L-745870 is a potent, selective, brain-penetrant and orally activedopamineD₄receptorantagonist with aK_iof 0.43 nM. L-745870 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^[2].
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^[2].

326.82

Solid

C₁₈H₁₉ClN₄

158985-00-3

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : 25 mg/mL(76.49 mM;Need ultrasonic)

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 (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (7.65 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.65 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (7.65 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.65 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。