Amisulpride [Dopamine D2 Receptor; Dopamine D3 Receptor Antagonist]

[CAT#: MOD2005ZP217]

A highly potent, selective dopamine D2 and D3 receptor antagonist. Atypical antipsychotic.

Target:: DRD2

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Product Overview

Synonyms

DAN 2163

Chemical Name

4-Amino-N-[(1-ethyl-2-pyrrolidinyl) methyl]-5-(ethylsulfonyl)-2-benzamide

Modulator Type

Antagonist

Relevant Disease

Neurological Disorders

In Vitro Assay

Assay Description

Amisulpride is an atypical dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively. Amisulpride (100 nM) inhibits the incorporation of [3H] thymidine caused by quinoxaline, with an IC50 value of 22±3 nM (n = 3). Amisulpride slightly but significantly increased [3H] dopamine release in rat striatum slices (under controlled conditions, S2/S1 = 0.88±0.04, n = 6; in the presence of 100 nM amisulpride In this case, n = 4; 1.04±0.08; P <0.05) and opposed the inhibitory effect of 7-OH-DPAT in two brain regions [1].

Reference

In Vivo Assay

Assay Description

Only the highest dose of amisulpride (100 mg/kg) can significantly reduce dopamine levels in the striatum or limbic system. Amisulpride significantly increased dopamine synthesis in the striatum and limbic system of rats at doses of 20 and 100 mg/kg. Amisulpride (0.5 to 75 mg/kg) does not cause a further increase in dopamine accumulation in the striatum, but dopamine synthesis in the limbic system is slightly accelerated at 75 mg/kg. Compared with the vehicle-treated control group, amisulpride (10 mg/kg) increased extracellular dopamine levels. The use of amisulpride (0.5 to 15 mg/kg s.c.) caused a time- and dose-dependent increase in the stimulation-induced dopamine release. Amisulpride significantly reduced striatum ACh levels at 30 and 100 mg/kg (respectively 87.5% and 56.3% of control levels) [1]. In two acute studies, amisulpride (70 mg/kg, p.o.) significantly increased the duration of swimming behavior [F(3,28) = 45.90, p <0.01] [2].

References

[1]. Schoemaker H, et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997 Jan;280(1):83-97.

[2]. Pawar GR, et al. Evaluation of antidepressant like property of amisulpride per se and its comparison with fluoxetine and olanzapine using forced swimming test in albino mice. Acta Pol Pharm. 2009 May-Jun;66(3):327-31.

Properties

Molecular Weight

369.48

Chemical Formula

C17H27N3O4S

SMILES

CCN1CCCC1CNC(=O)C1=C(OC)C=C(N)C(=C1)S(=O)(=O)CC

Solubility

Soluble in DMSO (25mM) or water (25mM, 1eq. HCl)

IC50

Ki: 2.8 nM (D2 receptor), 3.2 nM (D3 receptor)

CAS NO.

71675-85-9

PubChem Substance ID

2159

Purity

>98%

Storage

-20°C

Shipping

Room Temperature

Research Use Only

For research use only

Target Details

Target

DRD2

Official Name

DRD2

Alternative Names

The dopamine receptor D2, also known as D2R, is a protein encoded by the DRD2 gene in humans. The dopamine D2 receptor is the main receptor for most antipsychotic drugs. The structure of DRD2 combined with the atypical antipsychotic drug risperidone has been determined.

This gene encodes the D2 subtype of the dopamine receptor, which is coupled to the Gi subtype of the G protein-coupled receptor. This G protein-coupled receptor can inhibit the activity of adenylate cyclase.

In mice, the modulation and exploration of D2R surface expression by neurocalcium sensor 1 (NCS-1) in the dentate gyrus is related to synaptic plasticity and memory formation. A recent study showed that D2R has a potential role in restoring forearm cortical fear memory.

In Drosophila, activation of D2 autoreceptors protects dopamine neurons from MPP+-induced cell death, a toxin that mimics the pathology of Parkinson's disease.