Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 19, 2003, Pages 3247-3252

  Chen, Zhengming ^a   Miller, Wendy S ^a   Shan, Shen ^a   Valenzano, Kenneth J ^a  

^a PURDUE PHARMA L P   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

LIGAND; MU OPIATE RECEPTOR AGONIST; NOCICEPTIN RECEPTOR; NOCICEPTIN RECEPTOR AGONIST; NOCICEPTIN RECEPTOR ANTAGONIST; PIPERIDINE;

ARTICLE; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG TARGETING; MEDICAL LITERATURE; PHARMACOPHORE;

EID: 0041829500     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00665-6     Document Type: Article

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20. Values are means of three experiments. Human μ, κ and δ opioid receptor dose displacement binding assays were conducted according to the product inserts (Perkine Elmer Life Sciences). A compound was considered to be a full N/OFQ agonist when its ability to stimulate GTPγS binding was >75% in comparison to N/OFQ. An N/OFQ antagonist stimulated GTPγS binding with efficiency <25% in comparison to N/OFQ.