Abstract

In order to clarify the relationship between chemical structure and pharmacological action, 14 compounds of monohalogenated benzhydryl aminoethyl ether series of the general formula X- CH-O-CH2CH2Y (X=F, Cl, Br; Y=NMe2, NEt2, piperidino, morpholino, 1-pyrrolidinyl) were synthesized and their pharmacological activities were examined chiefly on antihistamine, antiacetylcholine, and antibarium actions. In general, monofluorinated derivatives showed marked antihistamine activity either by the Magnus or anti-histamine shock method. Chloromorpholine and bromomorpholine derivatives showed marked lowering of toxicity and an abnormally strong activity against histamine shock compared to that by Magnus method. These compounds may prove to be a new antihistamine agents and examinations are being made to see if they also possess sedative, antitussive, and hypotensive actions.

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