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

L-745870 is capable of antagonizing the ability of D₄receptors 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 D₄activation of cloned G protein-coupled inwardly rectifying K⁺channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells^[1].

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t_1/22.1-2.8 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].

363.28

Solid

C₁₈H₂₀Cl₂N₄

1173023-36-3

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 32.26 mg/mL(88.80 mM;Need ultrasonic)

0.1 M HCL : 25 mg/mL(68.82 mM;ultrasonic and adjust pH to 3 with HCl)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。