title: Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists.
abstract: A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K(+) channel and serotonin transporter.
authors: Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Company, Ltd, 3 Okubo, Tsukuba 300-2611, Japan. kaimei_cho@yahoo.co.jp
authors: Kaimei
authors: K
authors: Cho
authors: Makoto
authors: M
authors: Ando
authors: Kensuke
authors: K
authors: Kobayashi
authors: Hiroshi
authors: H
authors: Miyazoe
authors: Toshiaki
authors: T
authors: Tsujino
authors: Sayaka
authors: S
authors: Ito
authors: Tomoki
authors: T
authors: Suzuki
authors: Takeshi
authors: T
authors: Tanaka
authors: Shigeru
authors: S
authors: Tokita
authors: Nagaaki
authors: N
authors: Sato
mesh_terms: D002460:Cell Line; D003514:Cyclohexylamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D051638:Ether-A-Go-Go Potassium Channels / Q000378:metabolism; D006801:Humans; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D003514:Cyclohexylamines; D051638:Ether-A-Go-Go Potassium Channels; C496884:KCNH1 protein, human; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor; D012701:Serotonin