Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile

Journal of Medicinal Chemistry

Volumn 55, Issue 2, 2012, Pages 717-724

  Zhang, Hankun ^a   Tückmantel, Werner ^c   Eaton, J Brek ^b   Yuen, Po Wai ^c   Yu, Li Fang ^a   Bajjuri, Krishna Mohan ^a   Fedolak, Allison ^c   Wang, Daguang ^c   Ghavami, Afshin ^c   Caldarone, Barbara ^c   Paterson, Neil E ^c   Lowe, David A ^c   Brunner, Daniela ^c   Lukas, Ronald J ^b   Kozikowski, Alan P ^a  

^a UNIVERSITY OF ILLINOIS AT CHICAGO   (United States)

^b BARROW NEUROLOGICAL INSTITUTE   (United States)

^c PSYCHOGENICS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [(2 AZETIDINYL)METHOXY] 5 [2 (2 HYDROXYETHYL) CYCLOPROPYL]PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 (2 HYDROXYETHYL)CYCLOPROPYL]PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 (2 METHOXYETHYL) CYCLOPROPYL]PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 [2 (1 PYRROLIDINYLCARBONYLOXY)ETHYL]CYCLOPROPYL] PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 [2 (N CYCLOPROPYLCARBAMOYLOXY)ETHYL]CYCLOPROPYL] PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 [2 (N METHYLCARBAMOYLOXY)ETHYL]CYCLOPROPYL]PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 [2 (N PHENYLCARBAMOYLOXY)ETHYL]CYCLOPROPYL]PYRIDINE TRIFLUOROACETATE; 3 [(2 AZETIDINYL)METHOXY] 5 [2 [2 (N,N DIMETHYLCARBAMOYLOXY)ETHYL]CYCLOPROPYL] PYRIDINE TRIFLUOROACETATE; ANTIDEPRESSANT AGENT; CYCLOPROPANE DERIVATIVE; NEUROTRANSMITTER RECEPTOR; NICOTINIC RECEPTOR ALPHA4BETA2; PARTIAL AGONIST; SERTRALINE; TRIFLUOROACETIC ACID; UNCLASSIFIED DRUG; VARENICLINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIDEPRESSANT ACTIVITY; ARTICLE; BEHAVIOR; BINDING AFFINITY; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; EX VIVO STUDY; FORCED SWIMMING TEST; HUMAN; HUMAN CELL; IMMOBILIZATION; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MALE; MINIMUM INHIBITORY CONCENTRATION; MOUSE; NONHUMAN; RECEPTOR OCCUPANCY; THALAMUS;

ANIMALS; ANTIDEPRESSIVE AGENTS; BEHAVIOR, ANIMAL; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DRUG PARTIAL AGONISM; FEMALE; HUMANS; LIGANDS; MICE; MICE, INBRED BALB C; MOLECULAR CONFORMATION; NICOTINIC AGONISTS; RADIOLIGAND ASSAY; RATS; RECEPTORS, NICOTINIC; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84863012458     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201157c     Document Type: Article

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