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A-381393

Catalog No. T5397 CAS 726174-00-1

A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor).

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A-381393, CAS 726174-00-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 56.00
2 mg	In stock	$ 79.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 369.00
50 mg	In stock	$ 531.00
100 mg	In stock	$ 768.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.92%

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Description	A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor).
Targets&IC50	D4.2 receptor:1.9 nM (Ki, cell free), D4.4 receptor:1.5 nM (Ki, cell free), D4.7 receptor:1.6 nM (Ki, cell free)
In vitro	A-381393 potently bound to the membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when compared to D1, D2, D3, and D5 dopamine receptors. A-381393 potently inhibited the functional activity of agonist-induced GTP-gamma-S binding assay and 1 microM dopamine-induced-Ca2+ flux in human dopamine D4.4 receptor-expressing cells, but not in human dopamine D2L or D3 receptor cells [1]. A-381393 blocked both c-Fos expression and ERK1/2 phosphorylation produced by PD168077. Treatment with A-381393 alone significantly reduced the amount of Fos immunoreactivity as compared to basal expression observed in vehicle-treated controls [2].

Molecular Weight	320.43
Formula	C20H24N4
CAS No.	726174-00-1

Storage

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

Solubility Information

DMSO: 50 mg/mL (156.04 mM)

References and Literature

1. Nakane M, et al. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. 2. Bitner RS, et al. Dopamine D4 receptor signaling in the rat paraventricular hypothalamic nucleus: Evidence of natural coupling involving immediate early gene induction and mitogen activated protein kinase phosphorylation. Neuropharmacology. 2006 Apr;50(5):521-31.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Inhibitor Library GPCR Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library CNS-Penetrant Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Anti-Parkinson's Disease Compound Library

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Keywords

A-381393 726174-00-1 GPCR/G Protein Neuroscience Dopamine Receptor inhibit A381393 A 381393 Inhibitor inhibitor

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