化合物Bay 59-3074 T3699

Product Introduction
Bioactivity


英文名: Bay 59-3074

描述: Bay 59-3074 是选择性的CB1/CB2受体的部分激动剂，其在 CB1 受体 (Ki:48.3 nM) 和 CB2 受体 (Ki:45.5 nM)。它可用于缓解疼痛的研究。

体外活性: analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (110.29 mM)


关键字: inhibit | Cannabinoid Receptor | Bay 59-3074 | Inhibitor | Bay 593074 | Bay 59 3074

相关产品: SR144528 | MJ 15 | Hemopressin (human, mouse) acetate | (R)-Monlunabant | Otenabant | CB2 modulator 1 | CB2R agonist 2 | CB2R/FAAH modulator-3 | CB1 antagonist 2 | CID 16020046

相关库: ReFRAME Related Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Fluorochemical Library | GPCR Compound Library | Anti-Fibrosis Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途