Unichiral 2-(2′-pyrrolidinyl)-1,4-benzodioxanes: The 2 R,2′ S diastereomer of the N -methyl-7-hydroxy analogue is a potent α4β2- and α6β2-nicotinic acetylcholine receptor partial agonist

Journal of Medicinal Chemistry

Volumn 54, Issue 21, 2011, Pages 7588-7601

  Bolchi, Cristiano ^a   Gotti, Cecilia ^b   Binda, Matteo ^a   Fumagalli, Laura ^a   Pucci, Luca ^b   Pistillo, Francesco ^c   Vistoli, Giulio ^a   Valoti, Ermanno ^a   Pallavicini, Marco ^a  

^a UNIVERSITY OF MILAN   (Italy)

^b CNR   (Italy)

^c IRCCS NEUROMED   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1' METHYL 2' PYRROLIDINYL) 7 ACETYL 1,4 BENZODIOXANE; 2 (1' METHYL 2' PYRROLIDINYL) 7 BROMO 1,4 BENZODIOXANE; 2 (1' METHYL 2' PYRROLIDINYL) 7 HYDROXY 1,4 BENZODIOXANE; 2 (1' METHYL 2' PYRROLIDINYL) 7 ISOPROPOXY 1,4 BENZODIOXANE; 2 (1' METHYL 2' PYRROLIDINYL) 7 METHOXY 1,4 BENZODIOXANE; 2 (1' METHYL 2' PYRROLIDINYL) 7 METHYL 1,4 BENZODIOXANE; BENZODIOXAN DERIVATIVE; CHOLINERGIC RECEPTOR STIMULATING AGENT; LIGAND; NICOTINE; NICOTINIC RECEPTOR; NICOTINIC RECEPTOR ALPHA4BETA2; NICOTINIC RECEPTOR ALPHA6BETA2; PARTIAL AGONIST; PYRROLIDINE DERIVATIVE; UNCLASSIFIED DRUG; VARENICLINE;

ANIMAL TISSUE; ARTICLE; CHIRALITY; CONTROLLED STUDY; DEMETHYLATION; DIASTEREOISOMER; DRUG BINDING SITE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; MALE; MOLECULAR DOCKING; NONHUMAN; RAT; RECEPTOR AFFINITY; SMOKING CESSATION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING SITES; CEREBRAL CORTEX; CORPUS STRIATUM; DIOXANES; DOPAMINE; DRUG PARTIAL AGONISM; HEK293 CELLS; HUMANS; MALE; MODELS, MOLECULAR; NICOTINIC AGONISTS; PYRROLIDINES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NICOTINIC; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80455162598     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200937t     Document Type: Article

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