675599-62-9
Chemical Structure
PG01037 dihydrochloride
- CAS No.: 675599-62-9
- Formula:C26H28Cl4N4O
- Molecular Weight:554.34
IUPAC Name: (E)-N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)but-2-en-1-yl)-4-(pyridin-2-yl)benzamide dihydrochloride
InChIKey: DACFFMAXBWGOKQ-CZEFNJPISA-N
SMILES: O=C(NC/C=C/CN1CCN(C2=CC=CC(Cl)=C2Cl)CC1)C3=CC=C(C4=NC=CC=C4)C=C3.[H]Cl.[H]Cl
Biological Activity: PG01037 dihydrochloride is a blood-brain barrier-penetrant selective dopamine D3 receptor antagonist, and blocks D3R signaling in the nucleus accumbens, with a Ki of 0.7 nM. PG01037 dihydrochloride enhances psychostimulant-induced locomotion, locomotor sensitization, and dopamine release, and promotes excitation of D1-expressing medium spiny neurons through D1-like signaling. PG01037 dihydrochloride attenuates psychostimulant-associated reward and relapse behaviors, and alleviates MPTPp-induced motor impairment and dopaminergic neurodegeneration. PG01037 dihydrochloride can be used in research related to Parkinson's disease, addictive disorders, and cancer[1][2][3][4][6][7][8].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PG01037 dihydrochloride | 99.35% | PG01037 dihydrochloride is a blood-brain barrier-penetrant selective dopamine D3 receptor antagonist, and blocks D3R signaling in the nucleus accumbens, with a Ki of 0.7 nM. PG01037 dihydrochloride enhances psychostimulant-induced locomotion, locomotor sensitization, and dopamine release, and promotes excitation of D1-expressing medium spiny neurons through D1-like signaling. PG01037 dihydrochloride attenuates psychostimulant-associated reward and relapse behaviors, and alleviates MPTPp-induced motor impairment and dopaminergic neurodegeneration. PG01037 dihydrochloride can be used in research related to Parkinson's disease, addictive disorders, and cancer. | ||||||||||||||||||||
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References
- [1]. Manvich DF, et al. Selective D and D receptor antagonists oppositely modulate cocaine responses in mice via distinct postsynaptic mechanisms in nucleus accumbens. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2019 Jul;44(8):1445-1455.
- [2]. Elgueta D, et al. Pharmacologic antagonism of dopamine receptor D3 attenuates neurodegeneration and motor impairment in a mouse model of Parkinson's disease. Neuropharmacology. 2017 Feb 1;113:110-23.
- [3]. Higley AE, et al. PG01037, a novel dopamine D3 receptor antagonist, inhibits the effects of methamphetamine in rats. Journal of psychopharmacology (Oxford, England). 2011 Feb;25(2):263-73.
- [4]. Wang P, et al. Cortico-striatal gamma oscillations are modulated by dopamine D3 receptors in dyskinetic rats. Neural regeneration research. 2025 Apr 01;20(4):1164-1177.
- [6]. Hussein N, et al. The dopamine D receptor antagonists PG01037, NGB2904, SB277011A, and U99194 reverse ABCG2 transporter-mediated drug resistance in cancer cell lines. Cancer letters. 2017 Jun 28;396:167-180.
- [7]. Hussein N, et al. The dopamine (DA) D3 receptor antagonists (PG01037, NGB2904, SB-277011A, and U99194) significantly attenuate ABCG2-mediated multidrug resistance. Cancer Research. 2017 Jul 1;77(13_Supplement):1191-.
- [8]. Grundt P, 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. 2005 Feb 10;48(3):839-48. [Content Brief]
