Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a 'magic methyl' giving a 35-fold improvement in binding

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 15, 2011, Pages 4608-4611

  Lunn, Graham ^a   Banks, Bernard J ^a   Crook, Robert ^a   Feeder, Neil ^a   Pettman, Alan ^a   Sabnis, Yogesh ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Opioid ligand antagonist; Opiate; Opioid; Pruritis; Rotational energy barrier

Indexed keywords

3 AZABICYCLO[3.1.0]HEXANE; HEXANE; LIGAND; MU OPIATE RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFICACY; DRUG SYNTHESIS; GUINEA PIG; IN VIVO STUDY; MOUSE; NONHUMAN; PRURITUS;

ADMINISTRATION, ORAL; ANIMALS; AZABICYCLO COMPOUNDS; CHO CELLS; CRICETINAE; CRICETULUS; DOGS; DRUG EVALUATION, PRECLINICAL; HEXANES; HUMANS; LIGANDS; PROTEIN BINDING; PRURITUS; RATS; RECEPTORS, OPIOID, MU; SULFONAMIDES;

EID: 79960375048     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.05.132     Document Type: Article

References (12)

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6. Manuscript in preparation.
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8. i determined from [3H]DAMGO filter binding assay.
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