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Volumn 19, Issue 21, 2009, Pages 6166-6171

Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: In vitro profiling and in vivo evaluation

Author keywords

ATC0175; CNS; Food intake; GPCRs; MCH R1; Obesity; PK PD

Indexed keywords

ATC 0175; MELANIN CONCENTRATING HORMONE RECEPTOR 1; PYRIMIDINE ANTAGONIST; SIBUTRAMINE; UNCLASSIFIED DRUG;

EID: 71749107372     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.09.003     Document Type: Article
Times cited : (2)

References (27)
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    • Tran, T.-A; Beeley, N. R. A.; Thomsen, W.; Lin, I.; Sekiguchi, Y. Discovery of MCH-R1 antagonists from GPCR-directed libraries. 228th ACS National Meeting, Philadelphia, PA, USA, August 22-26, 2004, MEDI-051.
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    • Bjenning, C.; Thomsen, W.; Whelan, K.; Creehan, K.; Gonzalez, L.; Al-Shamma, H.; Tran, T.; Semple, G.; Funakoshi, T.; Nishiguchi, M.; Shimazaki, T.; Kanuma, K.; Sekiguchi, Y.; Chaki. S. Novel and potent non-peptide antagonists of Melanin-concentrating hormone receptor-1: ATC0065 and ATC0175 reduce appetite and bodyweight in high-fat diet-fed male rats. Society for Neuroscience Meeting, San Diego CA, Oct 22-27, 2004, Abstr. 629.8.
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    • note
    • 50 of 3.7 nM. Active compounds were identified by their ability to inhibit this Gαq-dependent response, in a concentration-dependent manner.
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    • note
    • The study (RenaSci Consultancy Ltd, BioCity Nottingham, Pennyfoot Street, Nottingham, UK) investigated the effect of chronic administration of 4x (and withdrawal) on body weight and food and water intake in female Wistar rats made obese by exposure to a simplified cafeteria diet (high-fat chow, chocolate and peanut granules) for 12 weeks, that is, dietary-induced obesity (DIO). Following the induction of obesity, rats were given deionised water orally for a 7 day baseline period and then dosed orally once daily with vehicle, one of four doses of 4x (1, 5, 10 and 15 mg/kg) or sibutramine (6 mg/kg PO) for up to 28 days.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.