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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Agonist/antagonist properties of nalbuphine, butorphanol and (-)-pentazocine in male vs. female rats.
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Agonist/antagonist properties of nalbuphine, butorphanol and (-)-pentazocine in male vs. female rats.

机译：纳布啡，丁啡诺和（-）-喷他佐辛在雄性与雌性大鼠中的激动剂/拮抗剂特性。

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To determine whether sex differences in the effects of mixed-action opioids could be due to differential activity at mu or kappa receptors, agonist/antagonist properties of nalbuphine, butorphanol and (-)-pentazocine were compared in male vs. female rats using a diuresis test. In water-loaded rats (2-h test), nalbuphine and (-)-pentazocine dose-dependently increased urination similarly in both sexes, whereas butorphanol increased urination more in females than in males on a ml/kg basis. The diuretic effects of all three opioids were at least partially blocked by the kappa receptor-selective antagonist nor-binaltorphimine (nor-BNI, 5 mg/kg) in both sexes. Kappa receptor-mediated antagonism of diuresis induced by U69,593 (0.56 mg/kg) was only observed with butorphanol in males. In water-loaded rats (1-h test), nalbuphine did not suppress, and butorphanol and (-)-pentazocine significantly suppressed urination in males only; all three mixed-action opioids dose-dependently blocked the antidiuretic effect ofthe selective mu agonist fentanyl (0.056 mg/kg) in both sexes. The ability of nalbuphine and (-)-pentazocine to block fentanyl-induced antidiuresis was not affected by pretreatment with nor-BNI in either sex. In contrast, the ability of butorphanol to block fentanyl-induced antidiuresis was attenuated by pretreatment with nor-BNI in males but not in females. These results suggest that sex differences in the effects of these mixed-action opioids are primarily due to their greater relative efficacy at the mu receptor in male than in female rats; butorphanol also may have greater efficacy at kappa receptors in females than in males.
机译：为了确定混合作用阿片类药物作用中的性别差异是否可能是由于对mu或kappa受体的活性不同所致，比较了利尿剂对雄性和雌性大鼠中纳布啡，丁苯啡诺和（-）-戊唑嗪的激动剂/拮抗剂特性测试。在载水量大的大鼠（2-h试验）中，纳布啡和（-）-喷他佐辛在男女中剂量依赖性地增加排尿量，而以毫升/千克计，丁苯啡诺在雌性中的排泄量比雄性更多。在男女中，所有三种阿片类药物的利尿作用至少部分被κ受体选择性拮抗剂去甲双萘酚（nor-BNI，5 mg / kg）阻断。仅在男性中使用布托啡诺观察到由U69,593（0.56 mg / kg）引起的Kappa受体介导的利尿拮抗作用。在负荷水的大鼠中（1-h试验），纳布啡没有抑制作用，而丁苯啡诺和（-）-戊唑嗪仅能显着抑制雄性排尿。这三种混合作用的阿片类药物均以剂量依赖性地阻断了选择性亩激动剂芬太尼（0.056 mg / kg）的抗利尿作用。两种性别的nor-BNI预处理均不影响纳布啡和（-）-戊唑嗪阻断芬太尼诱导的抗利尿作用的能力。相比之下，男性用nor-BNI预处理可减弱丁烷酚阻止芬太尼诱导的利尿作用的能力，而女性则不然。这些结果表明，这些混合作用阿片类药物作用的性别差异主要是由于它们在雄性大鼠中对mu受体的相对功效大于雌性大鼠;与男性相比，布托啡诺对女性的Kappa受体的疗效也可能更高。

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