产品
编 号：F281573
分子式：C25H32FN5O2
分子量：453.55
分子式：C25H32FN5O2
分子量：453.55
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2244614-14-8
产品详情
生物活性：
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.
体内研究：
Navacaprant (BTRX-335140) (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment.Navacaprant (BTRX-335140) (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water.1.19Pharmacokinetic Parameters of BTRX-335140 in rodents.RatsIV 1 mg/kg MiceIV 3 mg/kgRatsPO 5 mg/kg MicePO 10 mg/kg
CL (mL/min/kg)10566.5
t1/2 (h)1.811.916.192.57
AUC0-t (h?ng/mL)153725265232
Vss (L/kg)13.87.72
F (%)30.212
Animal Model:Rat PRL model
Dosage:0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:Oral gavage; 0.01-3 mg/kg once
Result:Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.
Animal Model:Adult male ICR mice with tail dipped into 50°C hot water
Dosage:1 mg/kg
Administration:Intraperitoneal injection; 1 mg/kg once
Result:Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.
体外研究：
Navacaprant (BTRX-335140) (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor.
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.
体内研究：
Navacaprant (BTRX-335140) (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment.Navacaprant (BTRX-335140) (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water.1.19Pharmacokinetic Parameters of BTRX-335140 in rodents.RatsIV 1 mg/kg MiceIV 3 mg/kgRatsPO 5 mg/kg MicePO 10 mg/kg
CL (mL/min/kg)10566.5
t1/2 (h)1.811.916.192.57
AUC0-t (h?ng/mL)153725265232
Vss (L/kg)13.87.72
F (%)30.212
Animal Model:Rat PRL model
Dosage:0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:Oral gavage; 0.01-3 mg/kg once
Result:Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.
Animal Model:Adult male ICR mice with tail dipped into 50°C hot water
Dosage:1 mg/kg
Administration:Intraperitoneal injection; 1 mg/kg once
Result:Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.
体外研究：
Navacaprant (BTRX-335140) (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor.
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