메뉴 건너뛰기




Volumn 19, Issue 13, 2009, Pages 3568-3572

Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists

Author keywords

GPCR; MCHIR antagonist; Melanin concentrating hormone; Obesity

Indexed keywords

2 AMINOBENZIMIDAZOLE DERIVATIVE; BENZIMIDAZOLE DERIVATIVE; MELANIN CONCENTRATING HORMONE RECEPTOR 1; MELANIN CONCENTRATING HORMONE RECEPTOR 1 ANTAGONIST; UNCLASSIFIED DRUG;

EID: 66349112548     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.04.147     Document Type: Article
Times cited : (9)

References (26)
  • 14
    • 34547476684 scopus 로고    scopus 로고
    • General reviews on MCH1R antagonists:
    • General reviews on MCH1R antagonists:. Luithin D.R. Life Sci. 81 (2007) 423
    • (2007) Life Sci. , vol.81 , pp. 423
    • Luithin, D.R.1
  • 17
    • 66349131650 scopus 로고    scopus 로고
    • DeVita, R. J.; Chang, L.; Chaung, D.; Hoang, M.; Jiang, J.; Lin, P.; Sailer, A. W.; Young, J. R. WO03045313, 2003.
    • DeVita, R. J.; Chang, L.; Chaung, D.; Hoang, M.; Jiang, J.; Lin, P.; Sailer, A. W.; Young, J. R. WO03045313, 2003.
  • 21
    • 66349124194 scopus 로고    scopus 로고
    • Moriya, M.; Kanatani, A.; Iwaasa, H.; Ishihara, A.; Fukami, T. WO2004011440, 2004.
    • Moriya, M.; Kanatani, A.; Iwaasa, H.; Ishihara, A.; Fukami, T. WO2004011440, 2004.
  • 22
    • 66349107978 scopus 로고    scopus 로고
    • note
    • 2, 2 mM EDTA, 50 μg/mL bacitracin, 0.2% BSA, pH 7.4) at room temperature for 2 h. The membranes were filtrated onto GF/C filter plates and dried. The radioactivity was counted using a microplate scintillation counter (TopCount, PerkinElmer). Non-specific binding was determined by including 1 μM unlabeled MCH in the binding reaction.
  • 23
    • 66349085360 scopus 로고    scopus 로고
    • note
    • 2+ in response to MCH. The cells were treated with the test compounds for 5 min before addition of MCH.
  • 24
    • 66349084462 scopus 로고    scopus 로고
    • a values were calculated by the SPARC on-line calculator (http://ibmlc2.chem.uga.edu/sparc/).
    • a values were calculated by the SPARC on-line calculator (http://ibmlc2.chem.uga.edu/sparc/).
  • 26
    • 66349110880 scopus 로고    scopus 로고
    • note
    • A 26-gauge guide cannula was stereotaxically implanted into the third ventricle of male SD rats as described previously (Endocrinology 146:3080-3086, 2005). After at least 1 week recovery, rats were fed a high fat diet for ∼3 h and compound 25 (10 or 30 mg/kg) or vehicle was orally administered. One hour after the drug administration, MCH (5 μg/μL/head, dissolved in artificial cerebrospinal fluid) was injected ICV and food intake for 2 h was measured. MCH injection was performed 1 h before the onset of the dark cycle.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.