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Cinolazepam

Cinolazepam structure

CAS No:
75696-02-5
Formula:
C18H13ClFN3O2
Chemical Name:
Cinolazepam
Synonyms:
1H-1,4-Benzodiazepine-1-propanenitrile,7-chloro-5-(2-fluorophenyl)-2,3-dihydro-3-hydroxy-2-oxo-;7-Chloro-5-(2-fluorophenyl)-2,3-dihydro-3-hydroxy-2-oxo-1H-1,4-benzodiazepine-1-propanenitrile;Cinolazepam;OX 373;Gerodorm
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

ChEBI: A 1,4-benzodiazepinone compound having a 2-cyanoethyl substituent at the 1-position, a hydroxy substituent at the 3-position, a 2-fluorophenyl group at the 5-position and a chloro substituent at the 7-position, it has general properties similar to those of diazepam and has been used for the short-term management of sleep disorders.

Solid

Cinolazepam is a 1,4-benzodiazepinone compound having a 2-cyanoethyl substituent at the 1-position, a hydroxy substituent at the 3-position, a 2-fluorophenyl group at the 5-position and a chloro substituent at the 7-position, it has general properties similar to those of diazepam and has been used for the short-term management of sleep disorders. It has a role as a sedative and an anticonvulsant. It is a 1,4-benzodiazepinone and an organochlorine compound.|Cinolazepam is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant activity. It is not approved in Canada or America.

Cinolazepam Basic Attributes

Molecular Weight：

357.771

Exact Mass：

357.77

ATC Code：

N - Nervous system

Characteristics

PSA：

76.7

XLogP3：

2.39578

Density：

1.39g/cm3

Melting Point：

190-193 °C

Boiling Point：

643.5ºC at 760 mmHg

Flash Point：

343ºC

Refractive Index：

1.646

Water Solubility：

1.20e-02 g/L

Toxicity

Toxicity Summary：

The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma Grade I or Grade II following very large ingestions.

Drug Information

Drug Indication：

For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms.

Pharmacology：

Cinolazepam is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant activity. It is not approved in Canada or America.

Absorption：

Bioavailability following oral administration is 90-100%.

Metabolism/Metabolites：

Hepatic.

Biological Half-Life：

9 hours

Mechanism of Action：

Cinolazepam binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

MeSH Entry Terms：

7-chloro-5-(2-fluorophenyl)-2,3-dihydro-3-hydroxy-2-oxo-1H-1,4-benzodiazepine-1-propionitrile

Computed Properties

Molecular Weight:357.8
XLogP3:2
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:3
Exact Mass:357.0680325
Monoisotopic Mass:357.0680325
Topological Polar Surface Area:76.7
Heavy Atom Count:25
Complexity:590
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes