Methods We performed a literature search of the PubMed and Cochrane databases in March 2020, using the keywords: "CGRP receptor antagonists", "gepants", "CGRP receptor blockers" and "CGRP acute medication". In total, 24 published studies were included. Results The development of first ...
CGRP receptor 作用机制 CALCRL拮抗剂(降钙素基因相关肽-1型受体拮抗剂) 治疗领域 神经系统疾病感染耳鼻咽喉疾病+ [4] 在研适应症 偏头痛慢性鼻窦炎伴鼻息肉鼻息肉+ [5] 非在研适应症 颞下颌关节障碍三叉神经痛 原研机构 Biohaven Ltd. 在研机构
We observed upregulation of CGRP in the DRG of rats with BCP and found that administration of a CGRP receptor blocker (CGRP8-37) potently inhibited BCP. Administration of BMP2-siRNA or a specific BMPR inhibitor is associated with downregulation of CGRP in the DRG, and also alleviating BCP (...
For CGRP, there are two receptors with approximately equal affinities [26]. The canonical CGRP receptor is a heterodimer of the GPCR calcitonin receptor-like receptor (CLR) and receptor activity-modifying protein 1 (RAMP1). A second CGRP receptor, AMY1, is a heterodimer of the GPCR calcitonin...
(GPCRs) and in particular, CGRP binds the amylin 1 (AMY1) receptor with equal affinity as its canonical receptor [26]. In the case of PACAP, the family member vasoactive intestinal peptide (VIP) caused migraine-like headaches comparable to PACAP, but only after prolonged infusion to mimic ...
Bourgault S, Vaudry D, Botia B, Couvineau A, Laburthe M, Vaudry H et al (2008) Novel stable PACAP analogs with potent activity towards the PAC1 receptor. Peptides 29(6):919–932 29. Banks WA, Kastin AJ, Komaki G, Arimura A (1993) Passage of pituitary adenylate cyclase ...
Both AITC and NaHS increased CGRP release from isolated rat tracheae, and both responses were inhibited by the TRPA1 antagonist, HC-030031, but was not affected by the TRPV1 receptor blocker, BCTC. Application of AITC or NaHS increased the cutaneous blood flow in the mouse ears. Similarly ...
EGCG-induced increase in mesenteric artery blood flow and reduction in mean arterial pressure were reversed by A-967079, CGRP receptor antagonist CGRP8-37, and CGRP depletion in perivascular nerves. Moreover, EGCG stimulated TRPA1-dependent intracellular Ca2+ elevation and CGRP release in a ...
Calcitonin gene-related peptide receptor antagonist BIBN4096BS for the acute treatment of migraine N Engl J Med, 350 (2004), pp. 1104-1110 Google Scholar 27 K.A. Petersen, L.H. Lassen, S. Birk, L. Lesko, J. Olensen BIBN4096BS antagonizes human alpha-calcitonin gene related peptide-...
The vasodilator response to PNS has been shown to be mediated by CGRPergic nerves because the response is blocked by a CGRP receptor antagonist (CGRP (8–37)) and a CGRP depletor (capsai- cin).26,27 In addition, injections of CGRP at 25, 50 and 100 nmol induced concentration-dependent...