title: Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.
abstract: Cyclopentylamine 4 was identified as a potent dual NK1R antagonist-SERT inhibitor. This compound demonstrated significant oral activity in the gerbil forced swimming test, suggesting that dual NK1R antagonists-SERT inhibitors may be useful in treating depression disorders.
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA. Electronic address: yong-jin.wu@bms.com.
authors: Yong-Jin
authors: YJ
authors: Wu
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Huan
authors: H
authors: He
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Qi
authors: Q
authors: Gao
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Dedong
authors: D
authors: Wu
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Robert
authors: R
authors: Bertekap
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Ryan S
authors: RS
authors: Westphal
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Snjezana
authors: S
authors: Lelas
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Amy
authors: A
authors: Newton
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Tanya
authors: T
authors: Wallace
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Matthew
authors: M
authors: Taber
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Carl
authors: C
authors: Davis
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: John E
authors: JE
authors: Macor
authors: Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
authors: Joanne
authors: J
authors: Bronson
mesh_terms: D000284:Administration, Oral; D000818:Animals; D018360:Crystallography, X-Ray; D003517:Cyclopentanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D005849:Gerbillinae; D006801:Humans; D008968:Molecular Conformation; D009043:Motor Activity / Q000187:drug effects; D064729:Neurokinin-1 Receptor Antagonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding; D018040:Receptors, Neurokinin-1 / Q000737:chemistry* / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins / Q000737:chemistry* / Q000378:metabolism; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D003517:Cyclopentanes; D064729:Neurokinin-1 Receptor Antagonists; D018040:Receptors, Neurokinin-1; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; C016329:cyclopentylamine
keywords: Dual NK(1) receptor antagonists–serotonin reuptake transporter inhibitor; NK(1) receptor (NK(1)R) antagonist; Serotonin reuptake transporter (SERT) inhibitor