title: Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
abstract: A novel class of small-molecule, highly potent, and subtype-selective somatostatin SST3 agonists was discovered through modification of a SST3 antagonist. As an example, (1R,2S)-9 demonstrated not only potent in vitro SST3 agonist activity but also in vivo SST3 agonist activity in a mouse oral glucose tolerance test (OGTT). These agonists may be useful reagents for studying the physiological roles of the SST3 receptor and may potentially be useful as therapeutic agents.
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Derun
authors.initials: D
authors.lastname: Li
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Zhicai
authors.initials: Z
authors.lastname: Wu
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Yang
authors.initials: Y
authors.lastname: Yu
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Richard G
authors.initials: RG
authors.lastname: Ball
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Liangqin
authors.initials: L
authors.lastname: Guo
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Edward
authors.initials: E
authors.lastname: Sherer
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Shuwen
authors.initials: S
authors.lastname: He
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Qingmei
authors.initials: Q
authors.lastname: Hong
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Zhong
authors.initials: Z
authors.lastname: Lai
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Hongbo
authors.initials: H
authors.lastname: Qi
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Quang
authors.initials: Q
authors.lastname: Truong
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: David X
authors.initials: DX
authors.lastname: Yang
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Gary G
authors.initials: GG
authors.lastname: Chicchi
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Kwei-Lan
authors.initials: KL
authors.lastname: Tsao
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Dorina
authors.initials: D
authors.lastname: Trusca
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Maria
authors.initials: M
authors.lastname: Trujillo
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Michele
authors.initials: M
authors.lastname: Pachanski
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: George J
authors.initials: GJ
authors.lastname: Eiermann
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Howard
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Yun-Ping
authors.initials: YP
authors.lastname: Zhou
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Bei B
authors.initials: BB
authors.lastname: Zhang
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
authors.affiliation: Departments of Medicinal Chemistry and Diabetes Research, Merck Research Laboratories , 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
authors.forename: William K
authors.initials: WK
authors.lastname: Hagmann
keywords: GPCR; Somatostatin; small-molecule SST3 agonists; somatostin receptor subtype 3 (SST3)