Development of Melanin Concentrating Hormone Receptor R1 Antagonists for the Pharmacological Treatment of Obesity
Pp. 200-228 (29)
Gildardo Rivera, Antonio Monge and Virgilio Bocanegra-Garcia
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.
Development, Melanin concentrating hormone (MCH), Melanin concentrating hormone
receptor 1 (MCH-R1), Structure-activity relationship (SAR), Obesity.
Departamento de Farmacia y Quimica Medicinal, Unidad Academica Multidisciplinaria Reynosa Aztlan, Universidad Autonoma de Tamaulipas, Calle 16 y Lago de Chapala, s/n, 88740, Reynosa, Mexico.