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阿片肽对犬食管下括约肌神经元诱导舒张的抑制作用。

Inhibition of neuronally induced relaxation of canine lower esophageal sphincter by opioid peptides.

作者信息

Barnette M S, Grous M, Manning C D, Callahan J F, Barone F C

机构信息

Department of Pharmacology, Smith Kline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939.

出版信息

Eur J Pharmacol. 1990 Jul 3;182(2):363-8. doi: 10.1016/0014-2999(90)90295-h.

Abstract

Opioid peptides have profound effects on gut motility. To assess their actions on enteric neurons regulating sphincteric smooth muscle, the ability of several opioid agonists to antagonize the neuronally induced relaxation of canine lower esophageal sphincter smooth muscle was examined. Opioid peptides selective for mu (FK 33-824) or delta [( D-Pen2,D-Pen5]enkephalin) receptors produced a concentration dependent inhibition of electrical field stimulation (EFS)-induced relaxation. In contrast, neither kappa (ketocycloclazine) or sigma (SK & F 10047) opioid agonists were potent inhibitors of EFS-induced relaxation. This inhibition was relatively selective for opioid agonists since BHT 933 (alpha 2 adrenoceptor agonist) and SK & F 89124 (D2 dopamine agonist) did not inhibit EFS-induced relaxation. Furthermore, naloxone antagonized the effects of both FK 33-824 and DPDPE. These functional data suggest that opioid receptors are present on sphincteric intrinsic inhibitory neurons and that stimulation of these neuronal receptors can regulate lower esophageal sphincter relaxation.

摘要

阿片肽对肠道运动有深远影响。为了评估它们对调节括约肌平滑肌的肠神经元的作用,研究了几种阿片类激动剂拮抗犬食管下括约肌平滑肌神经元诱导的舒张的能力。对μ(FK 33 - 824)或δ[(D - Pen2,D - Pen5]脑啡肽)受体有选择性的阿片肽产生了浓度依赖性的电场刺激(EFS)诱导舒张的抑制作用。相比之下,κ(酮环唑嗪)或σ(SK & F 10047)阿片类激动剂都不是EFS诱导舒张的有效抑制剂。这种抑制作用对阿片类激动剂具有相对选择性,因为BHT 933(α2肾上腺素能受体激动剂)和SK & F 89124(D2多巴胺激动剂)不抑制EFS诱导的舒张。此外,纳洛酮拮抗FK 33 - 824和DPDPE的作用。这些功能数据表明,阿片受体存在于括约肌内在抑制性神经元上,并且刺激这些神经元受体可以调节食管下括约肌的舒张。

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