Ontology highlight
ABSTRACT:
SUBMITTER: Ondachi PW
PROVIDER: S-EPMC4554999 | biostudies-literature | 2015 Sep
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry 20150717 17
Over the last several years we have synthesized and studied the in vitro and in vivo nAChR pharmacological properties of epibatidine (4) analogs. In this study we report the synthesis, nAChR in vitro and in vivo pharmacological properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs (5a-e and 6a-e). All of the analogs had high binding affinity for α4β2(∗)-nAChRs. Several of the analogs were potent antagonists of α4β2-nAChRs in in vitro efficacy tests and were potent antagonists of ...[more]