The synthesis of a series of 1-amino derivatives of 3-carboxymethyl-4-phenylisoquinoline and of dialkylaminoalkylamides of 2-methyl-3-carboxy-4-phenyl-1,2-dihydro-1-oxoisoquinoline and of 1-methoxy-3-carboxy-4-phenylisoquinoline is described. The pharmacological activity of some of these compounds was studied. 1-Morpholino-3-carboxymethyl-4-phenylisoquinoline (IV a) and 1-pyrrolidino derivatives (IV d) caused reduction in spontaneous activity and reactivity in mice whereas compounds (VIII a) and (XII b) showed good local anesthetic activity in infiltration tests.