【产品介绍】：

生物活性：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].
IC50 & Target[1][2][3]
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
Clinical Trial
NCT NumberSponsorConditionStart DatePhaseNCT02374567Hannover Medical SchoolDementia|Depression|Schizophrenia|Psychosomatic Disorders|Anxiety DisordersJanuary 2015Phase 3NCT02463825University of Calgary|Hotchkiss Brain Institute, University of CalgaryAmyotrophic Lateral Sclerosis (ALS)April 2015Phase 2NCT00374244Yale University|Stanley Medical Research InstituteSchizophreniaJanuary 2004Phase 2 NCT05507372Applied Biology, Inc.|Jupiter Wellness, Inc.Tinnitus, SubjectiveOctober 1, 2022Not ApplicableNCT00158223Icahn School of Medicine at Mount Sinai|National Institute of Mental Health (NIMH)Schizophrenia|Psychotic DisordersOctober 2004Phase 4NCT02600741Janssen Scientific Affairs, LLCSchizophreniaJuly 24, 2015NCT03272503University of Calgary|ALS Canada|Brain CanadaALS|Amyotrophic Lateral SclerosisOctober 27, 2017Phase 2NCT05716854Food and Drug Administration (FDA)|Spaulding Clinical Research LLCDrug-induced QT Prolongation|Pharmacokinetics|PharmacodynamicsMarch 21, 2023Phase 1NCT00004652National Center for Research Resources (NCRR)|University of Rochester|Office of Rare Diseases (ORD)Tourette SyndromeFebruary 1993Phase 2NCT02307396Technical University of MunichSchizophrenia|Schizophrenia and Disorders With Psychotic Features|Schizoaffective DisordersFebruary 1, 2015Phase 4
分子量：465.57
Formula：C28H25D4F2N3O
CAS 号：1803193-57-8
非标记 CAS：2062-78-4
性状：固体
颜色：White to off-white
中文名称：匹莫齐特 d4
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Powder：-20°C：3 years
In solvent：-80°C：6 months，-20°C：1 month
纯度 & 产品资料
纯度： ≥98.0%
参考文献
[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.
 [Content Brief]
[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.
 [Content Brief]
[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.
 [Content Brief]