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L-745870 trihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-745870 trihydrochloride图片
CAS NO:866021-03-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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,Ki为 0.43 nM,而对 D2(Ki为 960 nM) 和 D3(Ki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。
生物活性

L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally activedopamineD4receptorantagonist with aKiof 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2(Kiof 960 nM) and D3(Kiof 2300 nM) receptors, and exhibits moderate affinity for 5-HT2receptors, sigma sites and α-adrenoceptors[1][2][3].

IC50& Target[3]

Human D4Receptor

4.3 nM (Ki)

D2Receptor

960 nM (Ki)

D3Receptor

2300 nM (Ki)

体外研究
(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[1].

体内研究
(In Vivo)

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/22.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat[1].
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[1].

分子量

436.21

Formula

C18H22Cl4N4

CAS 号

866021-03-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.