Compounds > enkephalin--ala(2)-mephe(4)-gly(5)-

enkephalin--ala(2)-mephe(4)-gly(5)- and 8-carboxamidocyclazocine

enkephalin--ala(2)-mephe(4)-gly(5)- has been researched along with 8-carboxamidocyclazocine* in 2 studies

Other Studies

2 other study(ies) available for enkephalin--ala(2)-mephe(4)-gly(5)- and 8-carboxamidocyclazocine

Article	Year
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine. Bioorganic & medicinal chemistry, 2008, May-15, Volume: 16, Issue:10 A series of 7,8- and 8,9-fused pyrimidinone, aminopyrimidine and pyridone derivatives of 8-carboxamidocyclazocine (8-CAC) have been prepared and evaluated in opioid receptor binding assays. Targets were designed to corroborate a pharmacophore hypothesis regarding the bioactive conformation of the carboxamide of 8-CAC. In addition to the results from this study strongly supporting this pharmacophore hypothesis, a number of novel compounds with high affinity to opioid receptors have been identified. Topics: Animals; Azocines; Binding, Competitive; CHO Cells; Cricetinae; Cricetulus; Cyclazocine; Drug Design; Molecular Conformation; Narcotic Antagonists; Receptors, Opioid; Stereoisomerism; Structure-Activity Relationship	2008
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC. Bioorganic & medicinal chemistry letters, 2007, Dec-01, Volume: 17, Issue:23 A series of aryl-containing N-monosubstituted analogues of the lead compound 8-[N-((4'-phenyl)-phenethyl)]-carboxamidocyclazocine were synthesized and evaluated to probe a putative hydrophobic binding pocket of opioid receptors. Very high binding affinity to the mu opioid receptor was achieved though the N-(2-(4'-methoxybiphenyl-4-yl)ethyl) analogue of 8-CAC. High binding affinity to mu and very high binding affinity to kappa opioid receptors was observed for the N-(3-bromophenethyl) analogue of 8-CAC. High binding affinity to all three opioid receptors were observed for the N-(2-naphthylethyl) analogue of 8-CAC. Topics: Animals; CHO Cells; Cricetinae; Cricetulus; Cyclazocine; Humans; Protein Binding; Receptors, Opioid; Structure-Activity Relationship	2007

Article

Year

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.

Bioorganic & medicinal chemistry, 2008, May-15, Volume: 16, Issue:10

A series of 7,8- and 8,9-fused pyrimidinone, aminopyrimidine and pyridone derivatives of 8-carboxamidocyclazocine (8-CAC) have been prepared and evaluated in opioid receptor binding assays. Targets were designed to corroborate a pharmacophore hypothesis regarding the bioactive conformation of the carboxamide of 8-CAC. In addition to the results from this study strongly supporting this pharmacophore hypothesis, a number of novel compounds with high affinity to opioid receptors have been identified.

Topics: Animals; Azocines; Binding, Competitive; CHO Cells; Cricetinae; Cricetulus; Cyclazocine; Drug Design; Molecular Conformation; Narcotic Antagonists; Receptors, Opioid; Stereoisomerism; Structure-Activity Relationship

2008

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.

Bioorganic & medicinal chemistry letters, 2007, Dec-01, Volume: 17, Issue:23

A series of aryl-containing N-monosubstituted analogues of the lead compound 8-[N-((4'-phenyl)-phenethyl)]-carboxamidocyclazocine were synthesized and evaluated to probe a putative hydrophobic binding pocket of opioid receptors. Very high binding affinity to the mu opioid receptor was achieved though the N-(2-(4'-methoxybiphenyl-4-yl)ethyl) analogue of 8-CAC. High binding affinity to mu and very high binding affinity to kappa opioid receptors was observed for the N-(3-bromophenethyl) analogue of 8-CAC. High binding affinity to all three opioid receptors were observed for the N-(2-naphthylethyl) analogue of 8-CAC.

Topics: Animals; CHO Cells; Cricetinae; Cricetulus; Cyclazocine; Humans; Protein Binding; Receptors, Opioid; Structure-Activity Relationship

2007