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Volumn 20, Issue 18, 2010, Pages 5443-5448

Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists

Author keywords

Benzimidazoles; MCHR1 antagonists; Melanin concentrating hormone (MCH); Obesity

Indexed keywords

AMG 076; BENZIMIDAZOLE DERIVATIVE; GW 856464; MELANIN CONCENTRATING HORMONE RECEPTOR 1 ANTAGONIST; N (6 DIMETHYLAMINOMETHYL 5,6,7,8 TETRAHYDRO 2 NAPHTHYL) 4' FLUORO 1,1' BIPHENYL 4 CARBOXAMIDE; NGD 4715; SNAP 7941; UNCLASSIFIED DRUG;

EID: 77956176750     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.07.086     Document Type: Article
Times cited : (16)

References (56)
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    • International Association for the Study of Obesity (IASO) (http://www.iaso.org ).
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    • 77956172358 scopus 로고    scopus 로고
    • 3, 400 MHz): δ 7.76 (d, J = 7.8 Hz, 1H), 7.50-7.48 (m, 2H), 7.37-7.19 (m, 7H), 7.06 (d, J = 7.8 Hz, 1H), 6.94 (d, J = 7.8 Hz, 1H), 3.30-3.27 (m, 2H), 2.81 (t, J = 7.4 Hz, 2H), 2.68 (br s, 1H), 2.61-2.54 (m, 2H), 2.39-2.35 (m, 2H), 2.16 (s, 3H), 2.04 (br s, 1H), 1.87 (br s, 3H), 1.25 (br s, 2H), 0.88-084 (m, 2H); ESMS: m/z 485.4 (M+1)
    • 3, 400 MHz): δ 7.76 (d, J = 7.8 Hz, 1H), 7.50-7.48 (m, 2H), 7.37-7.19 (m, 7H), 7.06 (d, J = 7.8 Hz, 1H), 6.94 (d, J = 7.8 Hz, 1H), 3.30-3.27 (m, 2H), 2.81 (t, J = 7.4 Hz, 2H), 2.68 (br s, 1H), 2.61-2.54 (m, 2H), 2.39-2.35 (m, 2H), 2.16 (s, 3H), 2.04 (br s, 1H), 1.87 (br s, 3H), 1.25 (br s, 2H), 0.88-084 (m, 2H); ESMS: m/z 485.4 (M+1).
  • 53
    • 77956175178 scopus 로고    scopus 로고
    • note
    • 50 for the compound was calculated by graph pad prism software using the average CPM values
  • 54
    • 77956172116 scopus 로고    scopus 로고
    • note
    • Functional response of compounds was assessed using the IP3-SPA-YSI method. Briefly, CHO-K1 cells stably expressing hMCHR1 were incubated overnight with 0.5 μCi/well of 3H-myo-inositol to generate a pool of 3H-PIP2. After aspiration of labeling medium, the cells were incubated with test compounds followed by stimulation with 80 nM of agonist (MCH peptide). The resulting pool of 3H-IPs was extracted with formic acid and the amount of 3H-IPs generated in the cells was detected using the non-derivatized yttrium silicate SPA beads.
  • 56
    • 77956177640 scopus 로고    scopus 로고
    • note
    • C57BL/6J mice were fed a high fat diet (60% calories from fat, D12492 feed) for nearly 3 months until they reached an average body weight of approximately 45 g. Animals were grouped based on initial body weight. Compounds to be tested were then administered per orally twice daily for a period of 7 days. Body weight and food intake of the animals was recorded on a daily basis during the experimental duration.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.