Sugrue M F
J Pharm Pharmacol. 1984 Aug;36(8):548-9. doi: 10.1111/j.2042-7158.1984.tb04450.x.
A 1 h pretreatment with s.c. mianserin (0.5 mg kg-1) markedly blunted the oedema of the rat paw induced by the subplantar injection of 5-HT (5 micrograms). In contrast, i.p. mianserin (same dose) failed to modify 5-HT-induced oedema. However, pretreatment with SKF-525-A (40 mg kg-1) resulted in a profound potentiation of the action of i.p. mianserin, the effect of the combination of SKF-525-A and i.p. mianserin rivaling that of s.c. mianserin. It is concluded that i.p. mianserin is metabolized by the rat liver to compounds which possess a reduced propensity to block peripheral 5-HT receptors and that the i.p. route of administration is not to be recommended when mianserin is being studied as a 5-HT receptor antagonist in the rat.
皮下注射米安色林(0.5毫克/千克)进行1小时预处理,可显著减轻足底注射5-羟色胺(5微克)所致的大鼠爪部水肿。相比之下,腹腔注射米安色林(相同剂量)未能改变5-羟色胺诱导的水肿。然而,用SKF-525-A(40毫克/千克)预处理可导致腹腔注射米安色林的作用显著增强,SKF-525-A与腹腔注射米安色林联合使用的效果可与皮下注射米安色林相媲美。得出的结论是,腹腔注射米安色林在大鼠肝脏中被代谢为阻断外周5-羟色胺受体倾向降低的化合物,并且当将米安色林作为大鼠5-羟色胺受体拮抗剂进行研究时,不推荐采用腹腔注射途径给药。