Tìm theo
Bicifadine
Thuốc Gốc
Small Molecule
CAS: 71195-57-8
CTHH: C12H15N
PTK: 173.2542
Bicifadine (DOV-220075) is a nonopioid analgesic. It is an inhibitor of both the norepinephrine and serotonin transporters and an NMDA antagonist with a non-narcotic profile. Bicifadine was shown to have potent analgesic activity in vivo and was chosen for further development for the treatment of pain.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H15N
Phân tử khối
173.2542
Monoisotopic mass
173.120449485
InChI
InChI=1S/C12H15N/c1-9-2-4-10(5-3-9)12-6-11(12)7-13-8-12/h2-5,11,13H,6-8H2,1H3
InChI Key
InChIKey=OFYVIGTWSQPCLF-UHFFFAOYSA-N
IUPAC Name
1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane
Traditional IUPAC Name
1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane
SMILES
CC1=CC=C(C=C1)C12CC1CNC2
Độ hòa tan
1.72e-01 g/l
logP
2.06
logS
-3
pKa (Strongest Basic)
10.6
PSA
12.03 Å2
Refractivity
54.31 m3·mol-1
Polarizability
20.7 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Bicifadine is a chemically distinct molecule with a unique profile of pharmacological activity. Its primary pharmacological action is to enhance and prolong the actions of norepinephrine and serotonin by inhibiting the transport proteins that terminate the physiological actions of the two biogenic amines. Bicifadine is not a narcotic and is well-tolerated and, in preclinical studies, has been shown not to act at any opiate receptor. Bicifadine does not exhibit any anti-inflammatory activity and does not inhibit prostaglandin synthetase in vitro.
Cơ Chế Tác Dụng : Bicifadine (DOV-220075) is a nonopioid analgesic. It is an inhibitor of both the norepinephrine and serotonin transporters and an NMDA antagonist with a non-narcotic profile. Bicifadine was shown to have potent analgesic activity in vivo and was chosen for further development for the treatment of pain. Preclinical studies and clinical trials indicate that bicifadine's analgesic properties result through the enhancement and prolongation of norepinephrine and serotonin actions, however other actions may be involved.
Dược Động Học :

▧ Metabolism :
The primary enzymes responsible for the primary metabolism of bicifadine in humans are MAO-B and CYP2D6.
Chỉ Định : For the treatment of pain.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04889
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=47953
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=12015676
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03110
ChemSpider
http://www.chemspider.com/Chemical-Structure.43618.html
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