Rilmazafone (リスミー, Rhythmy, previously known as 450191-S) is a water-soluble

prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ...

developed in Japan. Inside the human body, rilmazafone is converted into several

benzodiazepine Benzodiazepines (BZD, BDZ, BZs), colloquially known as "benzos", are a class of central nervous system (CNS) depressant, depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed t ...

metabolites that have

sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its decelera ...

and

hypnotic A hypnotic (from Ancient Greek, Greek ''Hypnos'', sleep), also known as a somnifacient or soporific, and commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to sleep induction, induce sleep and to trea ...

effects. 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 Sing ...

. 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 N-terminus (beginning), of proteins or peptides. They are found in many organisms; in the cell, they are found in many organelles, in the cytosol (internal cellular f ...

enzymes in the small intestine to form the principal active benzodiazepine

rilmazolam Rilmazolam, is a benzodiazepine derivative which acts as a sedative and hypnotic drug, and the active metabolite of the drug Rilmazafone. It has never been developed for medical uses, yet the aforementioned prodrug is an approved medication in Ja ...

(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 Chlorobenzene derivatives GABAA receptor positive allosteric modulators Japanese inventions Benzodiazepine prodrugs Triazoles

See also

References

External links