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 相关产品 (6):

Cat. No. Product Name Effect Purity
  • HY-10095
    Olcegepant Antagonist 99.32%
    Olcegepant 是一种有效的,选择性的非肽段 CGRP1 拮抗剂,抑制人 CGRP,IC50 值为 0.03 nM, Ki 值为 14.4 pM。
  • HY-32709
    MK-0974 Antagonist 98.52%
    MK-0974 是一种高效的,选择性的,可口服的 CGRP receptor 拮抗剂,作用于人类和恒河猴的CGRP受体,Ki 值分别为 0.77 nM 和 1.2 nM。
  • HY-10302
    MK-3207 Hydrochloride Antagonist
    MK-3207 Hydrochloride 是一种有效的,可口服的 CGRP receptor 拮抗剂,IC50 值为 0.12 nM,Ki 值为 0.024 nM。
  • HY-15498
    BMS-927711 Antagonist 99.08%
    BMS-927711 是一种有效的降钙素基因相关肽 (CGRP) 受体拮抗剂,Ki 为 0.027 nM。
  • HY-10301
    MK-3207 Antagonist
    MK-3207是口服生物相容性的CGRP受体拮抗剂,IC50和Ki分别为0.12 nM和0.024 nM,对AM1,AM2,CTR和AMY3的抑制性较弱。
  • HY-10095A
    Olcegepant hydrochloride Antagonist
    Olcegepant hydrochloride (BIBN4096BS hydrochloride) 是高效选择性的降钙素基因相关肽 (CGRP) 的拮抗剂, 对人类CGRP的Ki值为14.4 pM。