Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 6, 2011, Pages 1748-1753

  Kiyoi, Takao ^a   Adam, Julia M ^a   Clark, John K ^a   Davies, Keneth ^a   Easson, Anna Marie ^a   Edwards, Darren ^a   Feilden, Helen ^a   Fields, Ruth ^a   Francis, Stuart ^a   Jeremiah, Fiona ^a   McArthur, Duncan ^a   Morrison, Angus J ^a   Prosser, Alan ^a   Ratcliffe, Paul D ^a   Schulz, Jurgen ^a   Wishart, Grant ^a   Baker, James ^a   Campbell, Robert ^a   Cottney, Jean E ^a   Deehan, Maureen ^a   Epemolu, Ola ^a   Evans, Louise ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cannabinoid; CB1 receptor agonist; Oral bioavailability

Indexed keywords

2,3 DIHYDRO 5 METHYL 3 (MORPHOLINOMETHYL) 6 (1 NAPHTHOYL)PYRROLO[1,2,3 DE][1,4]BENZOXAZINE; 3 (1,2,4 OXADIAZOL 3 YL)INDOLE DERIVATIVE; 3 (1,2,4 THIADIAZOL 3 YL)INDOLE DERIVATIVE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; CANNABINOID 1 RECEPTOR; CANNABINOID 1 RECEPTOR AGONIST; CANNABINOID 2 RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINOCICEPTION; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG POTENCY; DRUG STABILITY; DRUG SYNTHESIS; HYPERALGESIA; MAXIMUM PLASMA CONCENTRATION; MICROSOME; NEUROPATHIC PAIN; NONHUMAN; RAT; TAIL FLICK TEST; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; DRUG DISCOVERY; HETEROCYCLIC COMPOUNDS; RATS; RECEPTOR, CANNABINOID, CB1;

EID: 79952360671     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.082     Document Type: Article

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