| 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.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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)
| 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 |
| AUC 0-inf (ng/mL*h) |
495.955 ± 214.634 |
598.873 ± 212.319 |
| MRT (h) |
| | 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.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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)
| 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 |
| AUC 0-inf (ng/mL*h) |
495.955 ± 214.634 |
598.873 ± 212.319 |
| MRT (h) |
| | 性状 | Solid |
|---|
| 溶解性数据 | |
|---|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
|---|
| 储存方式 |
| Powder |
-20°C |
3 years |
|
4°C |
2 years |
| In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
|---|
| 参考文献 | |
|---|
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