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Volumn 14, Issue 24, 2004, Pages 6045-6048

Development of an efficient and selective radioligand for bradykinin B 1 receptor occupancy studies

Author keywords

Antagonist; Bradykinin B 1 receptor; Ex vivo; Radioligand

Indexed keywords

BRADYKININ B1 RECEPTOR; BRADYKININ B1 RECEPTOR ANTAGONIST; DIHYDROQUINOLINE DERIVATIVE; RADIOLIGAND; SULFUR 35;

EID: 8844253298     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.09.074     Document Type: Article
Times cited : (21)

References (23)
  • 4
    • 0033866867 scopus 로고    scopus 로고
    • Bradykinin antagonists: New opportunities
    • M.G. Bock, and J. Longmore Bradykinin antagonists: new opportunities Curr. Opin. Chem. Biol. 4 2000 401 406
    • (2000) Curr. Opin. Chem. Biol. , vol.4 , pp. 401-406
    • Bock, M.G.1    Longmore, J.2
  • 15
    • 8844274537 scopus 로고    scopus 로고
    • note
    • 35S] into the requisite starting material were unavailable
  • 16
    • 8844282311 scopus 로고    scopus 로고
    • For the assay protocol, see Ref.5a
    • For the assay protocol, see Ref.5a
  • 17
    • 8844241179 scopus 로고    scopus 로고
    • note
    • 35S (∼87 days)
  • 18
    • 8844254403 scopus 로고    scopus 로고
    • Panlabs (MDS Pharma Services, Bothell, WA)
    • Panlabs (MDS Pharma Services, Bothell, WA)
  • 21
    • 8844265759 scopus 로고    scopus 로고
    • note
    • 1 Ki: 0.02 nM (human), 0.05 nM (rabbit), 0.5 nM (dog), 34.0 nM (rat), and 0.02 (rhesus monkey)
  • 23
    • 8844241938 scopus 로고    scopus 로고
    • note
    • 1 receptor but relatively low specific activity (75 Ci/μmol), were also tested in the same assay format. Both required long incubation times (leading to dissociation artifacts) and high tissue concentrations (association artifacts) and could not be used for the development of a reliable assay


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.