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Volumn 18, Issue 20, 2008, Pages 5601-5604

Small, non-peptide C5a receptor antagonists: Part 1

Author keywords

Antagonist; C5a receptor; Complement; Inflammation

Indexed keywords

COMPLEMENT COMPONENT 5A RECEPTOR ANTAGONIST; COMPLEMENT COMPONENT C5A RECEPTOR; CP 289503; CP 447697; UNCLASSIFIED DRUG;

EID: 53349163281     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.106     Document Type: Article
Times cited : (14)

References (24)
  • 6
    • 53349102868 scopus 로고    scopus 로고
    • Merck and Co., US Patent 5614370, 1997.
    • Merck and Co., US Patent 5614370, 1997.
  • 13
    • 53349164062 scopus 로고    scopus 로고
    • Welfide Corp. WO Patent 0222556, 2002.
    • Welfide Corp. WO Patent 0222556, 2002.
  • 14
    • 53349167192 scopus 로고    scopus 로고
    • Neurogen Corp., WO Patent 0251414, 2002; WO Patent 082829, 2003.
    • Neurogen Corp., WO Patent 0251414, 2002; WO Patent 082829, 2003.
  • 17
    • 53349100672 scopus 로고    scopus 로고
    • Chemocentryx Inc. WO Patent 07051062, 2007.
    • Chemocentryx Inc. WO Patent 07051062, 2007.
  • 18
    • 53349096370 scopus 로고    scopus 로고
    • Jerini AG, WO06128670, 2006.
    • Jerini AG, WO06128670, 2006.
  • 19
    • 53349100674 scopus 로고    scopus 로고
    • note
    • Details of this work will be reported elsewhere.
  • 22
    • 53349117374 scopus 로고    scopus 로고
    • note
    • Hydride reduction of cyclohexanones forms predominantly trans alcohols, while larger nucleophiles favour cis. Isomers were separable by chromatography.
  • 23
    • 53349178414 scopus 로고    scopus 로고
    • note
    • 125I-labelled r-hC5a (NEN) to measure bound radioligand.
  • 24
    • 53349167075 scopus 로고    scopus 로고
    • note
    • Neutrophil degranulation was measured in cytochalasin B-primed isolated human neutrophils at 37 °C by quantification of released elastase by cleavage of the chromogenic MeOSuc-Ala-Ala-Pro-Val-pNA. C5aR antagonists were pre-incubated with neutrophils for 5 min at 37 °C prior to a 1 nM r-hC5a (Sigma) challenge.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.