CGRP是一种广泛分布于中枢和外周神经系统的神经肽,在偏头痛的发病机制中起重要作用,具有扩张血管、促进炎症、调节神经元敏化和增强体感疼痛的功能,其受体几乎位于所有可能涉及偏头痛发病的部位,CGRP受体拮抗剂通过阻断CGRP与其受体结合进而降低...
本发明一般地涉及式I化合物,(R)-N-(3-(7-甲基-1H-吲唑-5-基)-1-(4-(1-甲基哌啶-4-基)哌嗪-1-基)-1-氧代丙-2-基)-4-(2-氧代-1,2-二氢喹啉-3-基)哌啶-1-甲酰胺,包括可药用盐,其为CGRP-受体拮抗剂. The present invention generally relates to a compound of formula I, (R) -N- ...
On the basis of basic science studies over the past decade, a new generation of anti-migraine drugs is now being developed. At the forefront of these studies is a new calcitonin gene-related peptide (CGRP) receptor antagonist that is as effective as triptans in the acute treatment of ...
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
CGRP receptor inhibition, which has been shown to decrease spinal trigeminal activity, is likely to occur in the central nervous system rather than in the periphery including the trigeminal ganglion. This may be important for future therapeutic interventions with CGRP receptor antagonists in migraine. ...
Durham PL, Vause CV. Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine. CNS Drugs. 2010;24(7):539–48. Alder Biopharmaceuticals. Alder BioPharmaceuticals Announces Positive Eptinezumab Phase 3 Results for Prevention of Frequent Episodic Migraine.http://investor...
Rimegepant is Biohaven's orally-dosed CGRP receptor antagonist, which the Company is developing as a treatment for migraine. Rimegepant represents a novel mechanism that targets the underlying pathophysiology of migraine without causing vasoconstriction. The efficacy and sa...
Olesen J, Diener H, Husstedt I, Goadsby PJ, Hall D, Meier U, Pollentier S, Lesko LM (2004) Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med 3:1104–1110, 10.1056/NEJMoa030505 Article Google Scholar Ho TW, Mannix LK...
Efficacy of the non-peptide CGRP receptor antagonist BIBN4096BS in blocking CGRP-induced dilations in human and bovine cerebral arteries: Potential implications in acute migraine treatment 2002, Neuropharmacology Show abstract Vascular actions of calcitonin gene-related peptide and adrenomedullin 2004, Phys...
an alpha receptor antagonist, for example indoramin; an alpha receptor agonist; a vanilloid receptor antagonist; a renin inhibitor; a granzyme B inhibitor; a substance P antagonist; an endothelin antagonist; a norepinephrin precursor; anti-anxiety agents such as diazepam, alprazolam, chlordiazepoxide...