Tìm theo
Adinazolam
Các tên gọi khác (2) :
  • 8-Chloro-1-((dimethylamino)methyl)-6-phenyl-4H-S-triazolo(4,3-a)(1,4)benzodiazepine
  • Adinazolamum
antidepressive agents
Thuốc Gốc
Small Molecule
CAS: 37115-32-5
ATC: N05BA07
CTHH: C19H18ClN5
PTK: 351.833
Adinazolam (Deracyn®) is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed. Adinazolam was never FDA approved and was never available to the public.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H18ClN5
Phân tử khối
351.833
Monoisotopic mass
351.125073308
InChI
InChI=1S/C19H18ClN5/c1-24(2)12-18-23-22-17-11-21-19(13-6-4-3-5-7-13)15-10-14(20)8-9-16(15)25(17)18/h3-10H,11-12H2,1-2H3
InChI Key
InChIKey=GJSLOMWRLALDCT-UHFFFAOYSA-N
IUPAC Name
({12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaen-3-yl}methyl)dimethylamine
Traditional IUPAC Name
adinazolam
SMILES
CN(C)CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12
Độ hòa tan
6.72e-02 g/l
logP
4.4
logS
-3.7
pKa (strongest acidic)
18.38
pKa (Strongest Basic)
6.66
PSA
46.31 Å2
Refractivity
112.31 m3·mol-1
Polarizability
37.15 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Adinazolam is a benzodiazepine derivative used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia. Adinazolam binds with high affinity to the GABA benzodiazepine receptor complex. Considerable evidence suggest that the central pharmacologic/therapeutic actions of alprazolam are mediated via interaction with this receptor complex.
Cơ Chế Tác Dụng : Adinazolam (Deracyn®) is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed. Adinazolam was never FDA approved and was never available to the public. Adinazolam binds to peripheral-type 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 :

▧ Metabolism :
Hepatic. The main metabolite is N-desmethyladinazolam. The other two metabolites are alpha-hydroxyalprazolam and estazolam.
▧ Half Life :
Less than 3 hours.
Độc Tính : Signs of overdose may include muscle weakness, ataxia, dysarthria and particularly in children paradoxical excitement. In more severe cases diminished reflexes, confusion, and coma may ensue.
Chỉ Định : For the treatment of anxiety and status epilepticus.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Upjohn
    Sản phẩm biệt dược : Deracyn
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00546
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=37632
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509054
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02770
ChemSpider
http://www.chemspider.com/Chemical-Structure.34519.html
PharmGKB
http://www.pharmgkb.org/drug/PA164783813
Wikipedia
http://en.wikipedia.org/wiki/Adinazolam
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