TRPV1 antagonist 3 (Compound 7q) 是一种有效的TRPV1拮抗剂，对 capsaicin 的IC50值为 2.66 nM。 TRPV1 antagonist 3 具有模式选择性和良好的口服生物利用度 (F = 60%)，可透过血脑屏障。
| 生物活性 | TRPV1 antagonist 3 (Compound 7q) is a potentTRPV1antagonist with anIC50of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant[1]. |
| IC50& Target | hTRPV1 2.66 nM (IC50) | TRPM8 7.45 μM (IC50) |
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体外研究
(In Vitro) | TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels[1].
TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL)[1].
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体内研究
(In Vivo) | TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel[1].
TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats[1].
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[1].
| Animal Model: | KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model[1] | | 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)[1] | | 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)[1]
| Parameters | IV | 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 ± 2.337 | 1.133 ± 0.358 | | V (L/kg) | 0.003 ± 0.001 | 0.016 ± 0.006 | | CL (L/h/kg) | 0.024 ± 0.013 | 0.022 ± 0.01 | | Tmax(h) | | 0.711 ± 0.144 | | Cmax(ng/mL) | | 311.377 ± 108.017 | | AUC0-inf(ng/mL*h) | 495.955 ± 214.634 | 598.873 ± 212.319 | | MRT (h) |
| | 分子量 | | | Formula | | | 运输条件 | Room temperature in continental US; may vary elsewhere. | | 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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