title: Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
abstract: Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs have been prepared and evaluated for their GPR88 agonist activity and pharmacokinetic (PK) properties.
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA. Electronic address: carolyn.dzierba@bms.com.
authors.forename: Carolyn D
authors.initials: CD
authors.lastname: Dzierba
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Yingzhi
authors.initials: Y
authors.lastname: Bi
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Bireshwar
authors.initials: B
authors.lastname: Dasgupta
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Richard A
authors.initials: RA
authors.lastname: Hartz
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Vijay
authors.initials: V
authors.lastname: Ahuja
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Giovanni
authors.initials: G
authors.lastname: Cianchetta
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Godwin
authors.initials: G
authors.lastname: Kumi
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Li
authors.initials: L
authors.lastname: Dong
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Saadat
authors.initials: S
authors.lastname: Aleem
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Cynthia
authors.initials: C
authors.lastname: Fink
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Yudith
authors.initials: Y
authors.lastname: Garcia
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Michael
authors.initials: M
authors.lastname: Green
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Jianxin
authors.initials: J
authors.lastname: Han
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Soojin
authors.initials: S
authors.lastname: Kwon
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Ying
authors.initials: Y
authors.lastname: Qiao
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Jiancheng
authors.initials: J
authors.lastname: Wang
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Yulian
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Greg
authors.initials: G
authors.lastname: Zipp
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Zhi
authors.initials: Z
authors.lastname: Liang
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Neil
authors.initials: N
authors.lastname: Burford
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Meredith
authors.initials: M
authors.lastname: Ferrante
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Robert
authors.initials: R
authors.lastname: Bertekap
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Martin
authors.initials: M
authors.lastname: Lewis
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Angela
authors.initials: A
authors.lastname: Cacace
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: James
authors.initials: J
authors.lastname: Grace
authors.affiliation: Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381-1160, USA.
authors.forename: Alan
authors.initials: A
authors.lastname: Wilson
authors.affiliation: Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381-1160, USA.
authors.forename: Amr
authors.initials: A
authors.lastname: Nouraldeen
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Ryan
authors.initials: R
authors.lastname: Westphal
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: David
authors.initials: D
authors.lastname: Kimball
authors.affiliation: Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
authors.forename: Kenneth
authors.initials: K
authors.lastname: Carson
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: Joanne J
authors.initials: JJ
authors.lastname: Bronson
authors.affiliation: Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
authors.forename: John E
authors.initials: JE
authors.lastname: Macor
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004983:Ethanolamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D057809:HEK293 Cells; D006801:Humans; D015394:Molecular Structure; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D004983:Ethanolamines; C418740:GPR88 protein, human; D043562:Receptors, G-Protein-Coupled; C005332:N-phenylethanolamine
keywords: Agonist; GPR88; Phenyl amine; Phenylglycinol; Schizophrenia