Gemlapodect

Gemlapodect (RO554965) is an inhibitor of phosphodiesterase 10A (PDE10A). Gemlapodect can be used for researching schizophrenia[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Neurological Disease

PDE10A

Gemlapodect (5-15 mg；口服；一天一次持续 6 周) 显著改善儿童期发作性流利性障碍 (COFD) 患者的工作和生活社会功能，显示出生物安全性[2]。 Gemlapodect (10 mg/kg；口服；单剂量) 在 9 周龄的 SD 大鼠中不改变葡萄糖耐受性。[2]。 Gemlapodect (0.3 mg/kg；口服；一天一次持续 8 天) 在 10 周龄的 SD 大鼠中诱导葡萄糖耐受性轻微改善，空腹血糖无变化，空腹胰岛素降低[2]。 Animal Model: Adult male patients with COFD (18-50 years old)[2]. Dosage: 5-15 mg. Administration: Oral gavage; once daily for 6 weeks. Result: Improved the Stuttering, work, social life, family life and home responsibilities of COFD patients and showed biosafety. Animal Model: 9 weeks or 10 weeks male SD rats[2]. Dosage: 0.3 mg/kg or 10 mg/kg. Administration: Oral gavage; once daily for 1 or 8 days. Result: Showed insignificantly change of glucose tolerance in healthy rats.

[1]. Zagorska A, et al. Phosphodiesterase 10 Inhibitors - Novel Perspectives for Psychiatric and Neurodegenerative Drug Discovery. Curr Med Chem. 2018;25(29):3455-3481.  

[2]. GARIBALDI, et al. METHODS FOR THE TREATMENT OF CHILDHOOD-ONSET FLUENCY DISORDER. World Intellectual Property Organization. WO2022162193