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Literature summary for 3.1.4.17 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
Search for more literature for 3.1.4.17

Application

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

Inhibitors

Inhibitors Comment Organism Structure
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)

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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