- Molecular NameAmfepramone, Diethylpropion
- SynonymN/A
- Weight205.301
- Drugbank_IDDB00937
- ACS_NO90-84-6
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)2.64
- pkaN/A
- LogD (pH=7, predicted)1.6
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-0.98
- LogSw (predicted, AB/LogsW2.0)4.31
- Sw (mg/ml) (predicted, ACD/Labs)0.72
- No.of HBond Donors0
- No.of HBond Acceptors2
- No.of Rotatable Bonds5
- TPSA20.31
- StatusFDA approved
- AdministrationN/A
- PharmacologyA stimulant drug of the phenethylamine, amphetamine, and cathinone chemical classes that is used as an appetite suppressant.
- Absorption_value95.0
- Absorption (description)Diethylpropion is rapidly absorbed from the GI tract after oral administration.
- Caco_2N/A
- BioavailabilityN/A
- Protein bindingN/A
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolised by N-dealkylation, reduction, deamination, and N-hydroxylation primarily to active metabolites; keto reduction is stereoselective resulting in the formation of threo-hydroxylated metabolites; glucuronide formation also occurs along with the formation of hippuric and mandelic acids.
- Half lifeDerived from urinary excretion data, 1.5~3 h in subjects whose urines are acidic.
- ExcretionAbout 80 to 90% of a dose is excreted in the urine; the amount excreted in the urine is reduced when the urine is alkaline; of the urinary excreted material, N-ethylaminopropiophenone, norephedrine (phenylpropanolamine), and hippuric acid are the main metabolites together with small amounts of unchanged drug, aminopropiophenone, N-diethylnorephedrine, and N-ethylnorephedrine. Diethylpropion crosses the blood–brain barrier and the placenta. The drug and its metabolites are distributed into breast milk.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityManifestation of acute overdosage include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, and panic states. The estimated minimum lethal doses are 200 mg for a child and 2 g for an adult.
- LD50 (rat)N/A
- LD50 (mouse)600 mg/kg