SYNTHESIS, ANTIULCER AND ANTIDEPRESSIVE ACTIVITY OF LOPHENYL)-2-PHENYL-1,2,3,4-TETRAHYDROISOQUINOLINES

Citation
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
Citations number
14
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
ISSN journal
0014827X
Volume
49
Issue
7-8
Year of publication
1994
Pages
475 - 480
Database
ISI
SICI code
0014-827X(1994)49:7-8<475:SAAAAO>2.0.ZU;2-D
Abstract
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).