Hyperthermic and anorectic effects of oxazolidines derived from L-ephedrine in rats.
Oxazolidines synthesized from (-) ephedrine have been proposed as potential pro-drugs, but no pharmacological data on these compounds has been yet reported. In this study, four such compounds are tested in rats for ephedrine-like activity using the hyperthermia and anorexia models. The compounds were synthesized by reaction of (-) ephedrine with salicylaldehyde, acetone, cyclohexanone, and benzaldehyde, respectively. The results showed that all of the compounds decreased food intake significantly, but only the acetone and the salicylaldehyde derivatives caused a significant elevation of body temperature. All of the compounds were less effective than (-) ephedrine in the anorexia model. The acetone and salicylaldehyde derivatives showed similar potency to (-) ephedrine in the hyperthermia model.
University of Arkansas, Chemistry Department, Pine Bluff 71601.
R B
RB
Walker
D M
DM
Wood
M M
MM
Akmal
D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004435:Eating / Q000187:drug effects; D004809:Ephedrine / Q000031:analogs & derivatives / Q000378:metabolism* / Q000494:pharmacology; D008297:Male; D010080:Oxazoles / Q000494:pharmacology*; D011355:Prodrugs / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D010080:Oxazoles; D011355:Prodrugs; D004809:Ephedrine