Home Neuronal Signaling Dopamine Receptor antagonist - Adrenergic Receptor antagonist - 5-HT Receptor antagonist - STAT inhibitor Pimozide For research use only.

Pimozide

Synonyms: Orap, R6238

Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.

Pimozide Chemical Structure

Pimozide Chemical Structure

CAS No. 2062-78-4

Purity & Quality Control

Pimozide Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

Biological Activity

Description Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Targets
STAT3 [1] STAT5 [2] Dopamine D3 receptor [3]
(Cell-free assay)		 Dopamine D2 receptor [3]
(Cell-free assay)		 α1-adrenoceptor [3]
(Cell-free assay)		 Click to View More Targets
0.83 nM(Ki) 3.0 nM(Ki) 39 nM(Ki)
In vitro
In vitro

Pimozide, a STAT5 inhibitor, has no effect on prolactin-induced ERα phosphorylation.[4]
Cell Research Cell lines MMQ rat prolactinoma cell line
Concentrations 5 µM
Incubation Time --
Method

MMQ cells were treated with PRL (20 ng/ml) in the absence and presence of the JAK2 inhibitor AG-490 (50 μM), the PI3K inhibitor wortmannin (0.5 µM), the MEK inhibitor U0126 (10 µM) or the STAT5 inhibitor pimozide (5 µM).

(Data sourced from selleck products)

Chemical Information & Solubility

Molecular Weight 461.55 Formula

C28H29F2N3O
CAS No. 2062-78-4 SDF Download Pimozide SDF
Smiles FC1=CC=C(C=C1)C(CCCN2CCC(CC2)N3C(=O)NC4=CC=CC=C34)C5=CC=C(F)C=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (194.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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