L-745870 hydrochloride

L-745870盐酸盐

L-745870 hydrochloride

L656501-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D 4 receptor antagonist with a K i of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D 2 ( K i of 960 nM) and D 3 ( K i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT 2 receptors, sigma sites and α-adrenoceptors . In Vitro L-745870 is capable of antagonizing the ability of D 4 receptors to inhibit agonist-induced stimulation of [ 35 S]-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 Ca 2+ currents in transfected GH4C1 pituitary cells; inhibiting D 4 activation of cloned G protein-coupled inwardly rectifying K + channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

L-745870 盐酸盐是一种强效、选择性、脑穿透性和口服活性多巴胺 D 4 受体拮抗剂，其 K i 为 0.43 nM。L-745870 盐酸盐对 D 2（K i 为 960 nM）和 D 3（K i 为 2300 nM）受体的亲和力较弱，并表现出以下特征

1173023-36-3(DMSO)

C18H20Cl2N4

363.28 g/mol

C1CN(CCN1CC2=CNC3=C2C=CC=N3)C4=CC=C(C=C4)Cl.Cl