Abstract
By comparison with other analgetic drugs, including morphine, 1,2-dimethyl-3-phenyl-3-propionoxypyrrolidine (CI-427) has a prompt and unusually well sustained antinociceptive action in rodents by all routes. Its mg potency is inferior to codeine's by parenteral routes, equal or superior by the gastric route. It substantially lacks antipyretic (rats), anti-inflammatory (guinea pigs), antitussive (dogs), constipating (rats), respiratory depressant (dogs), and cardio-vascular (except at intravenous doses over 13 or 14 mg/kg; dogs) effects. It resembles meperidine in excitatory properties and body-temperature lowering action at high dosage but (as the hydrochioride) is less irritating subcutaneously. Of its constituent enantiomers, the d-isomer is about twice as potent and toxic parenterally as the l-isomer. By the gastric route the difference in effectiveness was less pronounced and there was some suggestion (P > 0.05) of mutual interference between the enantiomers. CNS side-effects were seen in unanesthetized dogs given 3.5 mg/kg of racernate intravenously during 1 minute.
Footnotes
- Received December 15, 1960.
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