Palvanil 是一种 Capsaicin (HY-10448) 类似物，对TRPV1受体表现出较强的脱敏能力，其具有抗疼痛和抗炎作用。
| 生物活性 | Palvanil is aCapsaicin(HY-10448) analogue, shows strong desensitizing capability against theTRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects[1][2]. |
体外研究
(In Vitro) | Palvanil (0.1-1000 nM; 0-300 min) leads to calcium increasment in HEK-293 intracellular[1].
Palvanil (1-10 nM; 5 min) treatment desensitizes TRPV1 to the effect of Capsaicin significantly[1].
Cell Viability Assay[1] | Cell Line: | HEK-293 cells | | Concentration: | 0.1, 0.5, 1, 5, 10, 50, 100 and 1000 nM | | Incubation Time: | 0-300 min | | Result: | Produced a dose-dependent increase in intracellular calcium with a EC50of 0.65 nM. |
Cell Viability Assay[1] | Cell Line: | HEK-293-TPRV1 cells | | Concentration: | 1-10 nM | | Incubation Time: | 5 min | | Result: | Desensitized TRPV1 to the effect of Capsaicin significantly (IC50=0.81 nM). |
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体内研究
(In Vivo) | Palvanil (subcutaneous injection; 1 or 10 mg/kg; once) treatment shows hypothermic effect[2].
Palvanil (intraperitoneal injection; 100 μL (15 nM) per mouse; once) treatment reduces Capsaicin-induced bronchoconstriction[2].
Palvanil (intravenous injection; 0.5, 0.75, and 1 mg/kg; once) treatment shows antinociceptive effects on Formalin-induced nocifensive behavior[2].
Palvanil (intravenous injection; 0.5, 0.75, and 1 mg/kg; once) treatment inhibits Carrageenan-induced inflammation[2].
Palvanil (intravenous injection; 0.5 and 1 mg/kg; once daily; 7 days) reduces mechanical allodynia and thermal hyperalgesia in spared nerve injury (SNI) mice[2].
| Animal Model: | Male CD-1 mice[2] | | Dosage: | 1 or 10 mg/kg | | Administration: | Subcutaneous injection; 1 or 10 mg/kg; once | | Result: | Led to a slight and short lasting hypothermic effect, produced late hyperthermia. |
| Animal Model: | Female BALB/C mice[2] | | Dosage: | 100 μL (15 nM) per mouse | | Administration: | Intraperitoneal injection; 100 μL (15 nM) per mouse; once | | Result: | Induced a significantly lower bronchoconstriction (from 0.47 to 0.605 cm H2O/L/s). |
| Animal Model: | Male CD-1 mice received formalin[2] | | Dosage: | 0.5, 0.75, and 1 mg/kg | | Administration: | Intravenous injection; 0.5, 0.75, and 1 mg/kg; once | | Result: | Reduced the second phase of Formalin-induced nociceptive behaviour in a dose-dependent manner. |
| Animal Model: | Male C57BL/6J mice with acute inflammation induced by Carrageenan[2] | | Dosage: | 2.5 mg/kg | | Administration: | Intravenous injection; 2.5 mg/kg; once | | Result: | Reduced the volume of the oedema in the ipsilateral hind paw (64%). |
| Animal Model: | Male CD-1 mice[2] | | Dosage: | 0.5 and 1 mg/kg | | Administration: | Intravenous injection; 0.5 and 1 mg/kg; once daily; 7 days | | Result: | Reduced mechanical allodynia and thermal hyperalgesia at 3 and 7 days after nerve injury in a dose-dependent manner. |
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| 来源 | - Plants
- Solanaceae
- Capsicum annuumL.
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| 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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