Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
357.068032587
InChI
InChI=1S/C18H13ClFN3O2/c19-11-6-7-15-13(10-11)16(12-4-1-2-5-14(12)20)22-17(24)18(25)23(15)9-3-8-21/h1-2,4-7,10,17,24H,3,9H2
InChI Key
InChIKey=XAXMYHMKTCNRRZ-UHFFFAOYSA-N
IUPAC Name
3-[7-chloro-5-(2-fluorophenyl)-3-hydroxy-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-1-yl]propanenitrile
Traditional IUPAC Name
cinolazepam
SMILES
OC1N=C(C2=CC=CC=C2F)C2=C(C=CC(Cl)=C2)N(CCC#N)C1=O
pKa (strongest acidic)
10.68
pKa (Strongest Basic)
-2.5
Refractivity
90.99 m3·mol-1
Dược Lực Học :
Cinolazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Cinolazepam is not approved for sale in the United States or Canada.
Cơ Chế Tác Dụng :
Cinolazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Cinolazepam is not approved for sale in the United States or Canada.
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.
Dược Động Học :
▧ Absorption :
Bioavailability following oral administration is 90-100%.
▧ Metabolism :
Hepatic.
▧ Half Life :
9 hours
Độc Tính :
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.
Chỉ Định :
For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms.