Lawrence C. Weaver

Pharmacologic study of endobenzyline bromide, a new cholinergic blocking agent

Abstract Endobenzyline bromide has been investigated for cholinergic blocking action. By most tests, it is approximately as potent as atropine and oxyphenonium, and some-what more potent than methantheline in activity. The agent appears to exert its blocking effect quite selectively on the postganglionic parasympathetic nerve effector system. It does not produce a blocking effect on autonomic ganglia or skeletal neuromuscular junctions. It appears to have little or no central nervous system activity and possesses a wide margin of therapeutic safety.

Toxicopathologic and pharmacologic properties of piperacetazine, a potent tranquilizing agent.

Abstract For one year piperacetazine was administered continuously to rats at 0.005, 0.01, and 0.025% concentrations of their diets, and daily to dogs at 0.25, 1.0 and 5.0 mg/kg/day dosages by capsules orally. The drug was well tolerated by both species. Laboratory studies of the animals did not reveal any significant pathologic effects that were attributable to the drug. Piperacetazine failed to alter the convulsant properties of Metrazol but did show moderately effective antihistaminic properties.

The acute and chronic toxicities of chlorphenoxamine

Abstract The acute toxicity of chlorphenoxamine and Keithon were compared in mice and no significant difference was found between the LD50 values or the CD50 values for the two drugs. Chlorphenoxamine was administered for 26 weeks to rats in concentrations of 0.166, 0.249, and 0.374% of the diet without the production of significant pathologic alterations. Further, no profound alteration of the growth rate of rats was apparent. Although the mean weights were lowest in the groups (both sexes) receiving the highest concentration of drug, the per cent weight gain did not appear to be appreciably different than that of the control group. Chlorphenoxamine was administered orally to dogs for 18 weeks at 10 mg/kg/day, then for an additional 29 weeks at 30 mg/kg/day. Initially, an occasional mild emetic response was noted in some of the dogs and a loss of body weight was apparent. Otherwise, the drug was well tolerated for the experimental period. Histologic and hematologic studies revealed no abnormalities due to the drug.

Morphine antagonism with amiphenazole (2, 4-diamino-5-phenyl-thiazole hydrochloride).

Summary Amiphenazole was effective in antagonizing morphine depression in dogs; bromosulfolane was less effective even at toxic doses. Amiphenazole did not significantly alter the analgetic effect of morphine in mice, though this compound alone produced a mild but transient analgetic effect.