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L-745870 hydrochloride

Catalog No. T11799 CAS 1173023-36-3

L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM.

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L-745870 hydrochloride Chemical Structure

L-745870 hydrochloride, CAS 1173023-36-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 56.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 188.00
50 mg	In stock	$ 313.00
100 mg	In stock	$ 455.00
200 mg	In stock	$ 655.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 97.36%

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Description	L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM.
Targets&IC50	D2 receptor (human):960 nM(Ki), D4 receptor (human):0.43 nM(Ki), D3 receptor (human):2300 nM(Ki)
In vitro	In vitro pharmacological studies revealed that L-745870 is an antagonist at human D4 receptors, in that L-745870 antagonized the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding,?blocked the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells,?blocked dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells,?inhibited D4 activation of cloned G protein-coupled inwardly rectifying K+ channels,?and antagonized dopamine-induced stimulation of extracellular acidification in transfected cells[1].
In vivo	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 high brain to plasma ratios in rat[1].?Evaluation of L-745870 in surrogate marker assays demonstrates that this compound is freely available for biological activity in the brain and that at doses of 5 to 60 mg/kg p.o. L-745870 would occupy 50% D4 receptors in the brain.?L-745870 has no effect on apomorphine-induced stereotypy in rats but does induce catalepsy in mice, albeit at a high dose of 100 mg/kg p.o. that is likely to occupy D2 receptors in vivo.?High doses of L-745870 might also be expected to cause extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors.?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[1].

Molecular Weight	363.28
Formula	C18H20Cl2N4
CAS No.	1173023-36-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (137.63 mM), Sonication is recommended.

0.1 M HCL: 20 mg/mL (55.05 mM), when pH is adjusted to 3 with HCl. Sonication is recommended.

References and Literature

1. Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8. 2. 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. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library ReFRAME Related Library Anti-Parkinson's Disease Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Orally Active Compound Library

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Keywords

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