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CGRP receptor antagonists block the receptor for calcitonin gene-related peptide (CGRP), a neuropeptide. In 1982 alternative RNA processing of the calcitonin gene was shown to produce CGRP in neural tissue. The receptor is formed by calcitonin receptor-like receptor (CALCRL) together with receptor activity-modifying protein 1 (RAMP1), as described in 1998. CGRP release from trigeminal neurons is studied in migraine models and in neurogenic vasodilation. Olcegepant, telcagepant, MK-3207 and ubrogepant are small-molecule antagonists of this receptor complex. CGRP 8-37 (human) is a truncated peptide antagonist, and α-CGRP(human) serves as the native agonist.
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain.
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SB 268262 is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor. This compound exhibits high affinity for CGRP receptors in the human brain, making it a valuable tool for studying CGRP signaling pathways. SB 268262 is applicable in research investigating the pharmacological properties of non-peptide CGRP receptor antagonists, also known as gepants, in models including rat, pig, and human meninges.
