L-745870, inhibitor

L-745870

Cat. Num. AAA5753383

• Purity: 98.00%
• Synonyms: L-745870; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C18H19ClN4
• SMILES: ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43
• CAS Number: 158985-00-3
• Target & IC50: Human dopamine D4 receptor: ic50 0.43nM (ki); Human dopamine D2 receptor: ic50 960nM (ki); Human dopamine D3 receptor: ic50 2300nM (ki)
• In Vitro: L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with the high brain to plasma ratios in the rat. L-745870 has no effect on apomorphine-induced stereotypy in rats but does induce catalepsy in mice, albeit at a high dose of 100mg/kg p.o. that is likely to occupy D2 receptors in vivo. Evaluation of L-745870 in surrogate marker assays shows that this compound is freely available for biological activity in the brain and L-745870(5 to 60mg/kg; p.o.) treatment, would occupy 50% D4 receptors in the brain. Following oral administration to squirrel monkeys, L745870 (10mg/kg p.o.) causes mild sedation and extrapyramidal motor symptoms, notably bradykinesia became apparent at 30mg/kg. High doses of L-745870 might also be expected to induce extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors. Lower doses of L-745870 has no observable behavioral effects in monkeys[1][2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for L-745870, inhibitor

L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960nM) and D3 (Ki: 2300nM) receptors affinity.

Product Categories/Family for L-745870, inhibitor

GPCR/G Protein; Dopamine Receptor; Neuroscience

References

Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8.
Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8.
Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47.
Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47.
Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2.
Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2.