Discovery of ML314, a brain penetrant nonpeptidic β-arrestin biased agonist of the neurotensin NTR1 receptor

ACS Medicinal Chemistry Letters

Volumn 4, Issue 9, 2013, Pages 846-851

  Peddibhotla, Satyamaheshwar ^a   Hedrick, Michael P ^a   Hershberger, Paul ^a   Maloney, Patrick R ^a   Li, Yujie ^a   Milewski, Monika ^a   Gosalia, Palak ^a   Gray, Wilson ^a   Mehta, Alka ^a   Sugarman, Eliot ^a   Hood, Becky ^a   Suyama, Eigo ^a   Nguyen, Kevin ^a   Heynen Genel, Susanne ^a   Vasile, Stefan ^a   Salaniwal, Sumeet ^a   Stonich, Derek ^a   Su, Ying ^a   Mangravita Novo, Arianna ^a   Vicchiarelli, Michael ^a   Roth, Gregory P ^a   Smith, Layton H ^a   Chung, Thomas D Y ^a   Hanson, Glen R ^b   Thomas, James B ^d   Caron, Marc G ^c   Barak, Lawrence S ^c   Pinkerton, Anthony B ^a   more..

^a BURNHAM INSTITUTE   (United States)

^b UNIVERSITY OF UTAH   (United States)

^c DUKE UNIVERSITY MEDICAL CENTER   (United States)

^d RTI INTERNATIONAL   (United States)

Author keywords

addiction; agonist; GPCR; neurotensin; NTR1; quinazoline; SR142948A; arrestin bias

Indexed keywords

2 CYCLOPROPYL 6,7 DIMETHOXY 4 [4 (2 METHOXYPHENYL)PIPERAZIN 1 YL]QUINAZOLINE; 2 [5 (2,6 DIMETHOXYPHENYL) 1 [4 [N (3 DIMETHYLAMINOPROPYL) N METHYLCARBAMOYL] 2 ISOPROPYLPHENYL] 1H PYRAZOL 3 YLCARBONYLAMINO]ADAMANTANE 2 CARBOXYLIC ACID; BETA ARRESTIN; G PROTEIN COUPLED RECEPTOR; NEUROTENSIN 1 RECEPTOR; NEUROTENSIN RECEPTOR; OPIATE AGONIST; QUINAZOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING SITE; BLOOD BRAIN BARRIER; CALCIUM MOBILIZATION; CONCENTRATION RESPONSE; CROSS REACTION; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DEVELOPMENT; DRUG PENETRATION; DRUG SOLUBILITY; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; LIVER CLEARANCE; LIVER HOMOGENATE; LIVER MICROSOME; MOUSE; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; X RAY CRYSTALLOGRAPHY;

RODENTIA;

EID: 84884257510     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml400176n     Document Type: Article

References (26)

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