Health & Environmental Research Online (HERO)

Print Feedback Export to File
Journal Article 
Relative Lipolytic Activities In Vitro Of A Series Of Phenethyl Amines 
Arnold, A; Mcauliff, JP 
Biochemical Pharmacology
ISSN: 0006-2952
EISSN: 1873-2968 
The relative lipolytic activities of a series of phenethyl amines were studied in-vitro. Epididymal fat tissue obtained from Sprague-Dawley-rats was incubated with 1-norepinephrine (51412) or 26 other phenethyl amines for 30 or 60 minutes. The extent of lipolysis was evaluated as the amount of glycerol released. The lipolytic activities of the amines were calculated relative to norepinephrine on a molar basis. The relative lipolytic activities were tabulated. With the exception of epinephrine (51434), N-substitution increased lipolytic effectiveness. With nordefrine (829743), alpha methyl substitution increased lipolytic effectiveness relative to the unsubstituted compound. Alpha methyl carbon substitution decreased the lipolytic effectiveness of dl-N-methyl-alpha-methylnorepinephrine, dl-N-isopropyl-alpha-methylnorepinephrine, and dl-N-cyclopentyl-alpha-ethylnorepinephrine. Alpha ethyl substitution markedly decreased the activity of the compounds, in some cases to negligible values. Amines having fewer than two phenolic hydroxyl groups or amines lacking an alpha carbon hydroxyl group also showed decreased lipolytic activity. The authors note that the data can serve as a basis for correlating lipolytic activities with other biochemical and pharmacological activities of phenethyl amines. 
DCN-143907; Laboratory techniques; In vitro studies; Biochemical analysis; Chemical properties; Bioassays; Laboratory animals; Biological effects; Analytical methods; Amino compounds; Pharmacology