A PDE10A inhibitor
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THPP-1

Item No. 34219

Technical Information
Formal Name
[2-(6-chloro-3-pyridinyl)-7,8-dihydro-4-(2-methoxyethoxy)pyrido[4,3-d]pyrimidin-6(5H)-yl]imidazo[1,5-a]pyridin-1-yl-methanone
CAS Number
1257051-63-0
Molecular Formula
C23H21ClN6O3
Formula Weight
Purity
≥98%
Formulation
A solid
λmax
221, 287 nm
SMILES
O=C(N1CC2=C(OCCOC)N=C(C3=CN=C(Cl)C=C3)N=C2CC1)C4=C5C=CC=CN5C=N4
InChi Code
InChI=1S/C23H21ClN6O3/c1-32-10-11-33-22-16-13-29(23(31)20-18-4-2-3-8-30(18)14-26-20)9-7-17(16)27-21(28-22)15-5-6-19(24)25-12-15/h2-6,8,12,14H,7,9-11,13H2,1H3
InChi Key
JBHLOPKIPKTRSU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    THPP-1 is an inhibitor of phosphodiesterase 10A (PDE10A; Ki = 1 nM).1 It is selective for PDE10A over PDE1A-9A and PDE11A (Kis = 44->50,000 nM for all). THPP-1 (3 mg/kg) decreases the number of avoidances in the conditioned avoidance response test in rats and reduces MK-801-induced increases in locomotor activity in mice.2 It improves novel object recognition in rats when administered at doses of 0.3 and 1 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Raheem, I.T., Breslin, M.J., Fandozzi, C., et alDiscovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. Bioorg. Med. Chem. Lett. 22(18), 5903-5908 (2012).

    2. Smith, S.M., Uslaner, J.M., Cox, C.D., et alThe novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology 64, 215-223 (2013).