Tìm theo
Propiomazine
Các tên gọi khác (7 ) :
  • 10-(2-Dimethylaminopropyl)-2-propionylphenothiazine
  • 2-Propionyl-10-(2-(dimethylamino)propyl)phenothiazine
  • 3-Propionyl-10-dimethylaminoisopropylphenothiazine
  • Propiomazin
  • Propiomazina
  • Propiomazine
  • Propiomazinum
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 362-29-8
ATC: N05CM06
CTHH: C20H24N2OS
PTK: 340.482
Propiomazine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, propiomazine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H24N2OS
Phân tử khối
340.482
Monoisotopic mass
340.16093409
InChI
InChI=1S/C20H24N2OS/c1-5-18(23)15-10-11-20-17(12-15)22(13-14(2)21(3)4)16-8-6-7-9-19(16)24-20/h6-12,14H,5,13H2,1-4H3
InChI Key
InChIKey=UVOIBTBFPOZKGP-UHFFFAOYSA-N
IUPAC Name
1-{10-[2-(dimethylamino)propyl]-10H-phenothiazin-2-yl}propan-1-one
Traditional IUPAC Name
propiomazine
SMILES
CCC(=O)C1=CC2=C(SC3=CC=CC=C3N2CC(C)N(C)C)C=C1
Độ hòa tan
0.454 mg/L
logP
4.79
logS
-4.7
pKa (strongest acidic)
16.64
pKa (Strongest Basic)
8.32
PSA
23.55 Å2
Refractivity
103.53 m3·mol-1
Polarizability
38.62 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Although propiomazine is a phenothiazine, it is not used as an antipsychotic. It posesses antihistamine effects and is mostly used as a sedative in treating insomnia.
Cơ Chế Tác Dụng : Propiomazine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, propiomazine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors. Propiomazine is an antagonist at types 1, 2, and 4 dopamine receptors, serotonin (5-HT) receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Its main use as a sedative is due to its antihistamine effect.
Dược Động Học :

▧ Protein binding :
81%
▧ Metabolism :
Unknown, but most likely hepatic as with other phenothiazines.
Độc Tính : Rare, serious side effects include convulsions (seizures); difficult or unusually fast breathing; fast or irregular heartbeat or pulse; fever (high); high or low blood pressure; loss of bladder control; muscle stiffness (severe); unusual increase in sweating; unusually pale skin; and unusual tiredness or weakness.
Chỉ Định : Propiomazine is largely used for its antihistamininc sleep inducing effects in treating insomnia.
Tương Tác Thuốc :
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
  • Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Guanethidine Propiomazine may decrease the effect of guanethidine.
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Dorevan
  • Công ty :
    Sản phẩm biệt dược : Dorevane
  • Công ty :
    Sản phẩm biệt dược : Indorm
  • Công ty :
    Sản phẩm biệt dược : Largon
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Propavan
  • Công ty :
    Sản phẩm biệt dược : Serentin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00777
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4940
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506205
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07405
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02361
ChemSpider
http://www.chemspider.com/Chemical-Structure.4771.html
PharmGKB
http://www.pharmgkb.org/drug/PA164778685
Wikipedia
http://en.wikipedia.org/wiki/Propiomazine
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