A selective dopamine D3 receptor antagonist
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PG-01037 (hydrochloride)

Item No. 22079

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2E)-4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridinyl)-benzamide, dihydrochloride
CAS Number
675599-62-9
Molecular Formula
C26H26Cl2N4O • 2HCl
Formula Weight
554.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mLDMSO: 30 mg/mLEthanol: 2 mg/mL
λmax
254, 284 nm
SMILES
ClC1=CC=CC(N2CCN(C/C=C/CNC(C3=CC=C(C4=NC=CC=C4)C=C3)=O)CC2)=C1Cl.Cl.Cl
InChi Code
InChI=1S/C26H26Cl2N4O.2ClH/c27-22-6-5-8-24(25(22)28)32-18-16-31(17-19-32)15-4-3-14-30-26(33)21-11-9-20(10-12-21)23-7-1-2-13-29-23;;/h1-13H,14-19H2,(H,30,33);2*1H/b4-3+;;
InChi Key
DACFFMAXBWGOKQ-CZEFNJPISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $203

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    25 mg

    $462

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    Product Description

    PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively).1 It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access.2 It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson's disease induced by MPTP.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grundt, P., Carlson, E.E., Cao, J., et al. Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor. J. Med. Chem. 48(3), 839-848 (2005).

    2. Orio, L., Wee, S., Newman, A.H., et al. The dopamine D3 receptor partial agonist CJB090 and antagonist PG01037 decrease progressive ratio responding for methamphetamine in rats with extended-access. Addict. Biol. 15(3), 312-323 (2010).

    3. Elgueta, D., Aymerich, M.S., Contreras, F., et al. Pharmacologic antagonism of dopamine receptor D3 attenuates neurodegeneration and motor impairment in a mouse model of Parkinson’s disease. Neuropharmacology 113(Pt A), 110-123 (2017).