词条 | Rilmazafone |
释义 |
| Watchedfields = changed | verifiedrevid = 451729144 | IUPAC_name = 1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-5-[(glycylamino)methyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide | image = Rilmazafone structure.svg | width = 220 | tradename = Rhythmy | Drugs.com = {{drugs.com|international|rilmazafone}} | legal_status = ℞-only (JP) | routes_of_administration = Oral (tablets) | bioavailability = | metabolism = | elimination_half-life = 10.5 h | excretion = Urine | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 99593-25-6 | ATC_prefix = none | PubChem = 5069 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4891 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = CU3H37T766 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08481 | C=21 | H=20 | Cl=2 | N=6 | O=3 | molecular_weight = 475.328 g/mol | smiles = ClC1=C(C(C2=CC(Cl)=CC=C2N3C(CNC(CN)=O)=NC(C(N(C)C)=O)=N3)=O)C=CC=C1 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C21H20Cl2N6O3/c1-28(2)21(32)20-26-17(11-25-18(30)10-24)29(27-20)16-8-7-12(22)9-14(16)19(31)13-5-3-4-6-15(13)23/h3-9H,10-11,24H2,1-2H3,(H,25,30) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = KYHFRCPLIGODFH-UHFFFAOYSA-N | synonyms = 5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide }}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
References1. ^DE Patent 2725164 2. ^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). 3. ^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). 4. ^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). 5. ^{{cite journal |author=Yasui M |author2=Kato A |author3=Kanemasa T |author4=Murata S |author5=Nishitomi K |author6=Koike K |author7=Tai N |author8=Shinohara S |author9=Tokomura M |author10=Horiuchi M |author11=Abe K. |title=[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes] |volume=25 |issue=3 |pages=143–51 |date=June 2005 |pmid=16045197 |journal=Nihon Shinkei Seishin Yakurigaku Zasshi }} 6. ^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. 7. ^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
8 : Acetamides|Benzodiazepines|Benzophenones|Chloroarenes|GABAA receptor positive allosteric modulators|Japanese inventions|Prodrugs|Triazoles |
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