Tìm theo
Sertindole
Các tên gọi khác (6 ) :
  • 1-[2-[4-[5-chloro-1-(4-Fluorophenyl)-indol-3-yl]-1-piperidyl]ethyl]imidazolidin-2-one
  • Serdolect
  • SerLect
  • Sertindol
  • Sertindole
  • Sertindolum
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 106516-24-9
ATC: N05AE03
CTHH: C24H26ClFN4O
PTK: 440.941
Sertindole, a neuroleptic, is one of the newer antipsychotic medications available. Serdolect is developed by the Danish pharmaceutical company H. Lundbeck. Like the other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. It is classified chemically as a phenylindole derivative. It was first marketed in 1996 in several European countries before being withdrawn two years later because of numerous cardiac adverse effects. It has once again been approved and should soon be available on the French and Australian market.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H26ClFN4O
Phân tử khối
440.941
Monoisotopic mass
440.177917386
InChI
InChI=1S/C24H26ClFN4O/c25-18-1-6-23-21(15-18)22(16-30(23)20-4-2-19(26)3-5-20)17-7-10-28(11-8-17)13-14-29-12-9-27-24(29)31/h1-6,15-17H,7-14H2,(H,27,31)
InChI Key
InChIKey=GZKLJWGUPQBVJQ-UHFFFAOYSA-N
IUPAC Name
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one
Traditional IUPAC Name
sertindole
SMILES
FC1=CC=C(C=C1)N1C=C(C2CCN(CCN3CCNC3=O)CC2)C2=C1C=CC(Cl)=C2
Độ hòa tan
9.63e-03 g/l
logP
3.77
logS
-4.7
pKa (strongest acidic)
14.36
pKa (Strongest Basic)
8.59
PSA
40.51 Å2
Refractivity
131.77 m3·mol-1
Polarizability
47.17 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Dược Lực Học : Sertindole is an atypical antipsychotic at least as effective as haloperidol and risperidone in the treatment of neuroleptic-responsive schizophrenia. Sertindole improves negative symptoms, and is also effective for the treatment of neuroleptic-resistant schizophrenia. Sertindole is generally well tolerated and is associated with a low rate of extrapyramidal symptoms (EPS).
Cơ Chế Tác Dụng : Sertindole, a neuroleptic, is one of the newer antipsychotic medications available. Serdolect is developed by the Danish pharmaceutical company H. Lundbeck. Like the other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. It is classified chemically as a phenylindole derivative. It was first marketed in 1996 in several European countries before being withdrawn two years later because of numerous cardiac adverse effects. It has once again been approved and should soon be available on the French and Australian market. Sertindole is an antipsychotic drug with affinity for dopamine D2, serotonin 5-HT2A and 5-HT2C, and alpha1-adrenoreceptors. Preclinical studies suggest that sertindole acts preferentially on limbic and cortical dopaminergic neurons and clinical trials have confirmed that sertindole is effective at a low dopamine D2 occupancy level.
Dược Động Học :
▧ Absorption :
Orally available.
▧ Metabolism :
Hepatic. Sertindole is metabolized by cytochrome P450 isoenzymes CYP 2D6 and CYP 3A4.
▧ Half Life :
3 days
Chỉ Định : Used in the treatment of schizophrenia.
Tương Tác Thuốc :
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Serdolect
  • Công ty :
    Sản phẩm biệt dược : Serlect
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06144
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60149
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504717
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07567
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00561
ChemSpider
http://www.chemspider.com/Chemical-Structure.54229.html
PharmGKB
http://www.pharmgkb.org/drug/PA164784002
Wikipedia
http://en.wikipedia.org/wiki/Sertindole
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