Tìm theo
Bifeprunox
Các tên gọi khác (2) :
  • Bifeprunox mesilate
  • Bifeprunoxum
Thuốc Gốc
Small Molecule
CAS: 350992-10-8
CTHH: C24H23N3O2
PTK: 385.4583
Bifeprunox is a novel atypical antipsychotic agent which, along with SLV313, aripiprazole and SSR-181507 combines minimal D2 receptor agonism with 5-HT receptor agonism. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H23N3O2
Phân tử khối
385.4583
Monoisotopic mass
385.179026995
InChI
InChI=1S/C24H23N3O2/c28-24-25-21-10-5-11-22(23(21)29-24)27-14-12-26(13-15-27)17-18-6-4-9-20(16-18)19-7-2-1-3-8-19/h1-11,16H,12-15,17H2,(H,25,28)
InChI Key
InChIKey=CYGODHVAJQTCBG-UHFFFAOYSA-N
IUPAC Name
7-{4-[(3-phenylphenyl)methyl]piperazin-1-yl}-2,3-dihydro-1,3-benzoxazol-2-one
Traditional IUPAC Name
bifeprunox
SMILES
O=C1NC2=C(O1)C(=CC=C2)N1CCN(CC2=CC(=CC=C2)C2=CC=CC=C2)CC1
Độ hòa tan
1.97e-02 g/l
logP
4.51
logS
-4.3
pKa (strongest acidic)
9.47
pKa (Strongest Basic)
7.83
PSA
44.81 Å2
Refractivity
116.49 m3·mol-1
Polarizability
43.09 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Bifeprunox is an atypical antipsychotic drug with mixed (agonist/antagonist) receptor activity with the neurotransmitters dopamine (D2/3/4) and serotonin. Bifeprunox differs from first-generation atypical antipsychotics in that it acts as a partial D2 agonist. This property is shared by aripiprazole, a drug already marketed in Europe and the US for treatment of schizophrenia. A placebo-controlled, dose-finding phase II trial in patients with schizophrenia showed that bifeprunox was both efficacious and well tolerated. Importantly, treatment with bifeprunox did not appear to cause some of the side effects seen with other atypicals agents in routine use, such as weight gain, hyperprolactinaemia and cardiotoxicity.
Cơ Chế Tác Dụng : Bifeprunox is a novel atypical antipsychotic agent which, along with SLV313, aripiprazole and SSR-181507 combines minimal D2 receptor agonism with 5-HT receptor agonism. [Wikipedia] In contrast to D2 receptor antagonism, partial D2 agonism is believed to decrease dopamine activity in an overactive dopamine system while simultaneously increasing dopamine activity in regions of the brain where dopaminergic activity is too low. By blocking overstimulated receptors and stimulating underactive ones, partial D2 agonists act as dopamine stabilisers. In common with aripiprazole, bifeprunox also acts as a serotonin, 5-HT1A agonist. This property may contribute to efficacy against the negative symptoms of schizophrenia and reduce the likelihood of extrapyramidal symptoms (EPS).
Chỉ Định : Bifeprunox is being evaluated for the treatment of schizophrenia, psychosis, and Parkinson's disease.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04888
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=208951
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=14878213
ChemSpider
http://www.chemspider.com/Chemical-Structure.181044.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241119
Wikipedia
http://en.wikipedia.org/wiki/Bifeprunox
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