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A-437203

Catalog No. T10213 CAS 220519-06-2

Synonyms: ABT-925, A37203, Lu201640

A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ﬀ old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.

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A-437203, CAS 220519-06-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 253.00
5 mg	In stock	$ 583.00
10 mg	In stock	$ 835.00
25 mg	In stock	$ 1,270.00
50 mg	In stock	$ 1,690.00
100 mg	In stock	$ 2,290.00
500 mg	In stock	$ 4,630.00
1 mL * 10 mM (in DMSO)	In stock	$ 666.00

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Purity: 98.62%

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Description	A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ﬀ old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.
Targets&IC50	D2 receptor:71 nM (Ki), D4 receptor:6220 nM , D3 receptor:1.6 nM
In vitro	A-437203 is an antagonist with high affinity for D3 receptors and relatively high selectivity compared to other dopamine receptor subtypes (44-fold selective for D3 vs D2)[1].
In vivo	A-437203 is initially tested alone in the rat forced swim test (FST). Doses of A-437203 evaluated are 0.52, 1.75, 5.24, and 17.46 μmol/kg i.p. Doses are chosen based on the selectivity of A-437203 for D3 vs D2 dopamine receptors and reports indicating that the effects of A-437203 at doses of 17.46 μmol/kg (10 mg/kg) or lower are clearly mediated by D3 but not D2 receptors since higher doses of the compound such as 174.6 μmol/kg (100 mg/kg) are necessary to bind and block D2 receptor from the irreversible inactivation induced by the alkylating agent EEDG. ANOVA revealed no significant difference between the treatments for any of the behaviors analyzed (F4, 45=1.12, p=0.359 for immobility, F4, 45=0.188, p=0.943 for climbing, and F4, 45=1.634, p=0.182 for swimming). Based on these results, the dose of 17.46 μmol/kg i.p. of A-437203 is selected for further experiments[1].
Animal Research	Male Sprague-Dawley rats weighing 250-350 g are used for these experiments. Haloperidol (0.27, 1.33, and 2.66 μmol/kg=0.1, 0.5, and 1.0 mg/kg i.p.), A-437203 (LU-201640) (0.52, 1.75, 5.24, and 17.46 μmol/kg=0.3, 1.0, 3.0, and 10.0 mg/kg i.p.), and L-745,870 (0.23, 1.15, 2.3, and 5.7 μmol/kg=0.1, 0.5, 1.0, and 2.5 mg/kg i.p.) are tested initially alone in order to determine effective dose ranges. In those experiments, haloperidol, A-437203, and L-745,870 are administered i.p. 24, 5, and 0.5 h before the test swim. In the subsequent antagonism experiments, Haloperidol (0.27 μmol/kg), A-437203 (17.46 μmol/kg) or L-745,870 (1.15 μmol/kg) are injected i.p. 15 min prior to each quinpirole injection (0.4 and 1.0 μmol/kg s.c.).

Synonyms	ABT-925, A37203, Lu201640
Molecular Weight	456.53
Formula	C20H27F3N6OS
CAS No.	220519-06-2

Storage

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

Solubility Information

DMSO: 60 mg/mL (131.43 mM)

References and Literature

1. Basso AM, et al. Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test. Neuropsychopharmacology. 2005 Jul;30(7):1257-68.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library GPCR Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max

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Keywords

A-437203 220519-06-2 GPCR/G Protein Neuroscience Dopamine Receptor A-37203 ABT925 ABT-925 A37203 ABT 925 A 437203 Lu201640 A437203 A 37203 inhibitor inhibit

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