Rilmazafone (リスミー, 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 benzodiazepine in several countries, including the United States, where it is not designated a

controlled substance A controlled substance is generally a drug or chemical whose manufacture, possession and use is regulated by a government, such as illicitly used drugs or prescription medications that are designated by law. Some treaties, notably the Single ...

. 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 Aminopeptidases are enzymes that catalyze the cleavage of amino acids from the amino terminus ( N-terminus) of proteins or peptides (exopeptidases). They are widely distributed throughout the animal and plant kingdoms and are found in many subcel ...

enzymes in the small intestine to form the principal active benzodiazepine 8-chloro-6-(2-chlorophenyl)-''N'',''N''-dimethyl-4''H''-1,2,4-triazolo ,5-a1,4]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.

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Drug Information Sheet
{{GABAAR PAMs Acetamides 2-Aminobenzophenones Chlorobenzenes GABAA receptor positive allosteric modulators Japanese inventions Benzodiazepine prodrugs Triazoles

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