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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.
CGRP Antagonist 2 is a competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor. It effectively inhibits CGRP-mediated signaling, which is crucial for the modulation of nociceptive pathways associated with pain perception. This reagent is widely utilized in research focused on migraine mechanisms and pain management therapies.
BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP receptor). This compound exhibits significant biological activity in blocking CGRP-mediated signaling pathways, making it a valuable tool for migraine research. It is particularly effective in studies examining intranasal delivery methods for rapid therapeutic intervention in migraine treatment.
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.
