PHARMACOLOGIC PROPERTIES OF N-ETHYL-3-PIPERIDYL BENZILATE METHOBROMIDE (JB-323), A POTENT ANTISPASMODIC AGENT

¹ Department of Pharmacology, Marquette University School of Medicine, Milwaukee, Wisconsin

1. N-Ethyl-3-piperidyl benzilate methobromide, JB-323, is an orally active antispasmodic agent with an atropine-like action.

2. In pentobarbitalized dogs, JB-323 has approximately the same spasmolytic potency as atropine and about four times that of Banthine on Prostigmininduced contractions of the sphincter of Oddi and ileum. It appears to be more effective than atropine in relaxing Prostigmin-induced spasm of the ureter and in inhibiting spontaneous contractions of the colon.

3. JB-323 possesses at least the same parasympatholytic activity as atropine and about seven times that of Banthine in blocking methacholine-induced chromodacryorrhea in rats.

4. JB-323 is approximately as effective as atropine and roughly three times as active as Banthine in protecting guinea pigs against fatal methacholineinduced bronchospasm.

5. No analgesic properties were demonstrated with JB-323 in animal studies.

6. JB-323 has less mydriatic effect than atropine when applied locally to the eye or injected intravenously in rabbits.

7. JB-323 has approximately the same antisalivary effect as atropine in unanesthetized rabbits.

8. JB-323 is relatively non-toxic in full spasmolytic dosage. In animals, it has essentially the same order of oral toxicity as atropine, but its intravenous toxicity is approximately four times that of atropine.