Ro 41-3290

Names

[ CAS No. ]:
143943-72-0

[ Name ]:
Ro 41-3290

[Synonym ]:
4H-Benzo[a]quinolizin-4-one, 10-chloro-6,7-dihydro-1-[[(3S)-3-hydroxy-1-pyrrolidinyl]carbonyl]-3-phenyl-
EIR1Q66583
10-Chloro-1-{[(3S)-3-hydroxy-1-pyrrolidinyl]carbonyl}-3-phenyl-6,7-dihydro-4H-pyrido[2,1-a]isoquinolin-4-one
RO-41-3290

Biological Activity

[Description]:

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.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Signaling Pathways >> Neuronal Signaling >> GABA Receptor
Research Areas >> Neurological Disease

[Target]

Benzodiazepine receptor[1]


[In Vivo]

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].

[References]

[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.


[Related Small Molecules]

(+)-Bicuculline | Picrotoxin | Aminooxyacetic acid hemihydrochloride | Riluzole | Baclofen | basmisanil | (R)-Baclofen | Etifoxine | Etomidate | Ginkgolide A | NS-11394 | 5alpha-Pregnan-3alpha-ol-20-one | CGP 52432 | L-655,708 | SAGE-217

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
723.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H21ClN2O3

[ Molecular Weight ]:
420.888

[ Flash Point ]:
391.2±32.9 °C

[ Exact Mass ]:
420.124084

[ LogP ]:
3.00

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.717

Related Compounds