STUDIES ON PROPHENPYRIDAMINE (TRIMETON) AND CHLORPROPHENPYRIDAMINE (CHLORTRIMETON)

¹ Biologicai Research Laboratories of Schering Corporation, Bloomfield, New Jersey

Several compounds were found to possess appreciable antihistaminic activity in guinea pigs, compounds (table 1) No. 1, 6, 7, 10, 12, 24 and 28 in the class of dialkylpropylamines and compounds No. 29, 37, 46 and 47 in the series of alkamine ethers.

The antihistaminic activity of 1-phenyl-1-(2-pyridyl)-3-N,N-dimethylpropylamine (1) and of the corresponding ether, 1-phenyl-1-(2-pyridyl)-methyl-N,N-dimethyl ethyl ether (29) was further increased by halogen substitution in para-position of the benzene ring.

Prophenpyridamine and chlorprophenpyridamine had a low systemic and local toxicity in acute and chronic tests. Halogenation of prophenpyridamine did not increase its systemic and local toxicity to any appreciable extent.