THE PHARMACOLOGICAL ACTIVITY OF DL-ALPHA, ALPHA-DIPHENYL, GAMMA-DIMETHYLAMINOVALERAMIDE (CENTRINE)

¹ Pharmacology Department, Research Division of Bristol Laboratories Inc., Syracuse, N. Y.

1. DL-alpha, alpha-diphenyl, gamma-dimethylaminovaleramide, Centrine (previously referred to as BL-139), shows approximately one-half the activity of atropine and one-fifth the activity of papaverine on isolated guinea pig and rabbit ileum strips.

2. Centrine causes a decrease in tone and a reduction in activity of most portions of the gastro-intestinal tract. It effectively counteracts the spasmogenic responses to acetylcholine and arecoline.

3. Oral administration requires very little increase in dosage to obtain responses comparable to those following intramuscular or intravenous administration.

4. Centrine is more effective in decreasing the activity of the intact colon than either atropine or Banthine and also has a greater duration of action.

5. Centrine is slightly less active than atropine in blocking the vasodepressor responses to acetylcholine and arecoline. Atropine is at least four times more active in blocking the effects of vagal stimulation on the heart.

6. Centrine has less mydriatic and salivary effects than atropine.

7. Dogs tolerate prolonged daily oral feedings of 25 mgm./kgm. of Centrine. Higher doses produce drying of the mucous surfaces. Prolonged daily oral administration of doses up to 50 mgm./kgm. does not produce any gross or microscopic abnormalities.