Bay 59-3074

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Chemical Structure| 406205-74-1 同义名 : -
CAS号 : 406205-74-1
货号 : A885020
分子式 : C18H13F6NO4S
纯度 : 98%
分子量 : 453.36
MDL号 : MFCD09027365
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 BAY 59-3074 is a structurally novel cannabinoid CB1/CB2 receptor partial agonist with analgesic properties. Rats learned to discriminate BAY 59-3074 (0.5 mg/kg, p.o., t-1 h) from vehicle in a fixed-ratio: 10, food-reinforced two-lever procedure after a median number of 28 training sessions. BAY 59-3074 generalized dose-dependently (ED50: 0.081 mg/kg, p.o.) and the cue was detectable between 0.25 and 4 h after administration. Complete generalization was also obtained after i.p. administration of BAY 59-3074 (ED50 value: 0.41 mg/kg), and the reference cannabinoids BAY 38-7271 (0.011 mg/kg), CP 55,940 (0.013 mg/kg), HU-210 (0.022 mg/kg), WIN 55,212-2 (0.41 mg/kg) and (-)-Delta9-tetrahydrocannabinol (0.41 mg/kg). The discriminative stimulus effects of BAY 59-3074 are specifically mediated by cannabinoid CB1 receptor activation[3]. BAY 59-3074 (0.3-3 mg/kg, p.o.) induced antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli 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). 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[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.03mL

2.21mL

1.10mL

22.06mL

4.41mL

2.21mL

参考文献

[1]De Vry J, Denzer D, 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, Jentzsch KR. 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.

[3]De Vry J, Jentzsch KR. 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

[4]De Vry J, Denzer D, Reissmueller E, Eijckenboom M, Heil M, Meier H, Mauler F. 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