首页> 外国专利> TREATMENT OF HYPERTENSION WITH COMPOUNDS THAT INHIBIT THE DESTRUCTION OF ENKEPHALINS OR ENDORPHINS

TREATMENT OF HYPERTENSION WITH COMPOUNDS THAT INHIBIT THE DESTRUCTION OF ENKEPHALINS OR ENDORPHINS

机译:用抑制脑啡肽或内啡肽破坏的化合物治疗高血压

摘要

A new class of anti-hypertensive agent is provided by substances that inhibit the breakdown of the endogenous substances, the enkephalins and/or the endorphins. The anti-hypertensive effect of an enkephalin breakdown inhibitor is greatly enhanced by being combined with a beta adrenergic blocking agent, herein designated as beta blocker. Specifically, D-phenylalanine, en enkephalin breakdown inhibitor when used alone produces excellent blood pressure lowering in animals and man. Use of a combination of D-phenylalanine and the beta blocker propranolol provides a greatly enhanced anti-hypertensive effect in the spontaneously hypertensive rat (SHR). Blood pressure lowering by D-phenylalanine, or the latter combination, is very long lasting in the SHR and man. If the blood pressure of the rat or human is normal, D-phenylalanine has little or no effect on blood pressure. The hypotensive effect of D-phenylalanine is prevented by pretreating the SHR with naloxone or naltrexone which are specific antagonists of enkephalins or endorphins.
机译:抑制内源性物质,脑啡肽和/或内啡肽分解的物质提供了一类新的抗高血压药。脑啡肽分解抑制剂的抗高血压作用通过与β肾上腺素能阻断剂(在本文中称为β受体阻滞剂)组合使用而大大增强。具体而言,当单独使用D-苯丙氨酸和脑啡肽分解抑制剂时,可在动物和人类中降低血压。 D-苯丙氨酸和β受体阻滞剂普萘洛尔的组合使用可大大增强自发性高血压大鼠(SHR)的抗高血压作用。在SHR和男性中,通过D-苯丙氨酸或后者的组合使血压降低的持续时间很长。如果大鼠或人的血压正常,则D-苯丙氨酸对血压几乎没有影响。通过用纳洛酮或纳曲酮预处理SHR来预防D-苯丙氨酸的降压作用,纳洛酮或纳曲酮是脑啡肽或内啡肽的特异性拮抗剂。

著录项

  • 公开/公告号EP1158972A4

    专利类型

  • 公开/公告日2003-05-02

    原文格式PDF

  • 申请/专利权人 EHRENPREIS SEYMOUR;BLUM KENNETH;

    申请/专利号EP20000903252

  • 发明设计人 EHRENPREIS SEYMOUR;BLUM KENNETH;

    申请日2000-01-12

  • 分类号A61K45/00;A61K31/198;A61K31/401;A61K31/52;A61P9/12;

  • 国家 EP

  • 入库时间 2022-08-21 23:51:56

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