Pimozide-d4

Names

[ Name ]:
Pimozide-d4

Biological Activity

[Description]:

Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> STAT

Research Areas >> Cancer

Research Areas >> Endocrinology

Signaling Pathways >> JAK/STAT Signaling >> STAT

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

Dopamine D2 receptor:1.4 nM (Ki)

opamine D3 receptor:2.5 nM (Ki)

opamine D1 receptor:588 nM (Ki)

α1-adrenoceptor:39 nM (Ki)

STAT3

STAT5

[References]

[1]. Ybema CE, et al. Adrenoceptors and dopamine receptors are not involved in the discriminative stimulus effect of the 5-HT1A receptor agonist flesinoxan. Eur J Pharmacol. 1994 Apr 21;256(2):141-7.

[2]. Cai N, et al. The STAT3 inhibitor pimozide impedes cell proliferation and induces ROS generation in human osteosarcoma by suppressing catalase expression. Am J Transl Res. 2017 Aug 15;9(8):3853-3866. eCollection 2017.

[3]. Erik A. Nelson, et al. The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors. Blood. 2011 Mar 24; 117(12): 3421-3429.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₂₅D₄F₂N₃O

[ Molecular Weight ]:
465.57

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.