S85296 |
Bay 59-3074 |
| MedMol | 98% |
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- 产品描述： Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties
- 靶点： Cannabinoid Receptor
- 体外研究： analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM
- 体内研究： In rat models of chronic neuropathic (chronic constriction injury, spared nerve injury, tibial nerve injury, and spinal nerve ligation models) and inflammatory pain (carrageenan and complete Freund's adjuvant models), BAY 59-3074 (0.3-3 mg/kg, p.o.) induced antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effects, which occur at doses above 1 mg/kg (e.g., hypothermia). Uptitration from 1 to 32 mg/kg p.o. (doubling of daily dose every 4th day) prevented the occurrence of such side effects, whereas antihyperalgesic and antiallodynic efficacy was maintained/increased. No withdrawal symptoms were seen after abrupt withdrawal following 14 daily applications of 1 to 10 mg/kg p.o.
- 参考文献：
1. De Vry J, et al. 3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects. J Pharmacol Exp Ther. 2004 Aug;310(2):620-32. 2. De Vry J, et al. Discriminative stimulus effects of the structurally novel cannabinoid CB1/CB2 receptor partial agonist BAY 59-3074 in the rat. Eur J Pharmacol. 2004 Nov 28;505(1-3):127-33.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.206 ml 11.029 ml 22.058 ml 5 mM 0.441 ml 2.206 ml 4.412 ml 10 mM 0.221 ml 1.103 ml 2.206 ml 50 mM 0.044 ml 0.221 ml 0.441 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
