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L-745870 is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

L-745870 is capable of antagonizing the ability of D₄ receptors to inhibit agonist-induced stimulation of [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 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.

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.

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)