Tìm theo
Camazepam
Các tên gọi khác (3) :
  • Camazepam
  • CMZ
  • CZ
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 36104-80-0
ATC: N05BA15
CTHH: C19H18ClN3O3
PTK: 371.818
Camazepam is a benzodiazepine which is a dimethyl carbamate ester of tamzepam, a metabolite of diazepam. Similarly to other drugs in its class, it has antxiolytic, anticonvulsant, hypnotic, and skeletal muscle relaxant properties. However, unlike other benzodiapeines camazepam is predominantly anxiolytic and is relatively weak as an anticonvulsant, hypnotic and skeletal muscle relaxant. [Wikipedia] Camazepam also has less side effects, such as impaired cognition and reaction times, compared to other benzodiazepines. However, impairment of cognition and disrupted sleep patterns will occur at doses higher than 40mg of carazepam. [Wikipedia] Camazepam is also believed to increase attention, and is associated with skin disorders. In the United States camazepam is regulated as a Schedule IV controlled substance.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
371.818
Monoisotopic mass
371.103669164
InChI
InChI=1S/C19H18ClN3O3/c1-22(2)19(25)26-17-18(24)23(3)15-10-9-13(20)11-14(15)16(21-17)12-7-5-4-6-8-12/h4-11,17H,1-3H3
InChI Key
InChIKey=PXBVEXGRHZFEOF-UHFFFAOYSA-N
IUPAC Name
7-chloro-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl N,N-dimethylcarbamate
Traditional IUPAC Name
camazepam
SMILES
CN(C)C(=O)OC1N=C(C2=CC=CC=C2)C2=C(C=CC(Cl)=C2)N(C)C1=O
Độ tan chảy
173-174
Độ hòa tan
1.82e-02 g/l
logP
3.34
logS
-4.3
pKa (Strongest Basic)
-1.7
PSA
62.21 Å2
Refractivity
98.63 m3·mol-1
Polarizability
38.05 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Cơ Chế Tác Dụng : Camazepam is a benzodiazepine which is a dimethyl carbamate ester of tamzepam, a metabolite of diazepam. Similarly to other drugs in its class, it has antxiolytic, anticonvulsant, hypnotic, and skeletal muscle relaxant properties. However, unlike other benzodiapeines camazepam is predominantly anxiolytic and is relatively weak as an anticonvulsant, hypnotic and skeletal muscle relaxant. [Wikipedia] Camazepam also has less side effects, such as impaired cognition and reaction times, compared to other benzodiazepines. However, impairment of cognition and disrupted sleep patterns will occur at doses higher than 40mg of carazepam. [Wikipedia] Camazepam is also believed to increase attention, and is associated with skin disorders. In the United States camazepam is regulated as a Schedule IV controlled substance. Camazepam has been shown to bind competitively to benzodiazepine receptors in the brain with a relatively low affinity in animal models. This binding of benzodiazepine receptors by camazepam and its active metabolites is responsible for its anticonvulsant effects. Notably, only three metabolites were shown to exert anticonvulsant activity, temazepam, oxazepam, and hydroxy camazepam. The anxiolytic properties of camazepam are also attributed to their ability to bind benzodiazepine receptors, also known as GABA receptors. When benzodiazepines bind to GABA receptors they increase the efficiency with which the inhibitory neurotransmitter GABA binds.
Dược Động Học :
▧ Absorption :
Almost completely absorbed into the bloodstream after oral administration. 90% bioavailability can be achieved in humans.
▧ Metabolism :
Metabolized by the liver into more than 10 metabolites, some of which are also active and posses anticonvulsant properties. [3] One active metabolite of note is temazepam which has roughly equal in effectiveness as an anxiolytic, but is less anticonvulsant, sedating, and motor-impairing. Camazepam undergoes enantioselective metabolism by human liver microsomes. [1]
▧ Route of Elimination :
Renally eliminated.
Chỉ Định : Camazepam has been used in placebo controlled studies for the treatment of patients suffering from anxiety and depression.
Dữ Kiện Thương Mại
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