PrNMI 是一种有效的、具有口服活性的外周限制性大麻素 1 受体 (CB1R) 激动剂。PrNMI 可抑制化疗引起的周围神经病变疼痛症状，并且还可作为癌症引起的骨痛的镇痛剂。
| 生物活性 | PrNMI is a potent and orally active agonist of peripherally restrictedcannabinoid 1 receptor (CB1R). PrNMI suppresses chemotherapy-induced peripheral neuropathy pain symptoms and also acts as an analgesic in cancer-induced bone pain[1][2]. |
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体外研究
(In Vitro) | PrNMI (1 nM-1 μM; 24 hours) shows no effects on viability of 66.1 breast tumor cells in vitro[2].
Cell Viability Assay[2] | Cell Line: | 66.1 breast cancer cell | | Concentration: | 1 nM, 10 nM, 100 nM, and 1 μM | | Incubation Time: | 24 hours | | Result: | Showed no effects on viability of 66.1 breast tumor cells in vitro. |
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体内研究
(In Vivo) | PrNMI (0.25 mg/kg; Intraplantar ipsilateral administration; i.p.) causes significantly greater suppression in mechanical but not cold allodynia on the ipsilateral paw compared to contralateral paw or systemic administration at 2 h post-PrNMI[1].
PrNMI (3.0 mg/kg; i.g.; 48 hours) dose-dependently suppresses CIPN symptoms in both male and female rats and is equally effective in male and female rats after oral administration[1].
PrNMI (1 mg/kg; p.o.; 48 hours) exhibits anti-allodynic effects in CIPN mediated mainly by CB1Rs[1].
PrNMI (1 mg/kg; p.o.; daily for two weeks) shows no significant tolerance to suppression of both mechanical and cold allodynia during the two-week testing period[1].
PrNMI (0.1, 0.3, and 0.6 mg/kg; i.p.) results in a significant, time-related reduction of flinching but not guarding in a dose-dependent manner. This suppression of flinching starts 1-hour post-injection and persists for at least 5 hours[2].
| Animal Model: | Chemotherapy-induced peripheral neuropathy (CIPN) rat model (Cisplatin; i.p.; daily 3 mg/kg for 4 weeks)[1] | | Dosage: | 0.25 mg/kg | | Administration: | Intraplantar ipsilateral administration; i.p. | | Result: | At 2 h post-PrNMI, mechanical but not cold allodynia suppression was significantly greater on the ipsilateral paw compared to contralateral paw or systemic administration. |
| Animal Model: | Chemotherapy-induced peripheral neuropathy (CIPN) rat model (i.p.; daily 3 mg/kg for 4 weeks)[1] | | Dosage: | 1 mg/kg | | Administration: | p.o.; daily for two weeks | | Result: | Suppressed mechanical and cold allodynia CIPN symptoms. |
| Animal Model: | 18–20 g female BALB/cAnNHsd mice (bearing murine mammary tumor line, 66.1; CIBP model)[2] | | Dosage: | 0.1, 0.3, and 0.6 mg/kg | | Administration: | i.p. | | Result: | Resulted in a significant, time-related reduction of flinching but not guarding in a dose-dependent manner. This suppression of flinching started 1-hour post-injection and persisted for at least 5 hours. |
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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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