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Volumn 17, Issue 19, 2007, Pages 5349-5352

Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1

Author keywords

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

Indexed keywords

6 [4 (2 BENZYLAMINOETHYL)PHENOXY]NICOTINAMIDE; AMIDE; DELTA OPIATE RECEPTOR; ETHER DERIVATIVE; KAPPA OPIATE RECEPTOR; LY 255582; MU OPIATE RECEPTOR; NALTREXONE; OPIATE ANTAGONIST; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

EID: 34548596549     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.08.008     Document Type: Article
Times cited : (10)

References (13)
  • 11
    • 2942703907 scopus 로고    scopus 로고
    • 3H]-bremazocine binding) opioid receptors expressed in CHO cells under high sodium conditions (n ≥ 2). 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 (n ≥ 2). 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
  • 12
    • 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 (n ≥ 2). 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: see
    • 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 (n ≥ 2). 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: see. Rodgers G., Hubert C., McKinzie J., Suter T., Statnick M., Emmerson P., and Stancato L. Assay Drug Dev. Technol. 1 (2003) 627
    • (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
  • 13
    • 34548597692 scopus 로고    scopus 로고
    • note
    • 5-Fluoro-2-pyridinecarboxamide was prepared from 2-amino-5-fluoropyridine via Sandmeyer reaction followed by ester/amide formation or direct amidation of 2-bromo-5-fluoropyridine, the Sandmeyer product, with CuCN in DMF.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.