Diphenylmethane 誘導体の研究 (第5報) N-Alkylaminopropyl-1,1-diphenyl-methylamine 類およびN-Alkylaminopropyl-1,2-diphenylethylamine 類の合成および薬理作用について

抄録

N-Alkylaminopropyl-1, 1-diphenylmethylamines and N-alkylaminoethylamines were synthesized and some pharmacological properties of these compounds were examined. Local anesthetic activities of IVa, Va, Ve, and Vf were more potent than that of procaine on the surface anesthesia in guinea pig cornea, but less potent than that of lidocaine. Vc had approximately the same potency as lidocaine. On the infiltration anesthesia in guinea pigs, Va, Vc, Ve, and Vf had almost the same potency of procaine. All of these compounds, however, had an intradermal irritancy in the rabbit skin. IVa, Va, and Ve produced marked inhibitory effect on the acetic acid-induced writhing in mice, and IVa, Vc, and Vd increased threshold of the tail pain response in mice. Vc and Vd were found to have an antitussive activity by the mechanically stimulating method in guinea pigs. Tremor caused by tremorine in mice was inhibited by IVa, but not by other compounds. All the test compounds produced a fall in the blood pressure of anesthetized rats and rabbits, and this action was not inhibited by pretreatment with atropine and diphenhydramine, respectively.