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Volumn 17, Issue 24, 2007, Pages 6841-6846

Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2

Author keywords

Carboxamido biaryl ethers; Obesity; Opioid receptor antagonists (OpRAs)

Indexed keywords

6 (2,3,4,5 TETRAHYDRO 1H BENZO[C]AZEPIN 7 YLOXY)NICOTAMIDE; 6 BICYCLOOXYNICOTINAMIDE DERIVATIVE; AMIDE; DELTA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR; LY 255582; MORPHINE; MU OPIATE RECEPTOR; NALTREXONE; NICOTINAMIDE; OPIATE ANTAGONIST; UNCLASSIFIED DRUG;

EID: 35848945462     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.10.025     Document Type: Article
Times cited : (14)

References (12)
  • 1
    • 2942685667 scopus 로고    scopus 로고
    • A brief summary of the epidemic of obesity and its health and economic impact, see and references cited therein
    • A brief summary of the epidemic of obesity and its health and economic impact, see. Stein C.J., and Colditz G.A. J. Clin. Endocrinol. Metab. 89 (2004) 2522 and references cited therein
    • (2004) J. Clin. Endocrinol. Metab. , vol.89 , pp. 2522
    • Stein, C.J.1    Colditz, G.A.2
  • 8
    • 2942703907 scopus 로고    scopus 로고
    • 3H]-bremazocine binding) opioid receptors expressed in CHO cells under high sodium conditions. Under low sodium binding conditions the affinity was reduced at the receptor subtypes, consistent with findings on the prototype Lilly 4-phenylpiperidine opioid antagonist series: see
    • 3H]-bremazocine binding) opioid receptors expressed in CHO cells under high sodium conditions. Under low sodium binding conditions the affinity was reduced at the receptor subtypes, consistent with findings on the prototype Lilly 4-phenylpiperidine opioid antagonist series: see. Emmerson P.J., McKinzie J.H., Surface P., Suter T.M., Mitch C.H., and Statnick M.A. Eur. J. Pharmacol. 494 (2004) 121
    • (2004) Eur. J. Pharmacol. , vol.494 , pp. 121
    • Emmerson, P.J.1    McKinzie, J.H.2    Surface, P.3    Suter, T.M.4    Mitch, C.H.5    Statnick, M.A.6
  • 9
    • 2542486572 scopus 로고    scopus 로고
    • In vitro functional assay, inhibiting agonist stimulated G-protein activation (measured using GTPγS binding) in CHO membranes expressing the cloned human mu, kappa, and delta receptors. In the present study, opioid ligand binding and GTPγS functional assays were converted to a homogeneous SPA permitting the development of simpler assays with dramatically increased throughput. Optimization in the presence of sodium chloride was designed to bias these assays toward the detection of opioid antagonists. Kb values for compounds with modest binding affinities were not determined. See for the assay development method
    • In vitro functional assay, inhibiting agonist stimulated G-protein activation (measured using GTPγS binding) in CHO membranes expressing the cloned human mu, kappa, and delta receptors. In the present study, opioid ligand binding and GTPγS functional assays were converted to a homogeneous SPA permitting the development of simpler assays with dramatically increased throughput. Optimization in the presence of sodium chloride was designed to bias these assays toward the detection of opioid antagonists. Kb values for compounds with modest binding affinities were not determined. See. Rodgers G., Hubert C., McKinzie J., Suter T., Statnick M., Emmerson P., and Stancato L. Assay Drug Dev. Technol. 1 (2003) 627 for the assay development method
    • (2003) Assay Drug Dev. Technol. , vol.1 , pp. 627
    • Rodgers, G.1    Hubert, C.2    McKinzie, J.3    Suter, T.4    Statnick, M.5    Emmerson, P.6    Stancato, L.7
  • 10
    • 35848946312 scopus 로고    scopus 로고
    • note
    • 1H NMR, MS, and one of the following methods for purity verification: HRMS, EA or HPLC. See WO2004026305 (A1) for details of compound preparation.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.