PDE10A
Enzyme and protein-coding gene in humans
From Wikipedia, the free encyclopedia
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A is an enzyme that in humans is encoded by the PDE10A gene.[5][6]
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.[6][7]
Inhibitors
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- AMG-579[9]
- Balipodect (TAK-063): IC50 = 300 pM[10]
- Compound 96: IC50 = 700 pM, high selectivity against all other members of the PDE family[8]
- CPL500036[11]
- Mardepodect (PF-2545920)[12]
- MK-8189
- Papaverine[13]
- Tofisopam
- CPL 36
Research
Preliminary evidence indicates a possible link between PDE10A expression and obesity in mice and humans.[14] 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.[15]
