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首页> 外文期刊>Journal of applied toxicology >The pharmacological properties of anisodamine.
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The pharmacological properties of anisodamine.

机译:山iso碱的药理特性。

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Anisodamine is a naturally occurring atropine derivative that has been isolated, synthesized and characterized by scientists in the People's Republic of China. Like atropine and scopolamine, anisodamine is a non-specific cholinergic antagonist exhibiting the usual spectrum of pharmacological effects of this drug class. It appears to be less potent and less toxic than atropine and displays less CNS toxicity than scopolamine. Anisodamine has been shown to interact with and disrupt liposome structure which may reflect its effects on cellular membranes. Experimental evidence implicates anisodamine as an anti-oxidant that may protect against free radical-induced cellular damage. Its cardiovascular properties include depression of cardiac conduction and the ability to protect against arrhythmia induced by various agents. Anisodamine is a relatively weak alpha(1) adrenergic antagonist which may explain its vasodilating activity. Its anti-thrombotic activity may be a result of inhibition of thromboxane synthesis. The T(1/2) of anisodamine in humans is about 2-3 h. Numerous therapeutic uses of anisodamine have been proposed including treatment of septic shock, various circulatory disorders, organophosphorus (OP) poisoning, migraine, gastric ulcers, gastrointestinal colic, acute glomerular nephritis, eclampsia, respiratory diseases, rheumatoid arthritis, obstructive jaundice, opiate addiction, snake bite and radiation damage protection. The primary therapeutic use of anisodamine has been for the treatment of septic shock. Several mechanisms have been proposed to explain its beneficial effect though most mechanisms are based upon the assumption that anisodamine ultimately acts by an improvement of blood flow in the microcirculation. Preliminary studies suggest another important therapeutic use of anisodamine is for the treatment of OP poisoning. Additional research is needed to delineate further the clinical usefulness of anisodamine relative to other anti-muscarinic drugs such as atropine and scopolamine.
机译:山iso碱是一种天然存在的阿托品衍生物,已被中华人民共和国的科学家分离,合成和表征。像阿托品和东pol碱一样,山iso碱是一种非特异性胆碱能拮抗剂,表现出该药物类别的通常药理作用范围。它似乎比阿托品的效力和毒性更低,并且比东pol碱显示的CNS毒性更低。已显示山iso碱与脂质体结构相互作用并破坏脂质体结构,这可能反映了其对细胞膜的作用。实验证据表明山iso碱是一种抗氧化剂,可以防止自由基引起的细胞损伤。它的心血管特性包括心脏传导抑制和防止各种药物引起的心律不齐的能力。山iso碱是一种相对较弱的α(1)肾上腺素能拮抗剂,可以解释其血管舒张活性。其抗血栓形成活性可能是抑制血栓烷合成的结果。人的山iso碱的T(1/2)约为2-3小时。已提出了山iso碱的多种治疗用途,包括治疗败血性休克,各种循环系统疾病,有机磷(OP)中毒,偏头痛,胃溃疡,胃肠道绞痛,急性肾小球肾炎,子痫,呼吸系统疾病,类风湿性关节炎,阻塞性黄疸,鸦片成瘾,蛇咬和辐射伤害保护。山iso碱的主要治疗用途是治疗败血性休克。尽管大多数机制是基于山iso碱最终通过改善微循环中的血流而起作用的假设,但已经提出了几种机制来解释其有益作用。初步研究表明山iso碱的另一种重要治疗用途是治疗OP中毒。与其他抗毒蕈碱药物(例如阿托品和东pol碱)相比,还需要进一步研究山iso碱的临床实用性。

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