Design, Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of Bridgehead Iodinated Analogues of N-{2-[4-(2-Methoxyphenyl) piperazin-1-yl] ethyl}-N-( …

R Al Hussainy, J Verbeek, D van der Born…

Index: Al Hussainy, Rana; Verbeek, Joost; Van Der Born, Dion; Braker, Anton H.; Leysen, Josee E.; Knol, Remco J.; Booij, Jan; Herscheid Journal of Medicinal Chemistry, 2011 , vol. 54, # 10 p. 3480 - 3491

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Citation Number: 13

Abstract

Here we describe the design, synthesis, and pharmacological profile of 5-HT1A receptor ligands related to 1 (WAY-100635). The cyclohexyl moiety in 1 and its O-desmethylated analogue 3 were replaced by the bridgehead iodinated bridge-fused rings: adamantyl, cubyl, bicyclo [2.2. 2] octyl, or bicyclo [2.2. 1] heptyl. All analogues displayed a (sub) nanomolar affinity for the 5-HT1A receptor in vitro. Compounds 6b and 7b appeared to be ...

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