[Clinico-pharmacologic studies with a M1 receptor antagonist (substance AWD 26-06) in a phase I clinical trial].

B Terhaag, T Gramatté, K Feller
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Abstract

The tolerability of the compound AWD 26-06 (which is to classify as a M1-antagonist in consequence of the pharmacological investigations) was investigated in 11 healthy male persons with increasing dosage from 5 to 150 mg. Dryness of the mouth and scratch in the throat were observed by a dosage of 50 mg onwards, a diminuation of the flow of saliva and the accommodation were observed by a dosage of 100 and 150 mg, respectively. The frequency of the heart, but not the blood pressure, is increased by 150 mg of AWD 26-06. The influence on the secretion of the gastric juice was investigated in normal conditions and after stimulation by Pentagastrin with a dosage of AWD 26-06 of 25 mg in comparison with a placebo on 7 healthy male persons. The volume of gastric juice was diminished by 35% in all fractions, but the secretion of HCl, measured as basal acid output and peak acid output, was diminished in 5 of the 7 persons by 20%. A further investigation in order to check the therapeutic effect in patients with ulcus ventriculi and ulcus duodeni, respectively, is necessary and useful.

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[M1受体拮抗剂(物质AWD 26-06)在I期临床试验中的临床药理学研究]。
化合物AWD 26-06(在药理学研究中被归类为m1拮抗剂)的耐受性在11名健康男性中进行了研究,剂量从5毫克增加到150毫克。当剂量为50毫克时,观察到口腔干燥和喉咙划伤,当剂量分别为100毫克和150毫克时,观察到唾液流动减少和调节。150mg的AWD 26-06会增加心脏的频率,而不是血压。研究了7名健康男性在正常情况下以及在AWD 26-06剂量为25 mg的Pentagastrin刺激后对胃液分泌的影响,并与安慰剂进行了比较。所有部分的胃液量都减少了35%,但7人中有5人的HCl分泌量(以基础酸输出量和峰值酸输出量衡量)减少了20%。进一步研究脑室沟和十二指肠沟的治疗效果是必要和有益的。
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