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
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.