Ouyang A
Gastrointestinal Section, Hospital of the University of Pennsylvania, Philadelphia 19104-4283.
Life Sci. 1989;45(16):1491-7. doi: 10.1016/0024-3205(89)90040-4.
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.
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。