290296-54-7
Chemical Structure
Netupitant hydrochloride
Synonym(s): CID 6451149 hydrochloride
- CAS No.: 290296-54-7
- Formula:C30H34Cl2F6N4O
- Molecular Weight:651.51
IUPAC Name: 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide hydrochloride
InChIKey: GJGWXFKSUTYHCU-UHFFFAOYSA-N
SMILES: O=C(C(C)(C)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N(C)C2=CN=C(N3CCN(CC3)C)C=C2C4=C(C)C=CC=C4.Cl.Cl
Biological Activity: Netupitant hydrochloride (CID 6451149 hydrochloride) is a blood-brain barrier penetrable, orally active NK1 receptor inhibitor with a Ki of 0.95 nM (CHO cells) against the human receptor. Netupitant hydrochloride antagonizes the effects induced by Substance P, inhibits the maximal response of Substance P with a long-lasting action, and suppresses NK1 agonist-induced behaviors in mice and gerbils. Netupitant hydrochloride reduces the frequency of bladder contractions, prolongs contraction intervals, decreases basal pressure at high doses, and acts on the afferent branch of the micturition reflex. Netupitant hydrochloride can be used in research related to overactive bladder, chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, anxiety disorders, and depression[1][2][3].
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Netupitant hydrochloride | Netupitant hydrochloride (CID 6451149 hydrochloride) is a blood-brain barrier penetrable, orally active NK1 receptor inhibitor with a Ki of 0.95 nM (CHO cells) against the human receptor. Netupitant hydrochloride antagonizes the effects induced by Substance P, inhibits the maximal response of Substance P with a long-lasting action, and suppresses NK1 agonist-induced behaviors in mice and gerbils. Netupitant hydrochloride reduces the frequency of bladder contractions, prolongs contraction intervals, decreases basal pressure at high doses, and acts on the afferent branch of the micturition reflex. Netupitant hydrochloride can be used in research related to overactive bladder, chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, anxiety disorders, and depression. | |||||||||||||||||||||
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References
- [1]. Palea S, et al. Netupitant, a Potent and Highly Selective NK1 Receptor Antagonist, Alleviates Acetic Acid-Induced Bladder Overactivity in Anesthetized Guinea-Pigs. Frontiers in pharmacology. 2016;7:234. [Content Brief]
- [2]. Rizzi A, et al. In vitro and in vivo pharmacological characterization of the novel NK₁ receptor selective antagonist Netupitant. Peptides. 2012 Sep;37(1):86-97. [Content Brief]
- [3]. Hoffmann T, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorganic & medicinal chemistry letters. 2006 Mar 01;16(5):1362-5. [Content Brief]
