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BD 40 A与其他一些β-肾上腺素能受体兴奋剂对豚鼠离体气管和心房作用的比较。

Comparison of the action of BD 40 A and some other beta-adrenoceptor stimulants on the isolated trachea and atria of the guinea pig.

作者信息

Ida H

出版信息

Arzneimittelforschung. 1976;26(5):839-42.

PMID:9101
Abstract

3-Formylamino-4-hydroxy-a-(N-1-methyl-2-p-methoxyphenethyl-aminomethyl)-benzylalcohol hemifumarate (BD 40A) was compared with isoproterenol, orciprenaline, trimetoquinol and salbutamol for its beta-adrenergic activity and selectivity in vitro. On trachea, the maximum relaxing responses to five agonists were similar, but the order of potency was BD 40A greater than trimetoquinol greater than isoproterenol greater than or equal to salbutamol greater than orciprenaline. On atria, the maximum chronotropic and inotropic responses to isoproterenol were greater than those to BD 40A, orciprenaline and trimetoquinol, and salbutamol caused the weakest cardiac stimulating effect. Namely, the latter four drugs appeared to be partial agonists on atria. Salbutamol showed the high selectivity for trachea, whereas orciprenaline and trimetoquinol were equipotent on trachea and atria. Isoproterenol was more potent on atria than on trachea. BD 40A had the highest bronchoselectivity among five agonists and seemed to act on the beta-adrenergic receptor directly.

摘要

将3-甲酰氨基-4-羟基-α-(N-1-甲基-2-对甲氧基苯乙胺甲基)-苄醇半富马酸盐(BD 40A)与异丙肾上腺素、奥西那林、曲美托喹酚和沙丁胺醇在体外进行β-肾上腺素能活性和选择性比较。在气管上,对这五种激动剂的最大舒张反应相似,但效价顺序为BD 40A>曲美托喹酚>异丙肾上腺素≥沙丁胺醇>奥西那林。在心房上,异丙肾上腺素的最大变时性和变力性反应大于BD 40A、奥西那林和曲美托喹酚,沙丁胺醇引起的心脏刺激作用最弱。也就是说,后四种药物在心房上似乎是部分激动剂。沙丁胺醇对气管表现出高选择性,而奥西那林和曲美托喹酚在气管和心房上的效力相当。异丙肾上腺素在心房上比在气管上更有效。BD 40A在五种激动剂中具有最高的支气管选择性,似乎直接作用于β-肾上腺素能受体。

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