Krause W, Schütt B, Duka T
Research Laboratories of Schering Aktiengesellschaft, Berlin, Germany.
Arzneimittelforschung. 1990 May;40(5):529-32.
Plasma levels of the beta-carboline, abecarnil (isopropyl 6-(benzyloxy)-4-(methoxymethyl)-9H-pyrido [3,4-b]indole-3- carboxylate, ZK112119) which is presently under development as an anxiolytic, were measured by HPLC with fluorescence detection in six healthy male volunteers given 30 micrograms/kg i.v. and 5 and 10 mg p.o. Following i.v. injection, plasma levels declined biphasically with half-lives of 6 min and 3.4 h. The total clearance was 13 ml/min/kg. After oral administration, maximum concentrations were reached after 2 h. The bioavailability was approximately 60%. The terminal half-life after p.o. administration was 7 h. No clinically relevant changes in ECG, vital signs or standard laboratory measurements occurred. Eight different adverse reactions were noted by the subjects. The most frequently reported side-effects were tiredness, dizziness, unsteady gait and lack of concentration.
对作为一种抗焦虑药正在研发的β-咔啉阿贝卡尼（异丙基6-（苄氧基）-4-（甲氧基甲基）-9H-吡啶并[3,4-b]吲哚-3-羧酸酯，ZK112119），在6名健康男性志愿者静脉注射30微克/千克以及口服5毫克和10毫克后，采用高效液相色谱荧光检测法测定了其血浆水平。静脉注射后，血浆水平呈双相下降，半衰期分别为6分钟和3.4小时。总清除率为13毫升/分钟/千克。口服给药后，2小时后达到最大浓度。生物利用度约为60%。口服给药后的终末半衰期为7小时。心电图、生命体征或标准实验室测量值未出现临床相关变化。受试者记录到8种不同的不良反应。最常报告的副作用是疲倦、头晕、步态不稳和注意力不集中。
