Calcitonin-gene-related peptide (CGRP) and adrenomedullin (AM), two structurally related peptides, are synthesized and secreted by many mammalian tissues, including the central nervous system. The two peptides, which were initially described as vasodilators, are now considered as multifunctional regulatory agents. Their cellular actions are mediated by pharmacologically distinct receptors, each comprising two subunits: a classic 7 transmembrane spanning G protein-coupled receptor (GPCR) and one of 3 single transmembrane spanning accessory receptor activity modifying proteins (RAMP). Two GPCRs?the calcitonin receptor (CTR) and calcitonin-receptor-like receptor (CLR)?contribute to CGRP/AM receptor phenotypes. In the brain, CGRP and AM are widely expressed and, in addition to their vasodilator effect, activate several autonomic centers involved in the regulation of fluid and electrolyte balance. Additionally, they have modulatory effects on the synthesis and release of several other neuropeptides and have neuroprotective roles. The potent vasodilator activity of CGRP in cerebral microvasculature is possibly relevant to the pathology of migraine.
|Title of host publication||Handbook of Biologically Active Peptides|
|Editors||Abba J Kastin|
|Place of Publication||San Diego CA USA|
|Pages||744 - 751|
|Number of pages||8|
|Publication status||Published - 2013|