| Peripheral injections of melanin-concentrating hormone receptor 1 antagonist S38151 decrease food intake and body weight in rodent obesity models. | |
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MedLine Citation:
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PMID: 23267345 Owner: NLM Status: PubMed-not-MEDLINE |
Abstract/OtherAbstract:
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The compound S38151 is a nanomolar antagonist that acts at the melanin-concentrating hormone receptor 1 (MCH(1)). S38151 is more stable than its purely peptide counterpart, essentially because of the blockade of its N-terminus. Therefore, its action on various models of obesity was studied. Acute intra-cerebroventricular (i.c.v.) administration of S38151 in wild-type rats counteracted the effect of the stable precursor of melanin-concentrating hormone (MCH), NEI-MCH, in a dose-dependent manner (from 0.5 to 50 nmol/kg). In genetically obese Zucker fa/fa rats, daily i.c.v. administration of S38151 induced dose-dependent (5, 10, and 20 nmol/kg) inhibition of food intake, water intake, and body weight gain, as well as increased motility (maximal effect observed at 20 nmol/kg). In Zucker fa/fa rats, intraperitoneal injection of S38151 (30 mg/kg) induced complete inhibition of food consumption within 1 h. Daily intraperitoneal injection of S38151 (10 and 30 mg/kg) into genetically obese ob/ob mice or diet-induced obese mice is able to limit body weight gain. Furthermore, S38151 administration (10 and 30 mg/kg) does not affect food intake, water intake, or body weight gain in MCHR1-deleted mice, demonstrating that its effects are linked to its interaction with MCH(1). These results validate MCH(1) as a target of interest in obesity. S38151 cannot progress to the clinical phase because it is still too poorly stable in vivo. |
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Authors:
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Odile Della-Zuana; Valérie Audinot; Viviane Levenez; Alain Ktorza; Françoise Presse; Jean-Louis Nahon; Jean A Boutin |
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Publication Detail:
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Type: Journal Article Date: 2012-12-21 |
Journal Detail:
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Title: Frontiers in endocrinology Volume: 3 ISSN: 1664-2392 ISO Abbreviation: Front Endocrinol (Lausanne) Publication Date: 2012 |
Date Detail:
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Created Date: 2012-12-25 Completed Date: 2012-12-26 Revised Date: 2013-02-20 |
Medline Journal Info:
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Nlm Unique ID: 101555782 Medline TA: Front Endocrinol (Lausanne) Country: Switzerland |
Other Details:
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Languages: eng Pagination: 160 Citation Subset: - |
Affiliation:
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Maladies Métaboliques, Institut de Recherches SERVIER Suresnes, France. |
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