Potent and selective PDE10A inhibitor (IC50values are 7.28, 239, 779, 919, 3100 and 3700 nM at PDE10A, 2A, 11A, 5A, 7B and 3A respectively and >5000 nM at PDE1B, 4A, 6, 8A and 9A). Reverses MK 801-induced hyperactivityin vivo.
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of phosphodiesterase 10A
Associated Targets
PDE11ATchem Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A 2 Activities
1.Höfgen N, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Tremmel P, Pangalos MN, Marquis KL et al.. (2010) Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.. J Med Chem, 53 (11):(4399-411). [PMID:20450197]
2.Hennenberg M, Schott M, Kan A, Keller P, Tamalunas A, Ciotkowska A, Rutz B, Wang Y, Strittmatter F, Herlemann A et al.. (2016) Inhibition of Adrenergic and Non-Adrenergic Smooth Muscle Contraction in the Human Prostate by the Phosphodiesterase 10-Selective Inhibitor TC-E 5005.. Prostate, 76 (15):(1364-74). [PMID:27418235]
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