Rilmazafone
 | |
| Systematic (IUPAC) name | |
|---|---|
|
1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-5-[(glycylamino)methyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide | |
| Clinical data | |
| Trade names | Rhythmy |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral (tablets) |
| Legal status |
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| Pharmacokinetic data | |
| Biological half-life | 10.5 h |
| Excretion | Urine |
| Identifiers | |
| CAS Number |
99593-25-6  |
| ATC code | none |
| PubChem | CID 5069 |
| ChemSpider |
4891 |
| UNII |
CU3H37T766 |
| KEGG |
D08481 |
| Synonyms | 5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide |
| Chemical data | |
| Formula | C21H20Cl2N6O3 |
| Molar mass | 475.328 g/mol |
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| (verify) | |
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 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
- ↑ DE Patent 2725164
- ↑ Yamamoto K, Hirose K, Matsushita A, Yoshimura K, Sawada T, Eigyo M, Jyoyama H, Fujita A, Matsubara K, Tsukinoki Y, et al. Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis. Nippon Yakurigaku Zasshi. 1984 Jul;84(1):109-54. (Japanese).
- ↑ Yamamoto K, Matsushita A, Sawada T, Naito Y, Yoshimura K, Takesue H, Utsumi S, Kawasaki K, Hirono S, Koshida H, et al. 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. Nippon Yakurigaku Zasshi. 1984 Jul;84(1):25-89. (Japanese).
- ↑ Ibii N, Horiuchi M, Yamamoto K. 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. Nippon Yakurigaku Zasshi. 1984 Aug;84(2):155-73. (Japanese).
- ↑ Yasui M; Kato A; Kanemasa T; Murata S; Nishitomi K; Koike K; Tai N; Shinohara S; Tokomura M; Horiuchi M; Abe K. (June 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]". Nihon Shinkei Seishin Yakurigaku Zasshi 25 (3): 143–51. PMID 16045197.
- ↑ Koike M, Norikura R, Sugeno K. Intestinal activation of a new sleep inducer 450191-S, a 1H-1,2,4-triazolyl benzophenone derivative, in rats. Journal of Pharmacobiodynamics. 1986 Mar;9(3):315-20.
- ↑ Muranushi N, Miyauchi S, Suzuki H, Sugiyama Y, Hanano M, Kinoshita H, Oguma T, Yamada H. Comparative hepatic transport of desglycylated and cyclic metabolites of rilmazafone in rats: analysis by multiple indicator dilution method. Biopharmaceutics and Drug Disposition. 1993 May;14(4):279-90.
External links
- (Japanese) "リスミー'リルマザホン塩酸塩水和物錠 Rhythmy (rilmazafone hydrochloride hydrate, tablets) Prescribing Information." (PDF). Shionogi & Co., Ltd.
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