Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 2, 2010, Pages 453-457

  Receveur, Jean Marie ^a   Murray, Anthony ^a   Linget, Jean Michel ^a   Nørregaard, Pia K ^a   Cooper, Martin ^a   Bjurling, Emelie ^a   Nielsen, Peter Aadal ^a   Högberg, Thomas ^a  

^a 7TM Pharma A S   (Denmark)

Author keywords

Blood brain barrier; CB1 antagonists; CB1 inverse agonists; CNS; DIO model; Obesity; Plasma brain ratio

Indexed keywords

4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; 4 CYANOMETHYLPYRAZOLE 3 CARBOXAMIDE; CANNABINOID 1 RECEPTOR; CANNABINOID 1 RECEPTOR ANTAGONIST; NITRILE; RIMONABANT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SOLUBILITY; LIPOPHILICITY; MOUSE; NONHUMAN; OBESITY; RAT; STRUCTURE ACTIVITY RELATION; SURFACE PROPERTY; WEIGHT REDUCTION;

AMIDES; ANIMALS; ANTI-OBESITY AGENTS; BLOOD-BRAIN BARRIER; BODY WEIGHT; DRUG INVERSE AGONISM; MICE; OBESITY; PIPERIDINES; PROTEIN BINDING; PYRAZOLES; RATS; RECEPTOR, CANNABINOID, CB1; STRUCTURE-ACTIVITY RELATIONSHIP;

MUS;

EID: 72249112327     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.003     Document Type: Article

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