New CGRP Antagonists

CGRP antagonists: hope for a new era in acute migraine treatment.

Calcitonin gene-related peptide (CGRP) has a widespread distribution throughout the trigeminovascular system and other brain areas involved in migraine pathogenesis. Serum levels of CGRP are elevated during the migraine attack and return to normal with alleviation of pain. Intravenous injection of CGRP in migraineurs results in delayed headache similar to migraine. Since CGRP receptor antagonis...

CGRP antagonists and antibodies for the treatment of migraine.

Introduction: Migraine is a highly devastating neurovascular disorder that affects up to 16% of the population worldwide. In spite of intensive research, its origin remains enigmatic with no therapeutic option appropriate for all migraine patients. One of the leading hypotheses is related to the function of the calcitonin gene-related peptide (CGRP). Regardless, the pharmaceutical options curre...

Development and potential of non-peptide antagonists for calcitonin-gene-related peptide (CGRP) receptors: evidence for CGRP receptor heterogeneity.

Calcitonin-gene-related peptide (CGRP) is a 37-amino-acid vasodilatory peptide, of which two isoforms, alpha CGRP and beta CGRP, have been described. The use of C-terminal fragments of CGRP peptide, such as human alpha CGRP-(8-37), has led to the pharmacological subdivision of CGRP receptors into CGRP-1 [high potency for binding of human alpha CGRP-(8-37)] and CGRP-2 (lower potency) receptors. ...

CGRP antagonists for the treatment of migraine: rationale and clinical data

CGRP is localized in primary spinal afferent C and Ad fibers of the sensory ganglia and in the CNS, for example, in the colliculi and cerebellum. Trigeminal nerve activation results in antidromic release of CGRP that leads to vasodilatation via a CGRP-receptor complex (calcitonin-like receptor and RAMP1). At central synapses in the trigeminal nucleus caudalis, CGRP on second-order neurons trans...

Anti-CGRP antibodies: a new approach to migraine prevention.