 | |
 Above: Rilmazafone molecular structureBelow: 3D molecular representation | |
| Clinical data | |
|---|---|
| Trade names | Rhythmy |
| Other names | 5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral (tablets) |
| ATC code |
|
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Eliminationhalf-life | 10.5 h |
| Excretion | Urine |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| ChemSpider |
|
| UNII | |
| KEGG |
|
| CompTox Dashboard(EPA) | |
| Chemical and physical data | |
| Formula | C21H20Cl2N6O3 |
| Molar mass | 475.33 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
Rilmazafone[1] (リスミー,Rhythmy, previously known as450191-S) is a water-solubleprodrug developed byShionogi.[2] Inside the human body, rilmazafone is converted into severalbenzodiazepine metabolites that havesedative andhypnotic effects.[3][4][5]
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 acontrolled 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 byaminopeptidase enzymes in the small intestine to form the principal active benzodiazepinerilmazolam (8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide).[6][7] 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 has been identified as a NPS (new psychoactive substance) in the U.S. and Europe.[8]
