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L-745870 trihydrochloride

CAS No. : 866021-03-6

MCE 站：L-745870 trihydrochloride

产品活性：L-745870 trihydrochloride 是一种有效的，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，K_i 为 0.43 nM，而对 D₂ (K_i 为 960 nM) 和 D₃ (K_i 为 2300 nM) 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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

In Vitro: 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; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells.

In Vivo: L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t_1/2 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.

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