SYNTHESIS AND ACTIVITIES OF A THIENYL DIHYDROPYRIDINE SERIES ON INTRACELLULAR CALCIUM IN A RAT PITUITARY CELL-LINE (GH3 B6)/

Citation
M. Varachelembege et al., SYNTHESIS AND ACTIVITIES OF A THIENYL DIHYDROPYRIDINE SERIES ON INTRACELLULAR CALCIUM IN A RAT PITUITARY CELL-LINE (GH3 B6)/, European journal of medicinal chemistry, 31(7-8), 1996, pp. 547-556
Citations number
38
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
31
Issue
7-8
Year of publication
1996
Pages
547 - 556
Database
ISI
SICI code
0223-5234(1996)31:7-8<547:SAAOAT>2.0.ZU;2-D
Abstract
The synthesis of a thienyl dihydropyridine series according to the Han tzsch method is described. The influence of these derivatives on intra cellular calcium ([Ca2+]i) in GH3 cells was evaluated in vitro using s pectrofluorimetry with indol as Ca2+ fluorescent probe. We compared th eir effects on [Ca2+]i and hormone release with those of nifedipine. T he most active tested compounds on [Ca2+]i were those methylated on th e 3-position of the thienyl ring (activity was about 75% of nifedipine ). Interestingly, the most efficient compounds on [Ca2+]i were also th e most efficient on hormone release.