PF-592379

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的多巴胺 D3 受体激动剂，EC50 为 21 nM；分别比 D2 和 D4 多巴胺受体表现出 >470 和 180 倍的功能选择性。

A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM; displays >470 and 180-fold functional selectivity over D2 and D4 dopamine receptors, respectively; demonstrates activity in animal models of male erectile dysfunction.Sexual Dysfunction Preclinical

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 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.

PF592379 | PF 592379

GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

Endocrinology

Sexual Dysfunction

710655-15-5

235.331

C13H21N3O

>98% (HPLC)

——

CCCN1CC(OCC1C)C2=CN=C(C=C2)N

5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine

(-20℃)

With Ice Pack

≥ 2 years