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Pimozide-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]. | [IC 50]
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. DOI:10.1016/0014-2999(94)90238-0
[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. PMID:28861175
[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. DOI:10.1182/blood-2009-11-255232 |
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