Novel N-substituted benzimidazolones as potent, selective, CNS-penetrant, and orally active M1 mAChR agonists

ACS Medicinal Chemistry Letters

Volumn 1, Issue 6, 2010, Pages 244-248

  Budzik, Brian ^a   Garzya, Vincenzo ^a   Shi, Dongchuan ^a   Walker, Graham ^a   Woolley Roberts, Marie ^a   Pardoe, Joanne ^a   Lucas, Adam ^a   Tehan, Ben ^a   Rivero, Ralph A ^a   Langmead, Christopher J ^a   Watson, Jeannette ^a   Wu, Zining ^a   Forbes, Ian T ^a   Jin, Jian ^a,b  

^a GLAXOSMITHKLINE   (United States)

^b University of North Carolina   (United States)

Author keywords

1 (N substituted piperidin 4 yl)benzimidazolones; benzimidazolones; CNS penetrant and orally active M1 mAChR agonists; M1 mAChR; M1 muscarinic acetylcholine receptor; subtype selective

Indexed keywords

1 (PIPERIDIN 4 YL)BENZIMIDAZOLONE; BENZIMIDAZOLE DERIVATIVE; MUSCARINIC M1 RECEPTOR AGONIST; UNCLASSIFIED DRUG;

AMNESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COGNITION; CONTROLLED STUDY; DOSE RESPONSE; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG PENETRATION; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALIA;

EID: 77956510685     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml100105x     Document Type: Article

References (22)

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21. The biological assay results in this paper are a mean of at least 2 determinations with standard deviation of <±0.3 unless otherwise noted.
22. Drug concentrations in hepatic porter vein and cardiac blood samples at various time points were measured and used to estimate in vivo clearance and oral bioavailability of test compounds.