The effect on ephedrine prodrugs on locomotor activity in rats.
1. Five oxazolidines were synthesized by reaction of (-) ephedrine with formaldehyde, propionaldehyde, butyraldehyde, isobutyraldehyde, and acetone, respectively. 2. Half-lives of hydrolysis were measured in pH 7.4 aqueous buffer. Half-lives varied from 12 seconds to 11 minutes. 3. The compounds were evaluated for their ability to increase locomotor activity in rats. All compounds significantly increased locomotor activity at 50 mg/kg dose. 4. The formaldehyde derivative had similar activity to (-) ephedrine. All other compounds were less active than (-) ephedrine.
Walker
R B
RB
Chemistry Department, University of Arkansas at Pine Bluff 71601, USA.
Fitz
L D
LD
Williams
L M
LM
McDaniel
Y M
YM
D000818:Animals; D000697:Central Nervous System Stimulants / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004809:Ephedrine / Q000494:pharmacology*; D006207:Half-Life; D008297:Male; D009043:Motor Activity / Q000187:drug effects*; D011355:Prodrugs / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D000697:Central Nervous System Stimulants; D011355:Prodrugs; D004809:Ephedrine