产品描述
PrNMI is a potent and orally active agonist of peripherally restricted cannabinoid 1 receptor (CB1R) . PrNMI suppresses chemotherapy-induced peripheral neuropathy pain symptoms and also acts as an analgesic in cancer-induced bone pain.
体外活性
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.
体内活性
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.
Cas No.
1541244-33-0
分子式
C29H31NO
分子量
409.573
别名
PrNMI
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years