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Biaryl piperidines as potent and selective delta opioid receptor ligands |
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| Authors: | Spiros Liras Stanton F. McHardy Martin P. Allen Barb E. Segelstein Steven D. Heck Dianne K. Bryce Anne W. Schmidt Michelle Vanase-Frawley Ernesto Callegari Stafford McLean |
| Affiliation: | 1. Neuroscience Medicinal Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA;2. Neuroscience Biology, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA;3. Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA |
| Abstract: | The design and synthesis of novel opiates are reported. Based on the message-address principle a novel class of 4,4- and 3,3-biaryl piperidines was designed and synthesized. Biological evaluation confirmed that these compounds exhibit high affinity and selectivity for the delta opioid receptor. Key structure–activity relationships that influence affinity, selectivity, functional activity and clearance are reported. |
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