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Volumn 19, Issue 21, 2009, Pages 6144-6147

Optimising metabolic stability in lipophilic chemical space: The identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist

Author keywords

Antagonist; Corticotrophin releasing factor 1; G protein coupled receptor; Metabolic stability

Indexed keywords

ANTALARMIN; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1;

EID: 71749088604     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.09.016     Document Type: Article
Times cited : (16)

References (24)
  • 21
    • 71749105948 scopus 로고    scopus 로고
    • note
    • 50 for the agonist dose-response curve which was determined on the same day.
  • 22
    • 71749120222 scopus 로고    scopus 로고
    • note
    • int figures of >70 are likely to translate to rapid in vivo clearance.
  • 23
    • 71749112661 scopus 로고    scopus 로고
    • note
    • The difference between human and rat microsomal stability in this case is surprising. From unpublished in-house experience in these assays rat liver microsomes generally show higher turn-over across chemotypes than human liver microsomes. The high turnover in rat microsomes for this compound suggests a possible atypical species difference in Cyp mediated metabolism for compound 7.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.