Abstract
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.
About this chapter
Cite this chapter as:
Gildardo Rivera, Antonio Monge, Virgilio Bocanegra-Garcia ;Development of Melanin Concentrating Hormone Receptor R1 Antagonists for the Pharmacological Treatment of Obesity, Anti-Obesity Drug Discovery and Development (2011) 1: 200. https://doi.org/10.2174/978160805163211101010200
DOI https://doi.org/10.2174/978160805163211101010200 |
Print ISSN 2210-2698 |
Publisher Name Bentham Science Publisher |