Vofopitant
Based on 1 Customer Validation
Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting.
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- Pureza: 99.41%
- No. CAS: 168266-90-8
- Fòrmula: C21H23F3N6O
- Peso molecular:432.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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NK1R 9.02 (pKi) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.08 nM
Compound: 3
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Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
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[PMID: 9804700] |
Vofopitant (GR 205171) (10 pM-1 mM; 60 min) potently inhibits [3H]-SP binding to NK1 receptors in mouse cerebral cortex homogenates with a pKi of 9.02[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vofopitant (GR-205171) (50 µg/kg; i.v.; single dose) abolishes fictive retching and emesis-associated antral contractility enhancement, reduces emesis-related hypersalivation and parasympathetic nerve activity, but does not affect gastric corpus relaxation, vagosalivary reflex-mediated salivation, or linguosalivary reflex responses in dogs[2].
Vofopitant (GR 205171) (10 mg/kg; s.c.; single dose) does not alter DRN serotonergic neuron firing or 5-HT1A autoreceptor sensitivity in male C57BL/6J mice[4].
Vofopitant (10 mg/kg/day; s.c.; continuous delivery; 21 days) reduces the potency of Ipsapirone (HY-19686) to inhibit DRN serotonergic neuron firing by ~1.5-fold, indicating functional desensitization of 5-HT1A autoreceptors in male C57BL/6J mice[4].
Vofopitant (10 mg/kg/day; s.c.; continuous delivery; 21 days) reduces the potency and maximal effect of 5-CT to stimulate [35S]GTP-γ-S binding in the DRN, indicating impaired G-protein coupling of desensitized 5-HT1A autoreceptors in male C57BL/6J mice[4].
Vofopitant (10 mg/kg/day; s.c.; continuous delivery; 21 days) significantly increases basal extracellular 5-HT levels in the DRN and potentiates Paroxetine (HY-122272)-induced cortical 5-HT overflow in male C57BL/6J mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice (20-26 g)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.; single dose
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Result:Did not reduce immobility time obviously at 3 mg/kg.
Exerted mild and non-significant reduction at 10 mg/kg.
Reduced immobility time significantly at 30 mg/kg.
Showed no notable changes in cortical monoamine levels at 30 mg/kg within 300 minutes.
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Animal Model:C57BL/6J (male, 8-10 weeks old, 20-25 g)[5]
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Dosage:10 mg/kg
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Administration:s.c.; single dose
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Result:Did not change firing frequency and pattern of DRN serotonergic neurons.
Exhibited comparable inhibitory potency of ipsapirone on neuronal firing between treatment and control groups.
Produced full inhibition at 100 nM ipsapirone in both groups.
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Animal Model:C57BL/6J (male, 8-10 weeks old, 20-25 g)[5]
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Dosage:10 mg/kg/day
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Administration:s.c.; continuous delivery; 21 days
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Result:Did not change basal firing rate of DRN serotonergic neurons.
Decreased ipsapirone’s inhibitory potency on neuronal firing and raised its concentration for full inhibition.
Displayed similar basal [35S]GTP-γ-S labelling in the DRN between groups.
Weakened 5-CT-induced [35S]GTP-γ-S binding with a right-shifted curve and lower maximal response.
Exerted no influence on basal extracellular 5-HT in the frontal cortex but elevated basal 5-HT levels in the DRN.
Enhanced paroxetine-triggered 5-HT elevation in both cortex and DRN of treated mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 168266-90-8
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Appearance Solid
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Peso molecular 432.44
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Fòrmula C21H23F3N6O
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Color Light yellow to yellow
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SMILES
COC1=C(CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)C=C(N4C(C(F)(F)F)=NN=N4)C=C1
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Synonyms
GR 205171
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (231.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zocchi A, et al. Effects of antidepressant drugs and GR 205171, an neurokinin-1 (NK1) receptor antagonist, on the response in the forced swim test and on monoamine extracellular levels in the frontal cortex of the mouse. Neurosci Lett. 2003;345(2):73-76. [Content Brief]
[2]. Furukawa N, et al. A neurokinin-1 receptor antagonist reduced hypersalivation and gastric contractility related to emesis in dogs. Am J Physiol. 1998;275(5):G1193-G1201. [Content Brief]
[3]. Heldt SA, et al. Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils. Behav Pharmacol. 2009;20(7):584-595. [Content Brief]
[4]. Guiard BP, et al. Sustained pharmacological blockade of NK1 substance P receptors causes functional desensitization of dorsal raphe 5-HT 1A autoreceptors in mice. J Neurochem. 2005;95(6):1713-1723. [Content Brief]
[5]. Mathew SJ, et al. A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept trial. Eur Neuropsychopharmacol. 2011;21(3):221-229. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3125 mL | 11.5623 mL | 23.1246 mL | 57.8115 mL |
| 5 mM | 0.4625 mL | 2.3125 mL | 4.6249 mL | 11.5623 mL | |
| 10 mM | 0.2312 mL | 1.1562 mL | 2.3125 mL | 5.7811 mL | |
| 15 mM | 0.1542 mL | 0.7708 mL | 1.5416 mL | 3.8541 mL | |
| 20 mM | 0.1156 mL | 0.5781 mL | 1.1562 mL | 2.8906 mL | |
| 25 mM | 0.0925 mL | 0.4625 mL | 0.9250 mL | 2.3125 mL | |
| 30 mM | 0.0771 mL | 0.3854 mL | 0.7708 mL | 1.9270 mL | |
| 40 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4453 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9635 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7226 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5781 mL |
Vofopitant Related Classifications
HY-12142 Related Classifications
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