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部分阿片受体激动剂地佐辛和环拉马朵在猫回盲括约肌处作为μ受体拮抗剂发挥作用。

The partial opiate receptor agonists, dezocine and ciramadol act as mu receptor antagonists at the feline ileocecal sphincter.

作者信息

Ouyang A

机构信息

Gastrointestinal Section, Hospital of the University of Pennsylvania, Philadelphia 19104-4283.

出版信息

Life Sci. 1989;45(16):1491-7. doi: 10.1016/0024-3205(89)90040-4.

DOI:10.1016/0024-3205(89)90040-4
PMID:2572952
Abstract

The effects of two novel synthetic narcotic agonist/antagonists dezocine and ciramadol were examined at the ileocecal sphincter (ICS) in the intact anesthetized cat. Changes in blood pressure were seen with higher doses of both dezocine and ciramadol. No ICS pressure changes were seen in the ICS to dezocine and an increase in ICS pressure was seen only to the highest dose of ciramadol examined (10 mg/kg). The antagonist action of the two drugs were examined against submaximal doses of the mu receptor agonist morphine sulfate, delta receptor agonist methionine enkephalin and the k-receptor agonist dynorphin. Both drugs inhibit the ICS response to morphine sulfate. No inhibition of the responses to methionine enkephalin or dynorphin were seen with dezocine and only partial inhibition of the ICS response to dynorphin was seen with ciramadol.

摘要

在完整的麻醉猫的回盲括约肌(ICS)处检测了两种新型合成麻醉性激动剂/拮抗剂地佐辛和环拉朵的作用。给予较高剂量的地佐辛和环拉朵后均出现血压变化。地佐辛对ICS压力无影响,仅在检测的最高剂量环拉朵(10mg/kg)时观察到ICS压力升高。检测了这两种药物对μ受体激动剂硫酸吗啡、δ受体激动剂甲硫氨酸脑啡肽和κ受体激动剂强啡肽的次最大剂量的拮抗作用。两种药物均抑制ICS对硫酸吗啡的反应。地佐辛对甲硫氨酸脑啡肽或强啡肽的反应无抑制作用,环拉朵仅对ICS对强啡肽的反应有部分抑制作用。

相似文献

1
The partial opiate receptor agonists, dezocine and ciramadol act as mu receptor antagonists at the feline ileocecal sphincter.部分阿片受体激动剂地佐辛和环拉马朵在猫回盲括约肌处作为μ受体拮抗剂发挥作用。
Life Sci. 1989;45(16):1491-7. doi: 10.1016/0024-3205(89)90040-4.
2
Hemodynamic and respiratory effects of dezocine, ciramadol, and morphine.地佐辛、环拉马朵和吗啡对血流动力学及呼吸的影响。
Clin Pharmacol Ther. 1985 Jul;38(1):84-8. doi: 10.1038/clpt.1985.139.
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Characterization of opiate-mediated responses of the feline ileum and ileocecal sphincter.猫回肠和回盲括约肌阿片介导反应的特征
J Clin Invest. 1982 Mar;69(3):507-15. doi: 10.1172/jci110476.
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Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists.混合阿片类激动剂/拮抗剂地佐辛的辨别性刺激效应:μ和δ阿片类激动剂的交叉替代作用
J Pharmacol Exp Ther. 1997 Dec;283(3):1009-17.
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Sites of action of mu-, kappa- and sigma-opiate receptor agonists at the feline ileocecal sphincter.μ、κ和σ阿片受体激动剂在猫回盲括约肌的作用部位。
Am J Physiol. 1988 Feb;254(2 Pt 1):G224-31. doi: 10.1152/ajpgi.1988.254.2.G224.
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