| Identification | Back Directory | [Name]
N-{4-[4-(2,3-Dichlorophenyl)-piperazin-1-yl]-trans-but-2-enyl}-4-(pyridin-2-yl)benzamide dihydrochloride hydrate | [CAS]
675599-62-9 | [Synonyms]
PG-01037 (hydrochloride)
PG01037 dihydrochloride hydrate
N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)benzamide dihydrochloride hydrate
N-{4-[4-(2,3-Dichlorophenyl)-piperazin-1-yl]-trans-but-2-enyl}-4-(pyridin-2-yl)benzamide dihydrochloride hydrate | [Molecular Formula]
C26H30Cl4N4O2 | [MDL Number]
MFCD20527309 | [MOL File]
675599-62-9.mol | [Molecular Weight]
572.354 |
| Chemical Properties | Back Directory | [Melting point ]
230-232 °C(Solv: isopropanol (67-63-0)) | [storage temp. ]
2-8°C | [solubility ]
H2O: ≥8mg/mL at ~60°C | [form ]
powder | [color ]
white to tan |
| Hazard Information | Back Directory | [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). 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. 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. | [Uses]
PG01037 dihydrochloride is a selective D3DR antagonist. | [storage]
Store at -20°C | [References]
[1] PETER GRUNDT. 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]. Journal of Medicinal Chemistry, 2005, 48 3: 839-848. DOI: 10.1021/jm049465g
[2] LAURA ORIO. PRECLINICAL STUDY: FULL ARTICLE: The dopamine D3 receptor partial agonist CJB090 and antagonist PG01037 decrease progressive ratio responding for methamphetamine in rats with extended-access[J]. Addiction Biology, 2010, 15 3: 312-323. DOI: 10.1111/j.1369-1600.2010.00211.x
[3] DANIELA ELGUETA . Pharmacologic antagonism of dopamine receptor D3 attenuates neurodegeneration and motor impairment in a mouse model of Parkinson’s disease[J]. Neuropharmacology, 2017, 113: Pages 110-123. DOI: 10.1016/j.neuropharm.2016.09.028 |
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