A PDE1 inhibitor
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ITI214 is an inhibitor of phosphodiesterase 1 (PDE1; Ki = 0.058 nM).1 It is selective for PDE1 over PDE2A, -3B, -4A, -5A, -6, -7B, -8A, -9A, -10A, and -11A (Kis = 0.16-18 ?M). ITI214 (3 and 6 mg/kg) enhances novel object recognition in rats. It increases prefrontal cortex cAMP and cGMP levels in mice when administered at a dose of 50 mg/kg.2 ITI214 (0.1, 3, and 10 mg/kg) reverses MK-801-induced decreases in spontaneous alteration in the T-maze continuous alternation task in mice.
1.Li, P., Zheng, H., Zhao, J., et al.Discovery of potent and selective inhibitors of phosphodiesterase 1 for the treatment of cognitive impairment associated with neurodegenerative and neuropsychiatric diseasesJ. Med. Chem.59(3)1149-1164(2016) 2.Pekcec, A., Schülert, N., Stierstorfer, B., et al.Targeting the dopamine D1 receptor or its downstream signalling by inhibiting phosphodiesterase-1 improves cognitive performanceBr. J. Pharmacol.175(14)3021-3033(2018)
LX1606 Hippurate (Telotristat etiprate)
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