| Bioactivity | 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. | ||||||||||||
| Invitro | 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; also has affinity at α1-adrenoceptor and 5-HT1A, with Kis of 39 nM and 310 nM, respectively[1]. Pimozide acts as an inhibitor of STAT3. Pimozide (0-15 μM) shows inhibitory of the proliferation of U2OS cells, with IC50 value at 24, 48, and 72 h of 22.16 ± 2.54, 17.49 ± 1.14 and 13.78 ± 0.34 μM, respectively. Pimozide (10 μM) inhibits the colony- and sphere-forming abilities of osteosarcoma cells. Pimozide (15 μM) induces G0/G1 phase cell cycle arrest, suppresses the extracellular signal-regulated kinase (Erk) signaling to inhibit cell viability, and produces ROS generation through inhibiting antioxidant enzyme gene catalase expression in osteosarcoma cells[2]. Pimozide acts as an inhibitor of STAT5. Pimozide reduces the expression of endogenous STAT5 target genes, and decreases STAT5 tyrosine phosphorylation[3]. | ||||||||||||
| Name | Pimozide | ||||||||||||
| CAS | 2062-78-4 | ||||||||||||
| Formula | C28H29F2N3O | ||||||||||||
| Molar Mass | 461.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |