Tìm theo
Diethylpropion
Các tên gọi khác (12 ) :
  • (+-)-Diethylpropion
  • (±)-diethylpropion
  • 1-phenyl-2-diethylamino-1-propanone
  • 2-(Diethylamino)-1-phenyl-1-propanone
  • 2-(Diethylamino)propiophenone
  • alpha-Benzoyltriethylamine
  • alpha-Diethylaminopropiophenone
  • Amfepramone
  • Amfepramonum
  • Anfepramona
  • Diethylcathinone
  • Diethylpropion
appetite depressants, stimulants
Thuốc Gốc
Small Molecule
CAS: 90-84-6
ATC: A08AA03
ĐG : Aidarex Pharmacuticals LLC , http://www.aidarex.com
CTHH: C13H19NO
PTK: 205.2961
A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H19NO
Phân tử khối
205.2961
Monoisotopic mass
205.146664235
InChI
InChI=1S/C13H19NO/c1-4-14(5-2)11(3)13(15)12-9-7-6-8-10-12/h6-11H,4-5H2,1-3H3
InChI Key
InChIKey=XXEPPPIWZFICOJ-UHFFFAOYSA-N
IUPAC Name
2-(diethylamino)-1-phenylpropan-1-one
Traditional IUPAC Name
diethylpropion
SMILES
CCN(CC)C(C)C(=O)C1=CC=CC=C1
Độ tan chảy
168
Độ hòa tan
1.22e+00 g/l
logP
2.8
logS
-2.2
pKa (strongest acidic)
17.43
pKa (Strongest Basic)
7.44
PSA
20.31 Å2
Refractivity
63.88 m3·mol-1
Polarizability
24.12 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Diethylpropion is a sympathomimetic stimulant drug marketed as an appetite suppressant. Chemically, it is the N,N-diethyl analog of cathinone. Its mechanism of action is similar to other appetite suppressants such as sibutramine, phentermine and dextroamphetamine.
Cơ Chế Tác Dụng : A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290) Diethylpropion is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. Diethylpropion (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that diethylpropion can raise levels of leptin which signal satiety. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage.
Dược Động Học :
▧ Absorption :
Diethylpropion is rapidly absorbed from the GI tract after oral administration.
▧ Metabolism :
Extensively metabolized through a complex pathway of biotransformation involving N-dealkylation and reduction. Many of these metabolites are biologically active and may participate in the therapeutic action of diethylpropion.
▧ Route of Elimination :
Diethylpropion is rapidly absorbed from the GI tract after oral administration and is extensively metabolized through a complex pathway of biotransformation involving N-dealkylation and reduction. Diethylpropion and/or its active metabolites are believed to cross the blood-brain barrier and the placenta. Diethylpropion and its metabolites are excreted mainly by the kidney.
▧ Half Life :
Using a phosphorescence assay that is specific for basic compounds containing benzoyl group, the plasma half-life of the aminoketone metabolites is estimated to be between 4 to 6 hours.
Độc Tính : The reported oral LD50 for mice is 600 mg/kg, for rats is 250 mg/kg and for dogs is 225 mg/kg. Manifestation of acute overdosage include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, and panic states.
Chỉ Định : Used in the management of exogenous obesity as a short-term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction.
Tương Tác Thuốc :
  • Acetophenazine Decreased anorexic effect, may increase psychotic symptoms
  • Alimemazine Decreased anorexic effect, may increase psychotic symptoms
  • Chlorpromazine Decreased anorexic effect, may increase psychotic symptoms
  • Ethopropazine Decreased anorexic effect, may increase psychotic symptoms
  • Fluoxetine Risk of serotoninergic syndrome
  • Fluphenazine Decreased anorexic effect, may increase psychotic symptoms
  • Fluvoxamine Risk of serotoninergic syndrome
  • Guanethidine Diethylpropion may decrease the effect of guanethidine.
  • Isocarboxazid Possible hypertensive crisis
  • Mesoridazine Decreased anorexic effect, may increase psychotic symptoms
  • Methdilazine Decreased anorexic effect, may increase psychotic symptoms
  • Methotrimeprazine Decreased anorexic effect, may increase psychotic symptoms
  • Paroxetine Risk of serotoninergic syndrome
  • Perphenazine Decreased anorexic effect, may increase psychotic symptoms
  • Phenelzine Possible hypertensive crisis
  • Prochlorperazine Decreased anorexic effect, may increase psychotic symptoms.
  • Promazine Decreased anorexic effect, may increase psychotic symptoms
  • Promethazine Decreased anorexic effect, may increase psychotic symptoms.
  • Propericiazine Decreased anorexic effect, may increase psychotic symptoms.
  • Propiomazine Decreased anorexic effect, may increase psychotic symptoms
  • Rasagiline Possible hypertensive crisis
  • Thiethylperazine Decreased anorexic effect, may increase psychotic symptoms
  • Thioridazine Decreased anorexic effect, may increase psychotic symptoms
  • Tranylcypromine Possible hypertensive crisis
  • Trifluoperazine Decreased anorexic effect, may increase psychotic symptoms
  • Triflupromazine Decreased anorexic effect, may increase psychotic symptoms
  • Venlafaxine Risk of serotoninergic syndrome
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
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    Sản phẩm biệt dược : Tylinal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00937
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=7029
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506622
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06954
ChemSpider
http://www.chemspider.com/Chemical-Structure.6762.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64720-208-10
PharmGKB
http://www.pharmgkb.org/drug/PA164778098
Wikipedia
http://en.wikipedia.org/wiki/Diethylpropion
RxList
http://www.rxlist.com/cgi/generic3/diethprop.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ten1435.shtml
Drugs.com
http://www.drugs.com/cdi/diethylpropion.html
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