Dm. Mondeshka et al., SYNTHESIS, ANTIULCER AND ANTIDEPRESSIVE ACTIVITY OF LOPHENYL)-2-PHENYL-1,2,3,4-TETRAHYDROISOQUINOLINES, Il Farmaco, 49(7-8), 1994, pp. 475-480
ophenyl)-2-methyl-1,2,3,4-tetrahydro-isoquinolines 2a-c have been synt
hesized by two methods and their biochemical and pharmacological prope
rties have been studied. Biochemical investigations showed that all th
e compounds are strong inhibitors of DA, NE and 5-HT reuptake, the str
ongest effect being observed with compound 2b (R=Br). 2a-c exhibited a
strong antiulcer activity on an experimental model of stress-induced
ulcers with minimal doses (0.1 to 3.0 mg/kg), the effect of 2b being 3
0 times higher as compared to the H-2-antagonist Ranitidin. At higher
doses (10 to 30 mg/kg) 2b and 2c inhibited the Reserpinptosis. The mos
t active compound in the reuptake inhibition 2b, expressed a high anti
depressive activity in some other tests, comparable to that of the ant
idepressant Nomifensin. 2b has been selected for further pharmacologic
al testing under the code name AN(12).