant reflex contractions evoked by distension of the rat duodenum in vivo: both NK1 and NK2 receptors are activated by endogenous ligands to produce NANC contractions of rat duodenum in vivo. However, the contractile response to i.v. administered NK1 receptor agonists, [Sar9] substance P sulfone and septide, may involve the release of mediators producing smooth muscle contraction via NK2 receptors.

摘要

本研究旨在确定速激肽在由气囊扩张诱发的抗阿托品反射性收缩中可能发挥的介导作用,该反射性收缩发生在经氨基甲酸乙酯麻醉、给予胍乙啶(34 μmol/kg,皮下注射)预处理的大鼠的十二指肠近端。用少量(0.2 - 0.3 ml)生理盐水扩张气囊会诱发相性节律性收缩(幅度约为11 mmHg),这些收缩会被阿托品(3 μmol/kg,静脉注射)或六甲铵(28 μmol/kg,静脉注射)迅速抑制。尽管持续静脉输注阿托品(2 μmol/h),低幅度的节律性相性收缩仍会恢复,而六甲铵能迅速抑制这些收缩,这表明存在一种抗阿托品的兴奋性反射。通过进一步扩张气囊(0.4 - 0.6 ml),这些抗阿托品收缩的幅度增加到约4 - 5 mmHg:在这些条件下,抗阿托品收缩会逐渐消退。静脉注射一氧化氮(NO)合酶抑制剂L - 硝基精氨酸甲酯(L - NAME,55 μmol/h)可防止这种消退,从而为研究速激肽受体拮抗剂的作用提供合适的基线(收缩幅度为7 - 8 mmHg)。静脉注射选择性速激肽NK2受体拮抗剂MEN 10,627(10 - 100 nmol/kg)和SR 48968(100 - 300 nmol/kg)或选择性NK1拮抗剂SR 140333(100 nmol/kg),在不影响乙酰胆碱(5.5 μmol/kg,静脉注射)诱导的十二指肠收缩的剂量下,能迅速且持久地抑制经氨基甲酸乙酯麻醉的大鼠中由气囊扩张产生的抗阿托品反射性十二指肠收缩,而SR - 48965(300 nmol/kg),即缺乏NK2受体阻断活性的SR - 48968的对映体,则无此作用。静脉注射选择性NK1受体激动剂[Sar9]P物质砜和septide或NK2受体选择性激动剂[βAla8]神经激肽A(4 - 10)会产生十二指肠的剂量依赖性收缩。SR 140333(100 nmol/kg,静脉注射)选择性地拮抗[Sar9]P物质砜和septide产生的十二指肠收缩,而不影响[βAla8]神经激肽A(4 - 10)产生的收缩。另一方面,MEN 10,627(30 - 100 nmol/kg,静脉注射)和SR 48968(100 - 300 nmol/kg,静脉注射)但不是SR 48965(300 nmol/kg,静脉注射)在相当程度上拮抗了由选择性NK2和NK1受体激动剂诱导的十二指肠收缩。我们得出结论,内源性速激肽参与介导体内大鼠十二指肠扩张诱发的抗阿托品反射性收缩:NK1和NK2受体均被内源性配体激活,从而在体内产生大鼠十二指肠的非肾上腺素能非胆碱能收缩。然而,对静脉注射NK1受体激动剂[Sar9]P物质砜和septide的收缩反应可能涉及通过NK2受体释放产生平滑肌收缩的介质。

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