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一种具有抗支气管痉挛和黏液调节特性的新型甲基黄嘌呤衍生物[7-(1,3-二硫杂环戊烷-2-基甲基)-1,3-二甲基黄嘌呤]的药理和毒理活性

Pharmacological and toxicological activities of a new methylxanthine derivative [7-(1,3-dithiolan-2-ylmethyl)1,3-dimethylxanthine] with antibronchospastic and mucoregulatory properties.

作者信息

Franzone J S, Reboani M C, Biglione V, Cirillo R

机构信息

Research Laboratories of Istituto Biologico Chemiotherapico ABC S.p.A., Turin, Italy.

出版信息

Drugs Exp Clin Res. 1990;16(6):263-76.

PMID:1964891
Abstract

7-(1,3-Dithiolan-2-ylmethyl)-1,3-dimethylxanthine (ABC 99) has been studied in the animal to evaluate its pharmacological activity. This compound was found to have antibronchospastic activity in vitro and in vivo markedly greater than aminophylline. The new compound also had moderate antitussic properties and was an active mucoregulator. ABC 99 acts as an intestinal muscle relaxant, but it has no cardiovascular, urinary, or CNS side effects. The mechanism of ABC 99 could be explained by its inhibition of guinea-pig lung phosphodiesterases and affinity for adenosine receptors, particularly A2 receptors. ABC 99 had a low acute toxicity in animals, indicating it may be useful for treating asthma and chronic bronchitis.

摘要

7-(1,3-二硫杂环戊烷-2-基甲基)-1,3-二甲基黄嘌呤(ABC 99)已在动物身上进行研究以评估其药理活性。发现该化合物在体外和体内具有的抗支气管痉挛活性明显大于氨茶碱。这种新化合物还具有适度的镇咳特性,并且是一种活性黏液调节剂。ABC 99可作为肠道肌肉松弛剂,但没有心血管、泌尿或中枢神经系统副作用。ABC 99的作用机制可以通过其对豚鼠肺磷酸二酯酶的抑制作用以及对腺苷受体(特别是A2受体)的亲和力来解释。ABC 99在动物中具有低急性毒性,表明它可能对治疗哮喘和慢性支气管炎有用。

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