Rilmazafone
From Infogalactic: the planetary knowledge core
Systematic (IUPAC) name | |
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1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-5-[(glycylamino)methyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide
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Clinical data | |
Trade names | Rhythmy |
AHFS/Drugs.com | International Drug Names |
Legal status |
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Routes of administration |
Oral (tablets) |
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 |
Molecular mass | 475.328 g/mol |
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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]
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).
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ 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) Lua error in package.lua at line 80: module 'strict' not found.
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Categories:
- Chemical articles having calculated molecular weight overwritten
- Infobox drug articles without a structure image
- Articles without EBI source
- Chemical pages without DrugBank identifier
- Drugs not assigned an ATC code
- Articles with Japanese-language external links
- Acetamides
- Benzodiazepines
- Benzophenones
- Chloroarenes
- GABAA receptor positive allosteric modulators
- Japanese inventions
- Prodrugs
- Triazoles
- Sedative stubs