CGRP Receptor

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.

GPCR & G Protein

GluR AMPA Receptor-kainate Receptor-NMDA Receptor Gamma-secretase Dopamine Receptor 5-HT Receptor P2 Receptor AChR Histamine Receptor MAO Beta Amyloid Substance P BACE CaMK NMDAR GlyT Neurotrophin Notch BChE Adenosine Kinase Adenosine Deaminase Neurotensin Receptor Serotonin Transporter Secretase Calcineurin Ion Channel

Isoform-selective Products

CGRP

All (6)
CGRP Receptor Antagonists (6)
New CGRP Receptor Products

Cat.No.	Product Name	Information
E1980	Atogepant	Atogepant(MK-8031, AGN-241689) is a potent, selective, orally available antagonist of the calcitonin gene-related peptide (CGRP) receptor, with ki of 0.026 nM for human CGRP receptor. It is used for the preventive treatment episodic migraine.
E1824	Vazegepant hydrochloride	Vazegepant hydrochloride (BHV-3500, Zavegepant), is a highly potent, selective, and structurally unique small molecule antagonist of CGRP receptor. It can also be used for the acute treatment of migraine.
S6659	Rimegepant (BMS-927711)	Rimegepant (BMS-927711, BHV-3000) is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM.
E1280	Ubrogepant	Ubrogepant (MK-1602) is an antagonist of human calcitonin gene-related peptide receptor (CGRP). It potently blocks human α–CGRP–stimulated cAMP responses with an IC50 of 0.081 nM in human CGRP receptor-expressing HEK293 cells.
S8212	Olcegepant	Olcegepant (BIBN4096; BIBN4096BS) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with an IC50 of 0.03 nM.
E8191^New	Rat CGRP-(8-37)	Rat CGRP-(8-37) is a truncated version of calcitonin gene-related peptide (CGRP) and a highly selective antagonist of CGRP receptor. It exhibits anti-nociceptive effects and is effective in abolishing mechanical and thermal allodynia produced by spinal hemisection and may play a role in chronic central neuropathic pain.
E1980	Atogepant	Atogepant(MK-8031, AGN-241689) is a potent, selective, orally available antagonist of the calcitonin gene-related peptide (CGRP) receptor, with ki of 0.026 nM for human CGRP receptor. It is used for the preventive treatment episodic migraine.
E1824	Vazegepant hydrochloride	Vazegepant hydrochloride (BHV-3500, Zavegepant), is a highly potent, selective, and structurally unique small molecule antagonist of CGRP receptor. It can also be used for the acute treatment of migraine.
S6659	Rimegepant (BMS-927711)	Rimegepant (BMS-927711, BHV-3000) is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM.
E1280	Ubrogepant	Ubrogepant (MK-1602) is an antagonist of human calcitonin gene-related peptide receptor (CGRP). It potently blocks human α–CGRP–stimulated cAMP responses with an IC50 of 0.081 nM in human CGRP receptor-expressing HEK293 cells.
S8212	Olcegepant	Olcegepant (BIBN4096; BIBN4096BS) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with an IC50 of 0.03 nM.
E8191^New	Rat CGRP-(8-37)	Rat CGRP-(8-37) is a truncated version of calcitonin gene-related peptide (CGRP) and a highly selective antagonist of CGRP receptor. It exhibits anti-nociceptive effects and is effective in abolishing mechanical and thermal allodynia produced by spinal hemisection and may play a role in chronic central neuropathic pain.
E8191^New	Rat CGRP-(8-37)	Rat CGRP-(8-37) is a truncated version of calcitonin gene-related peptide (CGRP) and a highly selective antagonist of CGRP receptor. It exhibits anti-nociceptive effects and is effective in abolishing mechanical and thermal allodynia produced by spinal hemisection and may play a role in chronic central neuropathic pain.