Anti-Obesity Drug Discovery and Development

Volume: 1

Development of Melanin Concentrating Hormone Receptor R1 Antagonists for the Pharmacological Treatment of Obesity

Author(s): Gildardo Rivera, Antonio Monge and Virgilio Bocanegra-Garcia

Pp: 200-228 (29)

DOI: 10.2174/978160805163211101010200

* (Excluding Mailing and Handling)


In this chapter we review the development of melanin concentrating hormone receptor 1 (MCH-R1) antagonists as a new perspective for the pharmacological treatment of obesity. We will initially focus on melanin concentrating hormone (MCH): structure, localization and function in the regulation of feeding behavior and energy balance and two receptors for MCH in humans. We will then review the discovery of the first MCH-R1 antagonists, the drug-design strategies used to obtained new series of MCH-R1 antagonists and an analysis of their structure-activity relationship. Finally, we will evaluate the absorption, distribution, metabolism and excretion, efficacy, safety and toxicity in preclinical and clinical trials.

Keywords: Development, Melanin concentrating hormone (MCH), Melanin concentrating hormone receptor 1 (MCH-R1), Structure-activity relationship (SAR), Obesity.

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