For research use only.
Catalog No.S4358 Synonyms: Orap, R6238
CAS No. 2062-78-4
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 α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
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|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 α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.|
Pimozide blocks of peak HERG tail currents with IC50 of 18.1 nM in CHO cells. Pimozide blocks of peak HERG tail currents with IC50 of 18.1 nM in CHO cells. Pimozide (3 nM) is sufficient to inhibit HERG currents in CHO cells. Pimozide (10 μM) demonstrates little affinity for KvLQT1/minK or Kv1.5, inhibiting these channels by less than 30% in CHO cells.  Pimozide is a potent inhibitor of CYP2D6 (with Ki of 20.2 μM and 0.75 μM after 5 and 15 min preincubation, respectively) and a moderate inhibitor of CYP3A ( with Ki of 124 μM and 76.7 μM after 5 and 15 min preincubation, respectively). Pimozide is metabolized in humans via N-dealkylation and that this metabolic step is catalyzed principally by human CYP3A. 
Pimozide (0.4 mg/kg) blocks establishment but not expression of amphetamine-produced environment-specific conditioning in rats.  Pimozide (0.6 mg/kg) attenuates conditioned preparatory responses to a conditional stimulus (CS+) signaling delivery of a meal in rats.  Pimozide (1.0 mg/kg, i.p.) combined with cocaine (20 mg/kg, i.p.) attenuates significantly a cocaine-induced increase in the in vivo recovery of D2 dopamine (DA) in rats. 
-  Kang J, et al. Eur J Pharmacol, 2000, 392(3), 137-140.
-  Desta Z, et al. J Pharmacol Exp Ther, 1998, 285(2), 428-437.
-  Beninger RJ, et al. Science, 1983, 220(4603), 1304-1306.
-  Blackburn JR, et al. Behav Neurosci, 1987, 101(3), 352-360.
-  Parsons LH, et al. J Neurochem, 1993, 60(1), 376-379.
-  C E Ybema, et al. Eur J Pharmacol. 1994 Apr 21;256(2):141-7.
-  Nan Cai, et al. Am J Transl Res. 2017 Aug 15;9(8):3853-3866.
-  Erik A Nelson, et al. Blood. 2011 Mar 24;117(12):3421-9.
|In vitro||DMSO||92 mg/mL warmed (199.32 mM)|
|Ethanol||''9 mg/mL warmed|
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