|Description||Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK-receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. Check for active clinical trials or closed clinical trials using this agent. On 10/10 2014 FDA approved netupitant for the treatment of nausea and vomiting in patients undergoing cancer chemotherapy.|
|Synonyms||AGE94200; AGE-94200; AGE 94200;Ro 67-3189; Ro-67-3189; Ro67-3189; CHEBI441603; CID6451149; D05152; UNII-7732P08TIR, CHEMBL206253, AG-E-94200, Netupitant|
|Current Developer||Helsinn Group and Eisai Inc|
Aprepitant is a specific NK-1R antagonist, used as an antiemetic agent.
Kassinin, a tachykinin peptide derived from the Kassina frog, is secreted as a defense response, and is involved in neuropeptide signalling and shows selectivit...
MEN 10376 is a selective NK2 receptor antagonist.
An agonist of neurokinin 2 (NK2) receptor
Osanetant is a non-peptide neurokinin 3 (NK3) receptor antagonist. It is developed for the treatment of schizophrenia and other central nervous system (CNS) dis...
CP 99994 dihydrochloride
The hydrochloride salt form of CP 99994, which is a high affinity NK1 antagonist and could attenuate endothelium-dependent contraction induced by substance P.
L760735 is a high-affinity NK1 receptor antagonist with IC50 value of 0.19 nM. It is selective over NK2 and NK3 receptors. It is used in the synthetic preparati...
Eledoisin-Related Peptide is a tachykinin receptor ligand.