Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H20Cl2N6O3 |
Molecular Weight | 475.328 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C(=O)C1=NN(C(CNC(=O)CN)=N1)C2=CC=C(Cl)C=C2C(=O)C3=CC=CC=C3Cl
InChI
InChIKey=KYHFRCPLIGODFH-UHFFFAOYSA-N
InChI=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)
Molecular Formula | C21H20Cl2N6O3 |
Molecular Weight | 475.328 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/3428781Curator's Comment: description was created based on several sources, including
https://www.jstage.jst.go.jp/article/jjsca1981/8/4/8_4_384/_article
Sources: http://www.ncbi.nlm.nih.gov/pubmed/3428781
Curator's Comment: description was created based on several sources, including
https://www.jstage.jst.go.jp/article/jjsca1981/8/4/8_4_384/_article
Rilmazafone (previously known as 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan. It has sedative and hypnotic effects. Rilmazafone induces impairment of motor function and has hypnotic properties. 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 benzodiazepine-2-carboxamide. Preclinical studies have shown its excellent effects inducing and maintaining sleep with little effect on the skeletal muscle. Earlier the clinical dose for this drug as a premedicant was found to be 2-4mg.
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/6145419
Curator's Comment: Known to be CNS penetrant in rat. Human data not available.
Approval Year
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sources: http://www.ncbi.nlm.nih.gov/pubmed/6149175 |
Curative | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Safety evaluation and drug development based on biological fate of drugs -efforts made to overcome drug interaction in drug development-. | 2002 |
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[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]. | 2005 Jun |
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Potentiation of ethanol in spatial memory deficits induced by some benzodiazepines. | 2006 Aug |
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Effects of melatonin and rilmazafone on nocturia in the elderly. | 2007 Sep-Oct |
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Evaluation of anxiolytic-like effects of some short-acting benzodiazepine hypnotics in mice. | 2008 Jul |
|
Hypnotic and sleep quality-enhancing properties of kavain in sleep-disturbed rats. | 2009 Nov |
Patents
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:03:49 UTC 2023
by
admin
on
Fri Dec 15 16:03:49 UTC 2023
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Record UNII |
CU3H37T766
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C29756
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99593-25-6
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C041075
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5069
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RILMAZAFONE
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C76944
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CHEMBL2107197
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2380
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DTXSID10244150
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100000080583
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SUB10315MIG
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CU3H37T766
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m9616
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5933
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ACTIVE MOIETY |