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Heterocyclic aminopyrrolidine derivatives as melatoninergic agents |
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| Authors: | Sun Li-Qiang Chen Jie Mattson Ronald J Epperson James R Deskus Jeffrey A Li Wen Sen Takaki Katherine Hodges Donald B Iben Lawrence Mahle Cathy D Ortiz Astrid Molstad David Ryan Elaine Yeleswaram Krishnaswamy Xu Cen Luo Guanglin |
| Affiliation: | a Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA b Bristol-Myers Squibb Pharmaceutical Research Institute, One Squibb Drive, New, Brunswick, NJ 08903, USA |
| Abstract: | A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT1 and MT2 receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT1 and MT2 melatonin receptors with low vasoconstrictive activity. |
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