PHARMACOLOGIC DATA ON DL-2-AMINO-1-(p-METHYLPHENYL)-PROPANE

¹ Research Division, Smith, Kline and French Laboratories, Philadelphia, Pennsylvania

1. In the present studies, the hyperkinesthetic activity of dl-2-amino-1-(p-methylphenyl)-propane (No. 42) in rats was found to be one-fifth intraperitoneally and one-tenth orally that of d-amino-1-phenylpropane (No. 2).

2. Orally No. 42 exhibited only one-twentieth the activity of No. 2 in antagonizing the depressant effect of phenobarhital. The analeptic potency of No. 42 therefore does not parallel its effectiveness in producing an increase in motor activity.

3. Subcutaneously in dogs, 5 mgm. manifested the same antiappetite potency as 1 mgm. of No. 2. It is therefore concluded that No. 42 may be a useful anorexigenic agent with a low order of "awakening" effect.

4. No. 42 may exhibit analgetic activity as indicated by the fact that doses of 5.0 to 20.0 mgm. intraperitoneally markedly elevated pain thresholds in cats.

5. In subacute and chronic toxicity studies no evidence of changes due to administration of No. 42 was observed by histological examination of tissues removed from rats, rabbits, guinea-pigs and dogs which received massive daily doses (up to 30 mgm.) of this compound for periods of one to three months.

6. The data obtained in the present experiments indicate that No. 42 should be evaluated clinically as an antiappetite and as an analgetic agent.