Synthesis of two optically active calcium channel antagonists labelled with carbon-11 for in vivo cardiac PET imaging

F Dollé, F Hinnen, H Valette, C Fuseau, R Duval…

Index: Dolle, Frederic; Hinnen, Francoise; Valette, Heric; Fuseau, Chantal; Duval, Raphael; Peglion, Jean-Louis; Crouzel, Christian Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 4 p. 749 - 764

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Citation Number: 23

Abstract

(±)-S11568 (1. 3-ethyl-5-methyl-(±)-2-[(2-(2-aminoethoxy) ethoxy) methyl]-4-(2, 3- dichlorophenyl)-6-methyl-1, 4-dihydropyridine-3, 5-dicarboxylate), has an in vitro profile of high potency and of high electivity for the low-voltage dependent L-type calcium channel. In in vitro binding studies, it displaced specifically bound (-)-[3H] PN 200–110 (isradipine (2), the reference molecule for in vitro studies) from cardiac and vascular smooth muscle ...