cas: 85815-37-8 Rilmazafone Hydrochloride

cas: 85815-37-8 Rilmazafone Hydrochloride

CBNumber: CB02469946

Chemical Name: Rilmazafone Hydrochloride

Molecular Formula: C21H21Cl3N6O3

Formula Weight: 511.79

CAS No.: 85815-37-8

Rilmazafone Rhythmy, previously known as 450191-S is a water-soluble prodrug developed in Japan. Once metabolized, rilmazafone is converted into several benzodiazepine metabolites that have sedative and hypnotic effects These metabolites induce impairment of motor function and have hypnotic properties.

Rilmazafone is not a benzodiazepine, since there is no benzene ring fused with a diazepine ring in the compound; in fact, the parent drug has no diazepine ring. It is therefore not classified as a benzodiazepene in several countries, including the United States, where it is not designated a controlled substance. Rilmazafone has no effects on benzodiazepine receptors itself, nor does it produce any psychoactive effects prior to metabolism. However, once inside the body it is metabolized by aminopeptidase enzymes in the small intestine to form the principal active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo [1,5-a]benzodiazepine-2-carboxamide.As can be seen in the molecular diagram below, the principal metabolite contains a benzodiazepine ring structure (i.e., a benzene ring fused with a diazepine ring), unlike the parent compound (rilmazafone), which has no diazepine ring

Rilmazafone induces impairment of motor function and has hypnotic properties. Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo benzodiazepine-2-carboxamide. Preclinical studies have shown its excellent effects inducing and maintaining sleep with little effect on the skeletal muscle. Earlier the clinical dose for this drug as a premedicant was found to be 2-4mg. Zolpidem Triazolam Rilmazafone Elderly Residual effects Randomized study,

Rilmazafone is considered to be a benzodiazepine pro-drug, and in Japan, is used for the short-term treatment of insomnia. Benzodiazepines are scheduled as Prescription Medicines in Schedule 1 of the Medicines Regulations 1984. However, rilmazafone is itself not a benzodiazepine.