1. GPCR/G Protein
    Neuronal Signaling
  2. CGRP Receptor

CGRP Receptor

CGRP receptor is a heterotrimer: a large peptide with 7 transmembrane domains, named calcitonin receptor-like receptor (CLR or CRLR), is supplemented by a small single transmembrane peptide, named receptor activity-modifying protein (RAMP1) that forms the CGRP-specific ligand binding site. CGRP receptors are expressed by multiple different cell types within the nervous, cardiovascular and immune systems that are thought to play important roles in migraine pathology: on cerebral vascular smooth muscle, where they cause vasodilation, on dural mast cells triggering their degranulation, at the central terminals of the trigeminal nerve, where CGRP is a neuromodulator at second-order nociceptive neurons in the spinal trigeminal nucleus caudalis and in the dorsal horn of the spinal cord, where CGRP has a similar role in inducing central sensitisation to tactile stimuli. CGRP is produced in both peripheral and central neurons. It is a potent peptide vasodilator and can function in the transmission of pain.

CGRP Receptor Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-10095
    Olcegepant Antagonist 98.22%
    Olcegepant is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
  • HY-32709
    MK-0974 Antagonist 98.52%
    MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively; displays >1500-fold lower affinity for the canine and rat receptors.
  • HY-10302
    MK-3207 Hydrochloride Antagonist
    MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
  • HY-15498
    BMS-927711 Antagonist 99.08%
    BMS-927711 is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
  • HY-10301
    MK-3207 Antagonist
    MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
  • HY-10095A
    Olcegepant hydrochloride Antagonist
    Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.