A dopamine D2 and D3 receptor partial agonist and 5-HT1A agonist (EC50s = 10

Pardoprunox (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
269718-83-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Pardoprunox is a partial agonist of dopamine D2 and D3 receptors (EC50s = 10 and 0.63 nM, respectively) and a full agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 501 nM) in radioligand binding assays.{40413} It is selective for dopamine D2 and D3 and 5-HT1A receptors over a panel of neurotransmitter receptors (Kis = >1,000 nM). Pardoprunox reduces the accumulation of cAMP induced by forskolin (Item No. 11018) in a concentration-dependent manner and blocks quinpirole-induced inhibition of dopamine release (pA2 = 8.5) in rat striatal slices. Pardoprunox increases contralateral turning behavior in a 6-OHDA rat model of Parkinson’s disease (ED50 = 0.03 mg/kg).{40414} It also reduces hyperlocomotion induced by amphetamine (Item Nos. 14204 | 15650 | ISO60188) and induces 5-HT1A-mediated flat body posturing and lower lip retraction in rats. Pardoprunox (0.01-0.3 mg/kg) increases locomotor activity in a marmoset model of Parkinson’s disease induced by MPTP in a dose-dependent manner. Formulations containing pardoprunox are under clinical investigation for the treatment of Parkinson’s disease-associated motor fluctuations.{40415}  

 

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Description

A dopamine D2 and D3 receptor partial agonist and 5-HT1A agonist (EC50s = 10, 0.63, and 501 nM, respectively); selective for dopamine D2, D3, and 5-HT1A receptors over a panel of neurotransmitter receptors (Kis = >1000 nM); increases contralateral turning behavior in a 6-OHDA rat model of Parkinson’s disease (ED50 = 0.03 mg/kg); reduces amphetamine-induced hyperlocomotion and induces 5-HT1A-mediated flat body posturing and lower lip retraction in rats; dose-dependently increases locomotor activity in an MPTP-induced marmoset model of Parkinson’s disease when administered at doses ranging from 0.01-0.3 mg/kg

Formal name: 7-(4-methyl-1-piperazinyl)-2(3H)-benzoxazolone, monohydrochloride

Synonyms:  DU-126891|SLV 308

Molecular weight: 269.7

CAS: 269718-83-4

Purity: ≥98%

Formulation: A crystalline solid

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

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