A selective dopamine D3 receptor antagonist (Kis = 0.7

PG-01037 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
675599-62-9
Storage:
-20
UN-No:
Non-Hazardous - /

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).{34174} 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.{36955} 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.{36956}  

 

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Description

A selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively); inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM); reduces progressive-ratio methamphetamine self-administration in rats allowed extended access at 32 mg/kg; 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 MPTP-induced Parkinson’s disease

Formal name: N-[(2E)-4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridinyl)-benzamide, dihydrochloride

Synonyms: 

Molecular weight: 554.3

CAS: 675599-62-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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