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替氟朵姆诱导大鼠利尿。阿片受体介导的中枢作用证据。

Tifluadom-induced diuresis in rats. Evidence for an opioid receptor-mediated central action.

作者信息

Shearman G T, Tolcsvai L

出版信息

Neuropharmacology. 1986 Aug;25(8):853-6. doi: 10.1016/0028-3908(86)90010-9.

Abstract

Tifluadom dose-dependently induced diuresis in rats after subcutaneous injection and oral application. (+)Tifluadom was at least 100-fold more potent than the (-)enantiomer in inducing diuresis. The diuretic action of tifluadom was dose-relatedly reduced by the opioid receptor antagonists naloxone and MR 2266. Naloxone methobromide did not antagonize the diuretic effect of tifluadom nor did the benzodiazepine receptor blocker Ro 15-1788. These data demonstrate that the diuretic effect of tifluadom is mediated centrally via an agonistic interaction between the drug and opioid receptors.

摘要

替氟朵美皮下注射和口服给药后,在大鼠中呈剂量依赖性地诱导利尿作用。(+)替氟朵美在诱导利尿方面的效力比(-)对映体至少强100倍。阿片受体拮抗剂纳洛酮和MR 2266可剂量依赖性地降低替氟朵美的利尿作用。甲溴酸纳洛酮不拮抗替氟朵美的利尿作用,苯二氮䓬受体阻滞剂Ro 15-1788也无此作用。这些数据表明,替氟朵美的利尿作用是通过药物与阿片受体之间的激动性相互作用在中枢介导的。

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