title: Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.
abstract: A series of 2,4-diaminopyridine derivatives was synthesized and evaluated as potential candidates for neuropeptide Y (NPY) Y1 receptor positron emission tomography (PET) tracers. Derivatives bearing substitutions allowing reliable access to radiolabeling were designed, focusing on Y1 binding affinity and lipophilicity. The advanced derivatives 2n and 2o were identified as promising PET tracer candidates.
authors.affiliation: Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co. Ltd, Okubo 3, Tsukuba, Ibaraki, Japan.
authors.forename: Minoru
authors.initials: M
authors.lastname: Kameda
authors.forename: Makoto
authors.initials: M
authors.lastname: Ando
authors.forename: Chisato
authors.initials: C
authors.lastname: Nakama
authors.forename: Kensuke
authors.initials: K
authors.lastname: Kobayashi
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Kawamoto
authors.forename: Sayaka
authors.initials: S
authors.lastname: Ito
authors.forename: Tomoki
authors.initials: T
authors.lastname: Suzuki
authors.forename: Takeshi
authors.initials: T
authors.lastname: Tani
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ozaki
authors.forename: Shigeru
authors.initials: S
authors.lastname: Tokita
authors.forename: Nagaaki
authors.initials: N
authors.lastname: Sato
mesh_terms: D015761:4-Aminopyridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D000631:Aminopyridines / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D049268:Positron-Emission Tomography; D017476:Receptors, Neuropeptide Y / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000631:Aminopyridines; D017476:Receptors, Neuropeptide Y; D011994:Recombinant Proteins; D013844:Thiazoles; C097212:neuropeptide Y-Y1 receptor; C026805:2,4-diaminopyridine; D015761:4-Aminopyridine