CGRP Receptor antagonistes/agonistes (CGRP Receptor Antagonists/agonists)

Calcitonin gene-related peptide (CGRP) is the most potent microvascular vasodilator known to date. Widely expressed in the nervous system, this peptide is considered to play a positive role in wound healing and protects against ischaemic and other traumas. However, whilst the protective mechanisms are not well understood, evidence indicates that these mechanisms become important in vascular-related stress. CGRP is both a potent vasodilator and hypotensive agent. Two distinct forms of CGRP receptors have been identified through pharmacological studies including CGRP1 receptor and CGRP2 receptor. Heterodimerization of CL with RAMP1 leads to the formation of a functional CGRP receptor on the cell surface, whilst association with RAMP 2 forms an AM1 and with RAMP 3 an AM/CGRP receptor is formed.