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Melanocortins: Multiple Actions and Therapeutic Potential pp 61–70Cite as

Melanocortins in Brain Inflammation: The Role of Melanocortin Receptor Subtypes

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Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 681))

Abstract

The melanocortins (MC) are released from neurons and paracrine cells in the CNS where they are involved in important physiological functions, including regulation of body temperature and immune responses. MC bind to melanocortin receptors, a class of cell surface G-protein-coupled receptors. Of the five subtypes of MC receptors that have been cloned in mammals, the MC1, MC3, MC4 and MC5 receptors are expressed in brain tissues. Expression of MC receptors in both brain cells and cells of the immune system suggests direct involvement of MC in regulation of inflammatory processes in the brain. The binding of MC to MC receptors induces activation of adenylate cyclase, increase in intracellular cAMP level and, consequently, inhibition of the nuclear transcription factor kappaB (NF-κB) signalling. Inflammatory processes contribute to development of severe CNS diseases, both in acute and chronic conditions. Thus far, the anti-inflammatory effects of MC in the CNS have been mainly studied using peptides that are relatively unselective for individual MC receptor subtypes. Consequently, these studies do not allow identification of specific MC receptor(s) involved in the regulation of inflammatory processes. However, recently synthesized ligands selective for individual MC receptors indicated that both MC4 and MC3 agonists are promising anti-inflammatory agents in treatment of brain inflammation.

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Authors and Affiliations

  1. Faculty of Medicine, University of Latvia, Sarlotes St. 1a, Riga, LV-1001, Latvia

    Ruta Muceniece

  2. Latvian Institute of Organic Synthesis, Riga, Latvia

    Maija Dambrova

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  1. Ruta Muceniece
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  2. Maija Dambrova
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Correspondence to Ruta Muceniece .

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  1. Fondazione IRCCS, Center for Preclinical Investigation, Ca Granda, Ospedale Maggiore Policlinico, Milano, Italy

    Anna Catania MD

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Muceniece, R., Dambrova, M. (2010). Melanocortins in Brain Inflammation: The Role of Melanocortin Receptor Subtypes. In: Catania, A. (eds) Melanocortins: Multiple Actions and Therapeutic Potential. Advances in Experimental Medicine and Biology, vol 681. Springer, New York, NY. https://doi.org/10.1007/978-1-4419-6354-3_5

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