产品
编 号：F755766
分子式：C23H25N3OS
分子量：391.53
分子式：C23H25N3OS
分子量：391.53
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
结构图
CAS No: 2765294-54-8
产品详情
生物活性：
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
体内研究：
TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel.TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats.TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66.Animal Model:KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model
Dosage:3, 10, and 30 mg/kg. 20 μL of solution of capsaicin (16 mg/20 mL) was injected s.c. under the skin of the dorsal surface of the right hind paw, or injected with 0.6% acetic acid (0.1 mL/10 g/mouse i.p.).
Administration:Intraperitoneally administration; 30 min
Result:In capsaicin-induced nociception, licking time decreased significantly in a dose-dependent manner. In acid-induced nociception, no significant anti-nociceptive activities were found compared with the control (SB-705498 and BCTC) at all dosage. In thermal-induced nociception, the latency time of nociceptive responses was increased at the doses of 10 and 30 mg/kg.
Animal Model:Spragur-Dawley male rats (220-250 g)
Dosage:10 mg/kg or 20 mg/kg
Administration:Intravenous injection of 10 mg/kg or oral dose of 20 mg/kg (Pharmacokinetic Analysis)
Result:In vivo pharmacokinetic parameters of TRPV1 antagonist 3 in rats (n=3)ParametersIV PO
t1/2 (h)0.106 ± 0.076
t1/2, ka (h)0.462 ± 0.096
t1/2, k10 (h) 0.527 ± 0.106
ka (1/h)1.65 ± 0.364
k10 (1/h)12.076 ± 2.3371.133 ± 0.358
V (L/kg)0.003 ± 0.0010.016 ± 0.006
CL (L/h/kg)0.024 ± 0.0130.022 ± 0.01
Tmax (h)0.711 ± 0.144
Cmax (ng/mL)311.377 ± 108.017
AUC 0-inf (ng/mL*h)495.955 ± 214.634598.873 ± 212.319
体外研究：
TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels.TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL) .
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
体内研究：
TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel.TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats.TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66.Animal Model:KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model
Dosage:3, 10, and 30 mg/kg. 20 μL of solution of capsaicin (16 mg/20 mL) was injected s.c. under the skin of the dorsal surface of the right hind paw, or injected with 0.6% acetic acid (0.1 mL/10 g/mouse i.p.).
Administration:Intraperitoneally administration; 30 min
Result:In capsaicin-induced nociception, licking time decreased significantly in a dose-dependent manner. In acid-induced nociception, no significant anti-nociceptive activities were found compared with the control (SB-705498 and BCTC) at all dosage. In thermal-induced nociception, the latency time of nociceptive responses was increased at the doses of 10 and 30 mg/kg.
Animal Model:Spragur-Dawley male rats (220-250 g)
Dosage:10 mg/kg or 20 mg/kg
Administration:Intravenous injection of 10 mg/kg or oral dose of 20 mg/kg (Pharmacokinetic Analysis)
Result:In vivo pharmacokinetic parameters of TRPV1 antagonist 3 in rats (n=3)ParametersIV PO
t1/2 (h)0.106 ± 0.076
t1/2, ka (h)0.462 ± 0.096
t1/2, k10 (h) 0.527 ± 0.106
ka (1/h)1.65 ± 0.364
k10 (1/h)12.076 ± 2.3371.133 ± 0.358
V (L/kg)0.003 ± 0.0010.016 ± 0.006
CL (L/h/kg)0.024 ± 0.0130.022 ± 0.01
Tmax (h)0.711 ± 0.144
Cmax (ng/mL)311.377 ± 108.017
AUC 0-inf (ng/mL*h)495.955 ± 214.634598.873 ± 212.319
体外研究：
TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels.TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL) .
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