PDE10A
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cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A is an enzyme that in humans is encoded by the PDE10A gene.
Various cellular responses are regulated by the second messengers cAMP and cGMP. Phosphodiesterases, such as PDE10A, eliminate cAMP- and cGMP-mediated intracellular signaling by hydrolyzing the cyclic nucleotide to the corresponding nucleoside 5-prime monophosphate.
Inhibitors
- AMG-579
- Balipodect (TAK-063): IC50 = 300 pM
- Compound 96: IC50 = 700 pM, high selectivity against all other members of the PDE family
- CPL500036
- Mardepodect (PF-2545920)
- MK-8189
- Papaverine
- Tofisopam
- CPL 36
Research
Preliminary evidence indicates a possible link between PDE10A expression and obesity in mice and humans. PDE10A is a regulatory protein involved in the signaling of the striatum, a region of the brain important for controlling movement and cognition. Dysfunction of the striatum has been linked to the development of schizophrenia. Inhibition of PDE10A has been identified as a potential treatment for the disorder, and an inhibitor compound (MK-8189) is as of February 2023 in Phase 2b clinical development for the treatment of schizophrenia.
Further reading
This article incorporates text from the United States National Library of Medicine, which is in the public domain.