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CAS No. : 168266-90-8
MCE 国际站:Vofopitant
产品活性:Vofopitant 是一种有效的 NK1 receptor 拮抗剂,对人,大鼠和雪貂的 NK1 receptor 的 pKi 值分别为 10.6,9.5 和 9.8。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Neurokinin Receptor
In Vitro: Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca2+ channel, with pKis of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK2 and NK3, with pIC50 of <5.0. GR205171 (300 µM) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus.
In Vivo: Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze. Vofopitant (GR205171, 30 mg/kg, i.p.) increases the extracellular 5-HT levels in the frontal cortex of paroxetine-treated wild-type mice, rather than in wild-type mice and paroxetine-treated NK1 receptor knockout mice.
相关产品:Talnetant hydrochloride | [Tyr8,Nle11] Substance P | Neurokinin A(4-10) TFA | Maropitant-13C,d3 | [Sar4] Substance P (4-11) | MEN11467 | Spantide I TFA | [MePhe8,Sar9] Substance P | (β-Ala8)-Neurokinin A (4-10) | [MePhe7]-Neurokinin B | MLGFFQQPKPR-NH2 | Vapreotide acetate | Rolapitant | Biotin-NeurokininA | [D-Pro2,D-Trp7,9] Substance P | MEN 10207 | Ibodutant | Netupitant metabolite Monohydroxy Netupitant | Fezolinetant | SB-222200 | Neurokinin A TFA | Neurokinin B TFA | Septide | CS-003 Free base | Phyllomedusin | Imnopitant | Men 10376 TFA | [Lys5,MeLeu9,Nle10]-NKA(4-10) | Fosaprepitant dimeglumine
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货号: HY-12142
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