Metabolism of Prolintane in Rats and the Effect of Prolintane Metabolites on General Activities in Mice

Abstract

1. The metabolism of prolintane in vivo has been investigated in rats; the pharmacological effects in mice of the metabolites from rats and rabbits have been examined.

2. In four rats receiving [³H]prolintane (50 mg/kg, intraperitoneal) about 57% of the radioactivity was excreted in the 48 h urine.

3. A pyrrolidine ring-opened metabolite (15% dose) and p-hydroxyprolintane (5% dose) were excreted as predominant metabolites together with traces of unchanged drug and oxoprolintane.

4. The general activities (ambulation and rearing) of mice were increased significantly by p-hydroxyprolintane and (ω — 1)-hydroxyprolintane as well as prolintane. Oxoprolintane was not effective on ambulation, but partially effective on rearing. However, PPGABA showed a depressant effect in mice rather than being stimulatory.