Kappa-opiate-induced diuresis and changes in blood pressure: demonstration of receptor stereoselectivity using (+)- and (-)-tifluadom.
Kappa-opiate-induced diuresis and changes in blood pressure: demonstration of receptor stereoselectivity using (+)- and (-)-tifluadom.
复制标题
Kappa-鸦片诱导的利尿和血压变化：使用 ( )- 和 (-)-tifluadom 演示受体立体选择性。
DOI：
10.1016/0014-2999(87)90677-7
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发表时间：
1987
影响因子：
5
通讯作者：
J. Huidobro
中科院分区：
文献类型：
--
作者：
H. Ureta;L. López;A. Pérez;J. Huidobro
(+)-静脉注射替氟多姆。产生了尿量的两相反应：在给药的第一个小时内，该药物产生了抗利尿作用，随后是利尿期。相比之下，与生理盐水处理的大鼠相比，(−)异构体产生的尿量略有减少。此外，(+)-替氟多姆还能显著减少尿Na+和K+的排出。(+)-替氟多姆的作用可被7.5 mg/kg纳洛酮阻断，但不能被苯二氮类拮抗剂Ro 15-1788阻断。平行实验证明，静脉注射。给非麻醉大鼠注射(+)-替氟多姆可引起持续至少15分钟的剂量相关升压反应。(+)-替氟多姆的这种作用可被纳洛酮阻断和拮抗。相比之下，(−)-替氟多姆要么对心血管系统不起作用，要么产生短暂的低血压。在戊巴比妥钠麻醉的大鼠中，100μg/kg(+)-替氟多姆引起的急剧低血压可被纳洛酮逆转，但不能被RO15-1788逆转。
(+)-Tifluadom injected i.p. produced a biphasic response of urine output: within the first hour of its administration the drug produced antidiuresis followed by a diuretic phase. In contrast, the (−) isomer produced a modest reduction in urine output as compared to the output of the saline-treated rats. In addition, (+)-tifluadom markedly reduced the output of urinary Na+and K+. The effects of (+)-tifluadom were blocked by 7.5 mg/kg naloxone but not by 10 mg/kg of the benzodiazepine antagonist Ro 15-1788. Parallel experiments demonstrated that the i.v. administration of (+)-tifluadom to non-anesthetized rats caused a dose-related pressor response that lasted for at least 15 min. This effect of (+)-tifluadom was blocked and antagonized by naloxone. In contrast, (−)-tifluadom was either inactive on the cardiovascular system or produced short-lasting hypotension. In pentobarbital-anesthetized rats, 100 μg/kg (+)-tifluadom caused a precipitous hypotension that was reversed by naloxone but not by Ro 15-1788.
DOI：
--
发表时间：
1982-03
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
S. Ward;P. Portoghese;A. Takemori
通讯作者：
S. Ward;P. Portoghese;A. Takemori