Pimozide

For research use only.

Catalog No.S4358 Synonyms: Orap, R6238

Pimozide Chemical Structure

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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Biological Activity

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.
Targets
STAT3 [6]
()
STAT5 [6]
()
Dopamine D3 receptor [6]
(Cell-free assay)
Dopamine D2 receptor [6]
(Cell-free assay)
5-HT1A [6]
(Cell-free assay)
0.83 nM(Ki) 3.0 nM(Ki) 310 nM(Ki)
In vitro

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. [1] 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. [2]

In vivo

Pimozide (0.4 mg/kg) blocks establishment but not expression of amphetamine-produced environment-specific conditioning in rats. [3] Pimozide (0.6 mg/kg) attenuates conditioned preparatory responses to a conditional stimulus (CS+) signaling delivery of a meal in rats. [4] 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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 92 mg/mL warmed (199.32 mM)
Water Insoluble
Ethanol ''9 mg/mL warmed

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.55
Formula

C28H29F2N3O

CAS No. 2062-78-4
Storage powder
in solvent
Synonyms Orap, R6238
Smiles FC1=CC=C(C=C1)C(CCCN2CCC(CC2)N3C(=O)NC4=CC=CC=C34)C5=CC=C(F)C=C5

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Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID