Ruwart M J, Klepper M S, Rush B D
J Pharmacol Exp Ther. 1980 Mar;212(3):487-90.
Subcutaneous clonidine (0.01--1.0 mg/kg) was found to delay small intestinal transit but not gastric emptying in the unanesthetized rat, with a maximal effect seen at 0.1 mg/kg. Gastric emptying was expressed as the percentage of intragastrically administered 51Cr emptied into the small intestine after 45 min. Small intestinal transit was the percentage of the small intestinal length traveled 45 min after oral or duodenal administration of black ink. The depression of small intestinal transit by clonidine to 20 to 30% of control values was blocked by phentolamine and yohimbine, but not by prazosin or phenoxybenzamine, suggesting a presynaptic (alpha-2) agonist action of clonidine. Pretreatment of rats with 6-hydroxydopamine, propranolol, atropine, methysergide, naloxone, mepyramine or metiamide failed to alter the effects of clonidine. These results suggest that an alpha adrenergic receptor, possibly presynaptic, regulates small bowel propulsion in rat without involvement of acetylcholine, norepinephrine, endorphins, histamine or serotonin.
皮下注射可乐定(0.01 - 1.0毫克/千克)可延缓未麻醉大鼠的小肠蠕动,但不影响胃排空,最大作用出现在0.1毫克/千克时。胃排空以45分钟后胃内注射的51Cr排入小肠的百分比表示。小肠蠕动以口服或十二指肠注射黑色墨水后45分钟内小肠移动的长度占小肠总长度的百分比表示。可乐定将小肠蠕动抑制至对照值的20%至30%,酚妥拉明和育亨宾可阻断此作用,但哌唑嗪或酚苄明则不能,这表明可乐定具有突触前(α-2)激动剂作用。用6-羟基多巴胺、普萘洛尔、阿托品、甲基麦角新碱、纳洛酮、美吡拉敏或甲硫咪特预处理大鼠,未能改变可乐定的作用。这些结果表明,一种α肾上腺素能受体(可能是突触前的)调节大鼠小肠推进,而不涉及乙酰胆碱、去甲肾上腺素、内啡肽、组胺或5-羟色胺。