Netupitant hydrochloride
Based on 4 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 290296-54-7
- Formula: C30H34Cl2F6N4O
- Molecular Weight:651.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Netupitant hydrochloride
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Biological Activity
Description
IC50 & Target
[3]|
hNK1 |
In Vitro
Netupitant hydrochloride potently and selectively inhibits NK1 receptor-mediated contractions in isolated guinea pig detrusor muscle strips, with a mean pKB value of 9.24[1].
Netupitant (1-100 nM; 24 min) hydrochloride potently inhibits Substance P (SP)-induced calcium mobilization in CHO cells expressing human NK1 receptors, exhibiting insurmountable antagonism with a pKB value of 8.87[2].
Netupitant (1 μM; 24 min) hydrochloride acts as a low-potency surmountable antagonist of Substance P-induced calcium mobilization in HEK293 cells expressing the rat NK1 receptor, with a pKB value of 6.57[2].
Netupitant (Compound 21) hydrochloride potently binds to human NK1 receptors expressed in CHO cells, with a Ki value of 0.95 nM, and exhibits at least 100-fold selectivity over NK2 and NK3 receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Netupitant (0.1-3 mg/kg; intravenous injection; infusion duration 5 min) hydrochloride dose-dependently prolongs the contraction interval without altering the micturition amplitude in anesthetized guinea pigs with acetic acid-induced overactive bladder[1].
Netupitant (1-10 mg/kg, i.p.; single administration) hydrochloride significantly reduces Substance P-induced nociceptive behaviors such as scratching, gnawing and licking in mice[2].
Netupitant (0.3-3 mg/kg; i.p.; single dose; 0.1-3 mg/kg; p.o.; single dose) hydrochloride inhibits GR73632 (HY-P1192)-induced foot-tapping behavior in gerbils[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin-Hartley (adult female, anesthetized, isovolumetric bladder contraction model)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; infusion over 5 min
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Result:Reduced bladder contraction frequency dose-dependently relative to basal values, with reductions observed at 1 mg/kg and 3 mg/kg.
Showed no effect on bladder contraction amplitude at any tested dose.
Was approximately 3.9 times as potent as L-733,060 in reducing bladder contraction frequency when doses were compared in µmol/kg.
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Animal Model:Dunkin-Hartley (adult female, anesthetized, acetic acid-induced bladder overactivity model)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; infusion over 5 min
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Result:Increased intercontraction interval dose-dependently relative to basal values, with increases observed at all tested doses.
Showed no effect on amplitude of micturition at any tested dose.
Decreased basal pressure at 0.3 mg/kg and 3 mg/kg.
Showed no effect on threshold pressure at any tested dose.
Was approximately 11 times as potent as L-733,060 in increasing intercontraction interval when doses were compared in µmol/kg.
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Animal Model:Swiss mice (male, 20-25 g)[2]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Slightly reduced SP-induced nociceptive behavior at 1 mg/kg.
Significantly reduced cumulative SP-induced nociceptive behavior measured over 10 minutes at 10 mg/kg.
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Animal Model:Mongolian gerbils (male and female, 45-65 g)[2]
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Dosage:0.3-3 mg/kg (i.p.); 0.1-3 mg/kg (p.o.)
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Administration:i.p.; single dose; p.o.; single dose
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Result:Dose-dependently inhibited GR73632-induced foot tapping behavior with an ID50 of 1.5 mg/kg when administered intraperitoneally.
Dose-dependently inhibited GR73632-induced foot tapping behavior with an ID50 of 0.5 mg/kg when administered orally.
Fully prevented GR73632-induced foot tapping for 24 hours, reduced the response by approximately 50% at 48 hours, and the response fully recovered by 72 hours when administered orally at 3 mg/kg.
Chemical Information
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CAS No. 290296-54-7
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Molecular Weight 651.51
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Formula C30H34Cl2F6N4O
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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
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Synonyms
CID 6451149 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Metab
Cancer cells co-opt nociceptive nerves to thrive in nutrient-poor environments and upon nutrient-starvation therapies. [Abstract]2022 Dec 6;34(12):1999-2017.e10. PMID: 36395769 -
Cancers (Basel)
2024 Nov 12;16(22):3807. PMID: 39594764 -
Exp Neurol
Accelerated onset of the vesicovesical reflex in postnatal NGF-OE mice and the role of neuropeptides. [Abstract]2016 Nov;285(Pt B):110-125. PMID: 27342083 -
bioRxiv
2024 Oct 30:2024.10.30.620736. PMID: 39554043
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Netupitant hydrochloride Related Classifications
HY-16347 Related Classifications
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