Ro 41-3290
目录号 : GC37547
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。
Cas No.:143943-72-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 143943-72-0 | SDF | |
| Canonical SMILES | O[C@@H]1CN(C(C2=C3N(C(C(C4=CC=CC=C4)=C2)=O)CCC5=CC=C(Cl)C=C53)=O)CC1 | ||
| 分子式 | C24H21ClN2O3 | 分子量 | 420.89 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3759 mL | 11.8796 mL | 23.7592 mL |
| 5 mM | 0.4752 mL | 2.3759 mL | 4.7518 mL |
| 10 mM | 0.2376 mL | 1.188 mL | 2.3759 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pharmacokinetics and pharmacodynamics of Ro 41-3696, a novel nonbenzodiazepine hypnotic
J Clin Pharmacol 1995 Aug;35(8):821-9.PMID:8522640DOI:10.1002/j.1552-4604.1995.tb04126.x.
This report describes the first evaluation in humans of Ro 41-3696. Based on its preclinical profile, Ro 41-3696, a nonbenzodiazepine partial agonist at the benzodiazepine receptor, offers promising perspectives as an innovative hypnotic drug in that it does not exhibit most of the disadvantages associated with full agonists. Single oral doses of 0.1, 0.3, 1.0, 3.0, 10, and 30 mg were administered sequentially to six groups of six healthy male volunteers in a placebo-controlled, double-blind design. Tolerability was assessed and pharmacokinetic and pharmacodynamic measurements were conducted during a period of 28 hours after drug intake. Ro 41-3696 was well tolerated at all doses, causing no clinically relevant changes in vital signs or laboratory parameters. At doses of 10 and 30 mg there were signs of unsteady gait, indicating a central nervous system depressant effect. Pharmacokinetic analyses revealed that Ro 41-3696 was absorbed and eliminated rapidly (tmax = approximately 1 hour; t1/2 = approximately 4 hours). At all times plasma levels of Ro 41-3290, the desethylated derivative of Ro 41-3696, were higher than those of the parent drug (tmax and t1/2 values = approximately 2 and 8 hours, respectively). Area under the curve (AUC) data indicated dose-proportional pharmacokinetics for both Ro 41-3696 and Ro 41-3290. Performance in both a tracking and a memory search test was significantly affected by doses of 10 and 30 mg, and long-term memory, as assessed by a word learning and recall test, was slightly impaired at these doses. The results of this study support the initiation of therapeutic efficacy studies with Ro 41-3696 in doses up to approximately 5 mg and further exploration of the characteristics of Ro 41-3290.
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.PMID:11307042DOI:10.1097/00002826-200103000-00003.
The objectives of this double-blind, placebo-controlled study were to assess the multiple-dose tolerability, pharmacodynamics, and pharmacokinetics of the hypnotic agent Ro 41-3696 in elderly men and women (55-75 y of age). On day 1 and days 3-8, doses of 1, 3, 5, and 10 mg were administered sequentially to 4 groups of 10 subjects, 2 of whom received placebo. Psychomotor performance tests (tracking and attention) were conducted just before and at 1.5, 4, and 8 hours after drug intake on days 1, 4, 6, and 8. Memory was assessed at 24 hours after drug intake on days 1 and 8 by recall of a list of 10 words, which had been learned at 2 hours after intake. Ro 41-3696 was well tolerated at all dose levels. One subject dropped out of the study because of a hypersensitive skin reaction during treatment with 10 mg. Performance in both a tracking test and a memory search test was significantly affected by a dose of 10 mg and moderately affected by doses of 3 and 5 mg. The results of the 1-mg dose were indistinguishable from those of placebo. Long-term memory, as assessed by a word learning and recall test, showed the same pattern. Partial tolerance to the impairing effects in the psychometric tests developed over the course of treatment. Pharmacokinetics of both Ro 41-3696 and its O-desethyl metabolite Ro 41-3290 were dose proportional and time independent. Ro 41-3696 was absorbed and eliminated rapidly (time of maximum plasma concentration, approximately 1 hour; elimination half-life, approximately 2 hours). Plasma levels of Ro 41-3290 were higher than those of the parent drug, and it was more slowly eliminated (values for time of maximum plasma concentration and elimination half-life, approximately 2 and approximately 7 hours, respectively).
Comparative tolerability, pharmacodynamics, and pharmacokinetics of a metabolite of a quinolizinone hypnotic and zolpidem in healthy subjects
Drug Metab Dispos 2000 Dec;28(12):1411-6.PMID:11095577doi
The objectives of this double-blind, placebo-controlled study were to assess the single dose tolerability, pharmacodynamics, and pharmacokinetics of Ro 41-3290 (5, 10, and 30 mg) and zolpidem (10 mg) in three sequential groups of 10 healthy male subjects. Pharmacodynamic (tracking, attention, and memory test) and pharmacokinetic measurements were conducted over a period of 24 and 50 h, respectively, after drug intake. Ro 41-3290 was well tolerated at all doses as was zolpidem. Performance in both a tracking and a memory search test was affected at 1.5 h after administration of zolpidem, whereas effects had vanished by 8 h. Ro 41-3290 induced moderate, dose-independent effects, which were most pronounced at 4 h after intake. Long-term memory, as assessed by a word learning and recall test, was not clearly affected by any drug. The pharmacokinetics of Ro 41-3290 were dose proportional with an elimination half-life of approximately 8 h. The relatively slow absorption of Ro 41-3290 (t(max) approximately 2.5 h) and the concentration-effect time delay do not make it a good candidate to replace its parent compound Ro 41-3696 as an investigational hypnotic.