title: The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.
abstract: The identification and subsequent optimisation of a selective non-peptidic NPY Y2 antagonist series is described. This led to the development of amine 2, a selective, soluble NPY Y2 receptor antagonist with enhanced CNS exposure.
authors.affiliation: GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK. gill@lunniss.net
authors.forename: Gillian E
authors.initials: GE
authors.lastname: Lunniss
authors.forename: Ashley A
authors.initials: AA
authors.lastname: Barnes
authors.forename: Nick
authors.initials: N
authors.lastname: Barton
authors.forename: Matteo
authors.initials: M
authors.lastname: Biagetti
authors.forename: Federica
authors.initials: F
authors.lastname: Bianchi
authors.forename: Stephen M
authors.initials: SM
authors.lastname: Blowers
authors.forename: Laura L
authors.initials: LL
authors.lastname: Caberlotto
authors.forename: Amanda
authors.initials: A
authors.lastname: Emmons
authors.forename: Ian P
authors.initials: IP
authors.lastname: Holmes
authors.forename: Dino
authors.initials: D
authors.lastname: Montanari
authors.forename: Roz
authors.initials: R
authors.lastname: Norris
authors.forename: Gemma V
authors.initials: GV
authors.lastname: Puckey
authors.forename: Dewi J
authors.initials: DJ
authors.lastname: Walters
authors.forename: Steve P
authors.initials: SP
authors.lastname: Watson
authors.forename: John
authors.initials: J
authors.lastname: Willis
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D002490:Central Nervous System / Q000187:drug effects; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000588:Amines; D011743:Pyrimidines; D017476:Receptors, Neuropeptide Y; D013141:Spiro Compounds; C095889:neuropeptide Y2 receptor