5-Hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity

…, A Fettes, C Freichel, S Gatti-McArthur…

Index: Pierson, Pascale David; Fettes, Alec; Freichel, Christian; Gatti-McArthur, Silvia; Hertel, Cornelia; Huwyler, Joerg; Mohr, Peter; Nakagawa, Toshito; Nettekoven, Matthias; Plancher, Jean-Marc; Raab, Susanne; Richter, Hans; Roche, Olivier; Sarmiento, Rosa Maria Rodriguez; Schmitt, Monique; Schuler, Franz; Takahashi, Tadakatsu; Taylor, Sven; Ullmer, Christoph; Wiegand, Ruby Journal of Medicinal Chemistry, 2009 , vol. 52, # 13 p. 3855 - 3868

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Citation Number: 22

Abstract

Obesity is a major risk factor in the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease, and cancer. Several pieces of evidence across different species, including primates, underscore the implication of the histamine 3 receptor (H3R) in the regulation of food intake and body weight and the potential therapeutic effect of H3R inverse agonists. A pharmacophore model, based on ...