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L-745870 hydrochloride  ≥99%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：一种有效的，选择性的可透过血脑屏障和具有口服活性的多巴胺 D4 受体拮抗剂，Ki 为0.43nM，而对D2 (Ki 为 960nM) 和 D3 (Ki 为 2300nM) 受体的亲和力相对较弱，对 5-HT2 受体，sigma 位点和α-肾上腺素受体表现出中等亲和力。
溶解性：溶于0.1 M HCL（25mg/mL 超声）
储备液保存：-80°C, 6 months; -20°C, 1 month。 (sealed storage, away from moisture)
靶点：Human D4 Receptor：4.3 nM (Ki);D2 Receptor：960 nM (Ki);D3 Receptor：2300 mM (Ki)
体外研究：L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO)cells; blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells;inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels; andantagonizing dopamine-induced stimulation of extracellular acidification in transfected cells.
体内研究：L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat. Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys.
保存条件：-20℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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