ITI-214 | Selective PDE1 inhibitor

ITI-214 chemical structure

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ITI-214 (1642303-38-5) is an ultra-potent and selective inhibitor of phosphodiesterase 1 (PDE1) – Ki = 58 pM.1 Active in various animal models of motor and cognitive functions.1-3 It has also been shown to suppress inflammatory responses 4,5 and improve vascular function5.

References/Citations:

  1. Li al. (2016), Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases; J. Med. Chem., 59 1149
  2. Snyder al. (2016), Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats; Psychopharmacology (Berl), 233 3113
  3. Pekcec al. (2018), Targeting the dopamine D1 receptor or its downstream signalling by inhibiting phosphodiesterase-1 improves cognitive performance; Br. J. Pharmacol., 175 3021
  4. O’Brien al. (2020), Inhibition of calcium-calmodulin phosphodiesterase (PDE1) suppresses inflammatory responses; Mol. Cell Neurosci., 102 103449
  5. Golshiri al. (2021), Selective Phosphodiesterase 1 Inhibition Ameliorates Vascular Function, Reduces Inflammatory Response, and Lowers Blood Pressure in Aging Animals; J. Pharmacol. Exp. Ther., 378 173
1642303-38-5, ITI-214, ITI-214 supplier, Lenrispodun, Lenrispodun phosphate, Lenrispodun supplier, PDE1 inhibitor, selective PDE1 inhibitor
Alternate Name:
Lenrispodun phosphate

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ITI-214 (1642303-38-5) is an ultra-potent and selective inhibitor of phosphodiesterase 1 (PDE1) – Ki = 58 pM.1 Active in various animal models of motor and cognitive functions.1-3 It has also been shown to suppress inflammatory responses 4,5 and improve vascular function5.

References/Citations:

  1. Li al. (2016), Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases; J. Med. Chem., 59 1149
  2. Snyder al. (2016), Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats; Psychopharmacology (Berl), 233 3113
  3. Pekcec al. (2018), Targeting the dopamine D1 receptor or its downstream signalling by inhibiting phosphodiesterase-1 improves cognitive performance; Br. J. Pharmacol., 175 3021
  4. O’Brien al. (2020), Inhibition of calcium-calmodulin phosphodiesterase (PDE1) suppresses inflammatory responses; Mol. Cell Neurosci., 102 103449
  5. Golshiri al. (2021), Selective Phosphodiesterase 1 Inhibition Ameliorates Vascular Function, Reduces Inflammatory Response, and Lowers Blood Pressure in Aging Animals; J. Pharmacol. Exp. Ther., 378 173