Preferred Label : Zavegepant;
NCIt synonyms : 1-Piperidinecarboxamide, 4-(1,2-Dihydro-2-oxo-3-quinolinyl)-N-((1R)-1-((7-methyl-1H-indazol-5-yl)methyl)-2-(4-(1-methyl-4-piperidinyl)-1-piperazinyl)-2-oxoethyl)-; 4-(1,2-Dihydro-2-oxo-3-quinolinyl)-N-((1R)-1-((7-methyl-1H-indazol-5-yl)methyl)-2-(4-(1-methyl-4-piperidinyl)-1-piperazinyl)-2-oxoethyl)-1-piperidinecarboxamide; Vazegepant;
NCIt definition : A highly soluble small molecule calcitonin gene related peptide (CGRP) receptor antagonist,
with potential analgesic and immunomodulating activities. Upon administration, zavegepant
targets, binds to and inhibits the activity of CGRP receptors located on mast cells
in the brain. This may inhibit neurogenic inflammation caused by trigeminal nerve
release of CGRP. In addition, by blocking the CGRP receptors located in smooth muscle
cells within vessel walls, zavegepant inhibits the pathologic dilation of intracranial
arteries. Zavegepant, by blocking the CGRP receptors, also suppresses the transmission
of pain by inhibiting the central relay of pain signals from the trigeminal nerve
to the caudal trigeminal nucleus. Altogether, this may relieve migraine. As CGRP receptors
induce the release of pro-inflammatory mediators, such as interleukin-6 (IL-6), from
inflammatory cells, zavegepant may prevent an IL-6-mediated inflammatory response.
Zavegepant may also inhibit the CGRP-mediated induction of eosinophil migration and
the stimulation of beta-integrin-mediated T cell adhesion to fibronectin at the site
of inflammation, and may abrogate the CGRP-mediated polarization of the T cell response
towards the pro-inflammatory state characterized by Th17 and IL-17. This may improve
lung inflammation and oxygenation, prevent edema, and further lung injury. CGRP, a
37 amino-acid peptide expressed in and released from a subset of polymodal primary
sensory neurons of the trigeminal ganglion and nerve fibers projecting to the airways
and by pulmonary neuroendocrine cells, plays an important role in pain transmission,
inflammation, and neurogenic vasodilatation. It is released upon acute lung injury
and upregulation of transient receptor potential (TRP) channels.;
UNII : ODU3ZAZ94J;
InChIKey : JJVAPHYEOZSKJZ-JGCGQSQUSA-N;
CAS number : 1337918-83-8;
Molecule name : BHV-3500; BHV 3500; BMS 742413; BMS-742413;
NCI Metathesaurus CUI : CL1406705;
Origin ID : C172616;
UMLS CUI : C5383284;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Manual NTBT mappings (CISMeF)
- Semantic type(s)
- concept_is_in_subset
