An evaluation of certain hypotensive agents. III. Tetrahydroisoquinoline and tetrahydroquinoline derivatives.

Abstract

The hypotensive activity of a series of diquaternarized tetrahydroisoquinoline and tetrahydroquinoiine derivatives was investigated in the anesthetized rat. The compounds were evaluated according to the mean duration of action of the dose of the compound producing a mean drop in blood pressure of approximately 50 per cent. Several of the compounds were further evaluated in normotensive dogs. The most active compounds were 1-(1,2,3,4-tetrahydroisoquinolino)-5-dimethylamino-3-hydroxy-3-ethinyl pentane dimethobromide (JB-5037), N-(3-dimethylamino-propyl)-1,2,3,4-tetrahydroisoquinoline dimethobromide (JB-621, IN-243) and 1-(1,2,3,4-tetrahydroisoquinolino)-5-dimethylamino-2-pentyne dimethiodide (JB-679).