Ro 41-3290 是一种催眠剂,是 Ro 41-3696 的去甲基化衍生物。Ro 41-3696 是一种苯二氮卓类 (benzodiazepine) 受体的部分激动剂。
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Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor. Ro 41-3290 is an investigational hypnotic. Benzodiazepine receptor[1]
At all times plasma levels of Ro 41-3290, the desethylated derivative of Ro 41-3696, are higher than those of the parent drug (tmax and t1/2 values=~2 and 8 hours, respectively)[1]. Pharmacokinetics of both Ro 41-3696 and its O-desethyl metabolite Ro 41-3290 are dose proportional and time independent. Ro 41-3696 is absorbed and eliminates rapidly (time of maximum plasma concentration, approximately 1 hour; elimination half-life, approximately 2 hours). Plasma levels of Ro 41-3290 are higher than those of the parent drug, and it is more slowly eliminated (values for time of maximum plasma concentration and elimination half-life, approximately 2 and approximately 7 hours, respectively)[2].
[1]. Dingemanse J, et al. Pharmacokinetics and pharmacodynamics of Ro 41-3696, a novel nonbenzodiazepine hypnotic. J Clin Pharmacol. 1995 Aug;35(8):821-9. [2]. Dingemanse J, et al. Multiple-dose tolerability, pharmacodynamics, and pharmacokinetics of the quinolizinone hypnotic Ro 41-3696 in elderly subjects. Clin Neuropharmacol. 2001 Mar-Apr;24(2):82-90.
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