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Vofopitant

Catalog No. T13329 CAS 168266-90-8

Synonyms: GR 205171

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

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Vofopitant, CAS 168266-90-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 455.00
25 mg	In stock	$ 855.00
50 mg	In stock	$ 1,370.00
100 mg	In stock	$ 1,870.00
500 mg	In stock	$ 3,750.00

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Purity: 97.61%

ee: 97.524%

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Description	Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).
Targets&IC50	NK1 receptor (rat):9.5 (pKi), NK1 receptor (human):10.6 (pKi), NK1 receptor (ferret):9.8(pKi)
In vitro	Co-administration of paroxetine (4 mg/kg; i.p.) with the NK1 receptor antagonists, Vofopitant/GR205171 (30 mg/kg; i.p.) or L733060 (40 mg/kg; i.p.), potentiated the effects of paroxetine on cortical [5-HT]ext in wild-type mice, whereas GR205171 (30 mg/kg; i.p.) had no effect on paroxetine-induced increase in cortical [5-HT]ext in NK1 receptor knock-out mice. When GR205171 (300 micro mol/L) was perfused by 'reverse microdialysis' into the dorsal raphe nucleus, it potentiated the effects of paroxetine on cortical [5-HT]ext, and inhibited paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus[2].
In vivo	In a T-maze experiment, Vofopitant (GR205171, 30 mg/kg, subcutaneously) enhances the selection of a 25-second delayed reward[3]. Furthermore, when administered intraperitoneally at the same dosage, Vofopitant elevates extracellular serotonin (5-HT) levels in the frontal cortex of wild-type mice treated with paroxetine, but not in untreated wild-type or in NK1 receptor knockout mice also treated with paroxetine[2].

Synonyms	GR 205171
Molecular Weight	432.44
Formula	C21H23F3N6O
CAS No.	168266-90-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. 2. Guiard BP, et al. Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. J Neurochem. 2004 Apr;89(1):54-63. 3. Loiseau F, et al. Antidepressant-like effects of agomelatine, melatonin and the NK1 receptor antagonist GR205171 in impulsive-related behaviour in rats. Psychopharmacology (Berl). 2005 Oct;182(1):24-32. Epub 2005 Sep 29.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library

Related Products

Related compounds with same targets

Vofopitant dihydrochloride Spantide acetate [Sar9,Met(O2)11]-Substance P Neurokinin A Fosaprepitant dimeglumine [Sar9,Met(O2)11]-Substance P acetate Lanepitant 2HCl GR-73632

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Keywords

Vofopitant 168266-90-8 GPCR/G Protein Neuroscience Neurokinin receptor GR 205171 GR205171 GR-205171 inhibitor inhibit

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