产品
编 号：F611514
分子式：C13H21N3O
分子量：235.33
分子式：C13H21N3O
分子量：235.33
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CAS No: 710655-15-5
产品详情
生物活性：
PF-592379 is a potent dopamine D3 receptor agonist with an EC50 of 21 nM.
体内研究：
PF-592379 is an oral dopamine 3 agonist in rat, and dog. PF-592379 has low-moderate clearance relative to liver blood flow of 6.3 and 8.5 mL/min/kg in dog and 44.8 and 58.2 mL/min/kg in rat. It has high permeability in Caco-2 cells and is completely absorbed in rat and dog pharmacokinetic studies with an oral bioavailability of 28% in both rats and 61 and 87% in the dogs.
体外研究：
PF-592379 appears to be a full agonist (Emax=95%) when compared with the standard Pramipexole, a D2/D3 receptor agonist for the treatment of Parkinson’s disease. PF-592379 is a potent and selective dopamine 3 agonist with EC50 and Ki of 21 nM and 322 nM, respectively. In vitro binding assays show that PF-592379 (PF-592,379) selectively binds human D3 receptors with a high affinity (Ki=215 nM). Although PF-592379 also binds to human D4 receptors (Ki=4165 nM), it displays a 19-fold binding selectivity for human D3 over D4 receptors. PF-592379 fails to bind human D2 (Ki≥10 μM), D1 (Ki≥10 μM), or D5 (Ki≥10 μM) receptors at concentrations of up to 10 μM, and thus is at least 46-fold selective for D3 over D2, D1, and D5 receptors.
PF-592379 is a potent dopamine D3 receptor agonist with an EC50 of 21 nM.
体内研究：
PF-592379 is an oral dopamine 3 agonist in rat, and dog. PF-592379 has low-moderate clearance relative to liver blood flow of 6.3 and 8.5 mL/min/kg in dog and 44.8 and 58.2 mL/min/kg in rat. It has high permeability in Caco-2 cells and is completely absorbed in rat and dog pharmacokinetic studies with an oral bioavailability of 28% in both rats and 61 and 87% in the dogs.
体外研究：
PF-592379 appears to be a full agonist (Emax=95%) when compared with the standard Pramipexole, a D2/D3 receptor agonist for the treatment of Parkinson’s disease. PF-592379 is a potent and selective dopamine 3 agonist with EC50 and Ki of 21 nM and 322 nM, respectively. In vitro binding assays show that PF-592379 (PF-592,379) selectively binds human D3 receptors with a high affinity (Ki=215 nM). Although PF-592379 also binds to human D4 receptors (Ki=4165 nM), it displays a 19-fold binding selectivity for human D3 over D4 receptors. PF-592379 fails to bind human D2 (Ki≥10 μM), D1 (Ki≥10 μM), or D5 (Ki≥10 μM) receptors at concentrations of up to 10 μM, and thus is at least 46-fold selective for D3 over D2, D1, and D5 receptors.
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