Rilmazafone

Rilmazafone[1] (リスミー, Rhythmy, previously known as 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan.[2] It has sedative and hypnotic effects.[3][4] Rilmazafone induces impairment of motor function and has hypnotic properties.[5]

Rilmazafone
Clinical data
Trade namesRhythmy
Other names5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral (tablets)
ATC code
  • none
Legal status
Legal status
  • ℞-only (JP)
Pharmacokinetic data
Elimination half-life10.5 h
ExcretionUrine
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H20Cl2N6O3
Molar mass475.33 g·mol−1
3D model (JSmol)
  (verify)

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 [1,5-a][1,4]benzodiazepine-2-carboxamide.[6][7]

Rilmazafone active metabolite

See also

References
  1. DE Patent 2725164
  2. Yamamoto K, Hirose K, Matsushita A, Yoshimura K, Sawada T, Eigyo M, Jyoyama H, Fujita A, Matsubara K, Tsukinoki Y (July 1984). "[Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica (in Japanese). 84 (1): 109–54. doi:10.1254/fpj.84.109. PMID 6149174.
  3. Yamamoto K, Matsushita A, Sawada T, Naito Y, Yoshimura K, Takesue H, Utsumi S, Kawasaki K, Hirono S, Koshida H (July 1984). "[Pharmacology of a new sleep inducer, 1H-1,2,4-triazolyl benzophenone derivative, 450191-S (II). Sleep-inducing activity and effect on the motor system]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica (in Japanese). 84 (1): 25–89. doi:10.1254/fpj.84.25. PMID 6149175.
  4. Ibii N, Horiuchi M, Yamamoto K (August 1984). "[Pharmacology of a 1H-1, 2, 4-triazolyl benzophenone derivative (450191-S), a new sleep-inducer (III). Behavioral study on interactions of 450191-S and other drugs in mice]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica (in Japanese). 84 (2): 155–73. doi:10.1254/fpj.84.155. PMID 6149177.
  5. Yasui M, Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, et al. (June 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]". Nihon Shinkei Seishin Yakurigaku Zasshi = Japanese Journal of Psychopharmacology. 25 (3): 143–51. PMID 16045197.
  6. Koike M, Norikura R, Sugeno K (March 1986). "Intestinal activation of a new sleep inducer 450191-S, a 1H-1,2,4-triazolyl benzophenone derivative, in rats". Journal of Pharmacobio-Dynamics. 9 (3): 315–20. doi:10.1248/bpb1978.9.315. PMID 3454653.
  7. Muranushi N, Miyauchi S, Suzuki H, Sugiyama Y, Hanano M, Kinoshita H, Oguma T, Yamada H (May 1993). "Comparative hepatic transport of desglycylated and cyclic metabolites of rilmazafone in rats: analysis by multiple indicator dilution method". Biopharmaceutics & Drug Disposition. 14 (4): 279–90. doi:10.1002/bdd.2510140402. PMID 8499579. S2CID 24923818.
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