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Volumn 49, Issue 7, 2006, Pages 2339-2352

Screening for cardiovascular safety: A structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists

Author keywords

[No Author keywords available]

Indexed keywords

CHROMONE DERIVATIVE; INDAZOLE DERIVATIVE; MELANIN CONCENTRATING HORMONE; MELANIN CONCENTRATING HORMONE RECEPTOR 1 BLOCKING AGENT; N [1 (1,3 BENZODIOXOL 5 YLMETHYL)PIPERIDIN 4 YL] 6,7 DICHLORO 4 OXO 4H CHROMENE 2 CARBOXAMIDE; N [1 (1,3 BENZODIOXOL 5 YLMETHYL)PIPERIDIN 4 YL] 7 METHOXY 4 OXO 4H CHROMENE 2 CARBOXAMIDE; RECEPTOR BLOCKING AGENT; THIOBUTABARBITAL; UNCLASSIFIED DRUG;

EID: 33645693576     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0512286     Document Type: Article
Times cited : (37)

References (24)
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    • Compounds were tested for % inhibition @ 10 μM in a standard panel of 78 receptors and ion channels offered from CEREP (www.cerep.com).
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    • note
    • Screening of 130 MCHr1 antagonists for hERG blockade using cell-based dofetilide binding assays showed no correlation between hERG blockade and hemodynamic effects in vivo.
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    • note
    • For studies in anesthetized dogs, the minimum pressure limit tolerated was 50% reduction in the MAP relative to vehicle treated animals. For studies in inactin-anesthetized rats, the minimum pressure limit tolerated was 70 mmHg. This minimum pressure level was implemented to ensure a functional cardiovascular system for the collection of the end-of-study blood sample used for drug plasma level determinations.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.