Synthesis and evaluation of phenylcarbamate derivatives as ligands for nicotinic acetylcholine receptors |
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Authors: | Gündisch Daniela Andrä Matthias Munoz Lenka Cristina Tilotta Maria |
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Institution: | Department of Pharmaceutical Chemistry, Rhein. Friedr.-Wilhelm-University, Kreuzbergweg 26, D-53115 Bonn, Germany. d.guendisch@uni-bonn.de |
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Abstract: | Phenylcarbamate derivatives were synthesized and evaluated in radioligand binding assays for different nicotinic acetylcholine receptor (nAChR) subtypes. Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8-20 exhibited much lower affinity for alpha7* nAChR than the analogues in the quinuclidine series 21-25, although the same structural elements are present. Furthermore, in contrast to the quinuclidine analogues 21-25, all (S)-pyrrolidine derivatives 8-12 and the piperidine analogues 15 and 16 exhibited higher affinities for alpha4beta2* nAChR. |
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