Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 2, 2014, Pages 674-678

  Jin, Zhuang ^a   Khan, Pasha ^a   Shin, Youseung ^a   Wang, Jingyi ^b   Lin, Li ^a   Cameron, Michael D ^a   Lindstrom, Jon M ^b   Kenny, Paul J ^a   Kamenecka, Theodore M ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

4 2 5; Positive allosteric modulators; Substituted heteroaromatics

Indexed keywords

3 [5 (PYRIDIN 3 YL) 2H TETRAZOL 2 YL]BENZONITRILE; 3,3' (2H TETRAZOLE 2,5 DIYL)DIPYRIDINE; 3,5 DI(PYRIDIN 3 YL) 1,2,4 OXADIAZOLE; 3[3 (PYRIDIN 3 YL) 1,2,4 OXADIAZOL 5 YL]BENZONITRILE DERIVATIVE; BENZONITRILE; NICOTINIC AGENT; NICOTINIC RECEPTOR ALPHA4BETA2; NICOTINIC RECEPTOR ALPHA4BETA2ALPHA5; NS 9283; UNCLASSIFIED DRUG; NICOTINIC RECEPTOR;

ALLOSTERISM; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; BINDING SITE; CONFORMATION; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; IN VITRO STUDY; POLYMERIZATION; RECEPTOR DOWN REGULATION; SMOKING CESSATION; SUZUKI REACTION; TOBACCO DEPENDENCE;

POSITIVE ALLOSTERIC MODULATORS; SUBSTITUTED HETEROAROMATICS; Α4Β2Α5;

ALLOSTERIC REGULATION; ANIMALS; HEK293 CELLS; HUMANS; MICE; NICOTINIC AGONISTS; NICOTINIC ANTAGONISTS; OXADIAZOLES; PYRIDINES; RECEPTORS, NICOTINIC; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84891849791     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.11.049     Document Type: Article

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