European Journal of Medicinal Chemistry p. 547 - 556 (1996)
Update date:2022-08-17
Topics:
Varache-Lembege
Nuhrich
Zemb
Devaux
Vacher
Vacher
Dufy
The synthesis of a thienyl dihydropyridine series according to the Hantzsch method is described. The influence of these derivatives on intracellular calcium ([Ca2+](i)) in GH3 cells was evaluated in vitro using spectrofluorimetry with indol as Ca2+ fluorescent probe. We compared their effects on [Ca2+](i) and hormone release with those of nifedipine. The most active tested compounds on [Ca2+](i) were those methylated on the 3-position of the thienyl ring (activity was about 75% of nifedipine). Interestingly, the most efficient compounds on [Ca2+](i) were also the most efficient on hormone release.
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