A PHARMACOLOGIC COMPARISON OF METHOCARBAMOL (AHR-85), THE MONOCARBAMATE OF 3-(o-METHOXYPHENOXY)-1,2-PROPANEDIOL WITH CHEMICALLY RELATED INTERNEURONAL DEPRESSANT DRUGS

¹ A. H. Robins Company Laboratory and Department of Physiology and Pharmacology, The Bowman Gray School of Medicine of Wake Forest College, Winston-Salem, North Carolina

Measurement of the oral effectiveness of mephenesin, mephenesin carbamate, guiacol glyceryl ether (GGE) and the monocarbamate of GGE (AHR-85) in the rat by challenging doses of strychnine after varying periods of absorption showed that the two carbamate esters have significantly longer protective action. Duration of protection decreases in the following order: AHR-85, mephenesin carbamate, mephenesin and GGE.

AHR-85 has significantly greater anti-pentylenetetrazol activity than mephenesin carbamate when 30 minutes' absorption is allowed after intraperitoneal injection. Both of these compounds afford greater protection against pentylenetetrazol than their unesterified parent compounds.

AHR-85 exceeds both mephenesin and mephenesin carhamate in its protection against electroshock-generated tonic extensor convulsions when comparisons are made 60 minutes after intraperitoneal injection into mice.

The paralytic activity of AHR-85 is approximately the same as that of mephenesin after 60 minutes' absorption from the peritoneal space but exceeds that of mephenesin carbamate at this time.

Oral doses of AHR-85 prolong the sleeping time of hexobarbital-injected mice comparable to large oral doses of reserpine.

Abolition of the multisynaptic flexion reflex is produced by AHR-85 in doses having little effect on the knee jerk.

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