PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research[1].

PDE10A-IN-2 hydrochloride (compound 14 3HCL; 2.5 mg/kg; oral administration; daily; for 3 weeks) treatment decreases the typical symptoms of PAH in rats[1].In Sprague-Dawley rats, the pharmacokinetic study of PDE10A-IN-2 hydrochloride (compound 14 3HCL; 10 mg/kg) shows the oral bioavailability up to ∼50%, and the T1/2 is 5.2 hours (p.o.), and the Cmax is 272 ng/mL[1].

[1]. Yuncong Yang, et al. Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension. Acta Pharm Sin B. 2020 Dec;10(12):2339-2347.