Page last updated: 2024-12-05

rilmazafone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Rilmazafone is a novel, non-benzodiazepine anxiolytic drug that acts as a selective agonist of the α5 subtype of the GABA-A receptor. It is being investigated as a potential treatment for anxiety disorders and other conditions, such as insomnia, epilepsy, and cognitive impairment. Studies suggest that rilmazafone may have a distinct pharmacological profile compared to benzodiazepines, potentially leading to improved therapeutic benefits with fewer side effects. Its mechanism of action involves enhancing GABAergic neurotransmission, which is thought to contribute to its anxiolytic and sedative effects. Rilmazafone's synthesis involves a multi-step chemical process, and its research focuses on exploring its efficacy, safety, and potential advantages over existing treatments.'

rilmazafone: structure given in first source; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5069
CHEMBL ID2107197
CHEBI ID135767
SCHEMBL ID123946
MeSH IDM0121959

Synonyms (28)

Synonym
1h-1,2,4-triazole-3-carboxamide, 5-(((aminoacetyl)amino)methyl)-1-(4-chloro-2-(2-chlorobenzoyl)phenyl)-n,n-dimethyl-
rilmazafona [spanish]
1h-1,2,4-triazole-3-carboxamide, 5-(((aminoacetyl)amino)methyl)-1-(4-chloro-2-(2-chlorobenzoyl)phenyl)-n,n-dimethyl-, monohydrochloride
rilmazafone [inn]
rilmazafone
5-((2-aminoacetamido)methyl)-1-(4-chloro-2-(o-chlorobenzoyl)phenyl)-n,n-dimethyl-1h-1,2,4-triazole-3-carboxamide
rilmazafonum [latin]
CHEBI:135767
rilmazafone (inn)
99593-25-6
D08481
5-[[(2-aminoacetyl)amino]methyl]-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-n,n-dimethyl-1,2,4-triazole-3-carboxamide
unii-cu3h37t766
rilmazafona
cu3h37t766 ,
rilmazafonum
CHEMBL2107197
AKOS016014131
SCHEMBL123946
rilmazafone [who-dd]
rilmazafone [mi]
DTXSID10244150
99593-25-6 free base)
HY-106547
Q7334297
CS-0026029
EX-A5707
1h-1,2,4-triazole-3-carboxamide,5-[[(aminoacetyl)amino]methyl]-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-n,n-dimethyl-

Research Excerpts

Overview

Rilmazafone (RZ) is an orally active sleep inducer. It can be activated to its cyclic form (M1) via the labile desglycylated metabolite (DG)

ExcerptReferenceRelevance
"Rilmazafone is a pro-drug that can be prescribed in Japan to treat insomnia. "( Rilmazafone: A designer benzodiazepine pro-drug involved in fatal intoxications.
Green, H; Johansson, A; Kronstrand, R; Roman, M; Truver, MT; Wu, X, 2023
)
3.8
"Rilmazafone (RZ) is an orally active sleep inducer which can be activated to its cyclic form (M1) via the labile desglycylated metabolite (DG). "( Comparative hepatic transport of desglycylated and cyclic metabolites of rilmazafone in rats: analysis by multiple indicator dilution method.
Hanano, M; Kinoshita, H; Miyauchi, S; Muranushi, N; Oguma, T; Sugiyama, Y; Suzuki, H; Yamada, H, 1993
)
1.96

Bioavailability

ExcerptReferenceRelevance
" Thus, the presence of 191DG improved the bioavailability of active metabolites after 450191-S administration."( Biopharmaceutical characterization of 450191-S, a ring-opened derivative of 1,4-benzodiazepine. II. Evidence for reduced first-pass extraction by rat liver.
Futaguchi, S; Koike, M; Sugeno, K; Takahashi, S,
)
0.13

Dosage Studied

ExcerptRelevanceReference
" The M-4 level was constantly low during 24 hr after dosing and then decreased gradually."( [Pharmacology of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivative, 450191-S (VI). Determination of metabolites in monkey plasma by combined high-performance liquid chromatography and enzyme immunoassay].
Sugeno, K; Yamaguchi, T; Yamashita, M, 1986
)
0.27
" Administration of nitrazepam with other drugs, except aminopyrine, or of estazolam together with haloperidol exhibited an anticonvulsive pattern different from the case of dosing with either drug alone."( [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].
Horiuchi, M; Ibii, N; Yamamoto, K, 1984
)
0.27
" In this study, the next-day residual effects of zolpidem, triazolam, and rilmazafone, following bedtime dosing in elderly subjects, were evaluated."( Residual effects of zolpidem, triazolam, rilmazafone and placebo in healthy elderly subjects: a randomized double-blind study.
Ito, W; Kanbayashi, T; Nishino, S; Satake, M; Shimizu, K; Shimizu, T; Shioya, T; Uemura, SI; Wakasa, M, 2015
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzophenonesAny aromatic ketone in which the carbonyl group is bonded to 2 phenyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-199027 (81.82)18.7374
1990's1 (3.03)18.2507
2000's2 (6.06)29.6817
2010's2 (6.06)24.3611
2020's1 (3.03)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 52.72

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index52.72 (24.57)
Research Supply Index3.66 (2.92)
Research Growth Index4.67 (4.65)
Search Engine Demand Index83.44 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (52.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (5.56%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (2.78%)4.05%
Observational0 (0.00%)0.25%
Other33 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]