Ramabadran K, Bansinath M, Turndorf H, Puig M M
Department of Anesthesiology, School of Medicine, New York University Medical Center, NY 10016.
Eur J Pharmacol. 1988 Oct 18;155(3):329-31. doi: 10.1016/0014-2999(88)90524-9.
Systemic administration of highly selective kappa opiate agonists, U-50488H and U-69593 (3, 10 and 30 mg/kg i.p.) produced significant inhibition of the gastrointestinal transit in mice as assessed by charcoal meal test. In contrast, the (+) stereoisomer of U-50488H, U-53455E did not inhibit the gastrointestinal motility. Furthermore, the kappa-selective antagonist, Mr 2266 (3 mg/kg) when administered along with the agonists, reversed the effects of the agonists. These results suggest that stereospecific kappa opiate receptors are involved in inhibition of gut motility in mice.
通过炭末试验评估，对小鼠腹腔注射高选择性κ阿片受体激动剂U - 50488H和U - 69593（3、10和30毫克/千克）进行全身给药，可显著抑制其胃肠蠕动。相比之下，U - 50488H的（+）立体异构体U - 53455E不会抑制胃肠蠕动。此外，κ选择性拮抗剂Mr 2266（3毫克/千克）与激动剂同时给药时，可逆转激动剂的作用。这些结果表明，立体特异性κ阿片受体参与了对小鼠肠道蠕动的抑制。
