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Postion:Product Catalog >A-437203
A-437203
  • A-437203

A-437203 NEW

Price $151 $349 $490
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: A-437203 CAS No.: 220519-06-2
Purity: 98.62% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameA-437203
DescriptionA-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ? old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.
Animal ResearchMale 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.).
In vitroA-437203 is a high-affinity antagonist for D3 receptors with 44-fold selectivity over D2 receptors, demonstrating relatively high selectivity among dopamine receptor subtypes[1].
In vivoA-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].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 60 mg/mL (131.43 mM)
KeywordsA-437203 | A-37203 | ABT925 | ABT 925 | A 437203 | A437203 | A 37203
Inhibitors RelatedOlanzapine | CLOZAPINE N-OXIDE | Mirtazapine | Promazine hydrochloride | Octopamine hydrochloride | Octodrine | Citicoline | Phenothiazine | Oxolinic acid | Mianserin hydrochloride | Doxepin hydrochloride | Fluphenazine dihydrochloride
Related Compound LibrariesBioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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