title: Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.
abstract: N-Substituted nipecotic and iso-nipecotic amides of beta-methylTrpLys tert-butyl ester were found to be novel, selective and potent agonists of the somatostatin subtype-2 receptor in vitro. For example iso-nipecotic amide 8a showed high hsst2 binding affinity (Ki = 0.5 nM) and good selectivity (h5/h2 = 832).
authors.affiliation: Merck Research Laboratories, Rahway, NJ 07065, USA. changyou_zhou@merck.com
authors.forename: C
authors.initials: C
authors.lastname: Zhou
authors.forename: L
authors.initials: L
authors.lastname: Guo
authors.forename: G
authors.initials: G
authors.lastname: Morriello
authors.forename: A
authors.initials: A
authors.lastname: Pasternak
authors.forename: Y
authors.initials: Y
authors.lastname: Pan
authors.forename: S P
authors.initials: SP
authors.lastname: Rohrer
authors.forename: E T
authors.initials: ET
authors.lastname: Birzin
authors.forename: S E
authors.initials: SE
authors.lastname: Huskey
authors.forename: T
authors.initials: T
authors.lastname: Jacks
authors.forename: K D
authors.initials: KD
authors.lastname: Schleim
authors.forename: K
authors.initials: K
authors.lastname: Cheng
authors.forename: J M
authors.initials: JM
authors.lastname: Schaeffer
authors.forename: A A
authors.initials: AA
authors.lastname: Patchett
authors.forename: L
authors.initials: L
authors.lastname: Yang
mesh_terms: D000818:Animals; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D007536:Isomerism; D009557:Nipecotic Acids / Q000138:chemical synthesis / Q000378:metabolism*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000378:metabolism; D011485:Protein Binding; D017481:Receptors, Somatostatin / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D009557:Nipecotic Acids; D009842:Oligopeptides; D017481:Receptors, Somatostatin; C027785:nipecotic acid amide; C094573:somatostatin receptor 5; C093733:somatostatin receptor 2