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Literature summary extracted from

  • Schmidt, C.J.; Chapin, D.S.; Cianfrogna, J.; Corman, M.L.; Hajos, M.; Harms, J.F.; Hoffman, W.E.; Lebel, L.A.; McCarthy, S.A.; Nelson, F.R.; Proulx-LaFrance, C.; Majchrzak, M.J.; Ramirez, A.D.; Schmidt, K.; Seymour, P.A.; Siuciak, J.A.; Tingley, F.D.; Williams, R.D.; Verhoest, P.R.; Menniti, F.S.
    Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia (2008), J. Pharmacol. Exp. Ther., 325, 681-690.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.1.4.17 medicine inhibition of PDE10A represents an important new target for the treatment of schizophrenia and related disorders of basal ganglia function Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.17 2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid potent inhibitor Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.4.17 additional information Rattus norvegicus PDE10A regulates both cAMP and cGMP signaling cascades to impact early signal processing in the corticostriatothalamic circuit ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.17 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.4.17 corpus striatum PDE10A is highly expressed in the medium spiny neurons of the striatum Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.17 3',5'-cAMP + H2O
-
 Rattus norvegicus 5'-AMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O
-
 Rattus norvegicus 5'-GMP
-
 ?
3.1.4.17 additional information PDE10A regulates both cAMP and cGMP signaling cascades to impact early signal processing in the corticostriatothalamic circuit Rattus norvegicus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.17 cyclic nucleotide phosphodiesterase 10A
-
 Rattus norvegicus
3.1.4.17 PDE10A
-
 Rattus norvegicus
3.1.4.17 phosphodiesterase 10A
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.17 0.000001
-
 the IC50 of the compound for inhibition of PDE10A in vitro is less than 1 nM Rattus norvegicus 2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid