메뉴 건너뛰기




Volumn 21, Issue 12, 2011, Pages 3616-3621

Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids

Author keywords

Asthma; CRTh2; DP2; Inflammation; Phenoxyacetic acid; Prostaglandin

Indexed keywords

CALCIUM ION; CHEMOATTRACTANT RECEPTOR HOMOLOGOUS EXPRESSED ON TH2 LYMPHOCYTE AGONIST; CHEMOATTRACTANT RECEPTOR HOMOLOGOUS EXPRESSED ON TH2 LYMPHOCYTE ANTAGONIST; IMMUNOLOGIC AGENT; PHENOXYACETIC ACID DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79957851179     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.101     Document Type: Article
Times cited : (8)

References (23)
  • 18
    • 79957851876 scopus 로고    scopus 로고
    • note
    • 2 or test compound) and 80 μL of purified granulocytes. After incubation at 37 °C for 15 min, the cells were fixed and incubated in the dark for a further 15 min at room temperature. Remaining red blood cells were lysed using a hypotonic shock. The level of CD11b expression was determined by flow cytometry using lack of CD16 expression to distinguish eosinophils from neutrophils.
  • 20
    • 42149195403 scopus 로고    scopus 로고
    • At other biological targets, partial agonists or antagonists have had consistently higher lipophilicity than would be expected for an agonist of comparable affinity. See for example
    • At other biological targets, partial agonists or antagonists have had consistently higher lipophilicity than would be expected for an agonist of comparable affinity. See for example: Parker, M. A.; Kurrasch, D. M.; Nichols, D. E. Bioorg. Med. Chem. 2008, 16, 4661.
    • (2008) Bioorg. Med. Chem. , vol.16 , pp. 4661
    • Parker, M.A.1    Kurrasch, D.M.2    Nichols, D.E.3
  • 21
    • 71049187691 scopus 로고    scopus 로고
    • Dilute bovine serum albumin was used as part of the buffer medium for cost reasons. This is relatively commonplace see for example At these dilute serum albumin concentrations and with relatively free compounds this approximation is expected to have minimal impact. However, significant differences between protein shifts across species can occur, and so independent plasma protein binding measurements in 100% plasma were undertaken for 34 across multiple species. Relatively consistent values were obtained: human 4.6, rat 5.6, dog 3.0, cyno 2.6 (% free)
    • Dilute bovine serum albumin was used as part of the buffer medium for cost reasons. This is relatively commonplace (see for example Liu, J.; Fu, Z.; Wang, Y.; Schmitt, M.; Huang, A.; Marshall, D.; Tonn, G.; Seitz, L.; Sullivan, T.; Tang, H. L.; Collins, T.; Medina, J. Bioorg. Med. Chem. Lett. 2009, 19, 6419. ). At these dilute serum albumin concentrations and with relatively free compounds this approximation is expected to have minimal impact. However, significant differences between protein shifts across species can occur, and so independent plasma protein binding measurements in 100% plasma were undertaken for 34 across multiple species. Relatively consistent values were obtained: human 4.6, rat 5.6, dog 3.0, cyno 2.6 (% free)..
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 6419
    • Liu, J.1    Fu, Z.2    Wang, Y.3    Schmitt, M.4    Huang, A.5    Marshall, D.6    Tonn, G.7    Seitz, L.8    Sullivan, T.9    Tang, H.L.10    Collins, T.11    Medina, J.12
  • 22
    • 79957858840 scopus 로고    scopus 로고
    • note
    • 3N requires C, 52.7; H, 4.5; N, 1.5; S, 7.8%. Found: C, 52.4; H, 4.5; N, 1.2; S, 7.8%.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.