Synonym
THPP-1; THPP 1; THPP1;
IUPAC/Chemical Name
[2-(6-Chloropyridin-3-yl)-4-(2-methoxyethoxy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl](imidazo[1,5-a]pyridin-1-yl)methanone
InChi Key
JBHLOPKIPKTRSU-UHFFFAOYSA-N
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
SMILES Code
O=C(N1CCC2=NC(C3=CC=C(Cl)N=C3)=NC(OCCOC)=C2C1)C4=C5C=CC=CN5C=N4
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
464.91
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Uliana DL, Martinez A, Grace AA. THPP-1 PDE10A inhibitor reverses the cognitive deficits and hyperdopaminergic state in a neurodevelopment model of schizophrenia. Schizophr Res. 2024 Dec;274:315-326. doi: 10.1016/j.schres.2024.10.003. Epub 2024 Oct 21. PMID: 39437478.
2: Vardigan JD, Lange HS, Tye SJ, Fox SV, Smith SM, Uslaner JM. Behavioral and qEEG effects of the PDE10A inhibitor THPP-1 in a novel rhesus model of antipsychotic activity. Psychopharmacology (Berl). 2016 Jul;233(13):2441-50. doi: 10.1007/s00213-016-4290-1. Epub 2016 Apr 27. PMID: 27117142.
3: Raheem IT, Breslin MJ, Fandozzi C, Fuerst J, Hill N, Huszar S, Kandebo M, Kim SH, Ma B, McGaughey G, Renger JJ, Schreier JD, Sharma S, Smith S, Uslaner J, Yan Y, Coleman PJ, Cox CD. Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5903-8. doi: 10.1016/j.bmcl.2012.07.072. Epub 2012 Jul 27. PMID: 22892116.
4: Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic- like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. 2013 Jan;64:215-23. doi: 10.1016/j.neuropharm.2012.06.013. Epub 2012 Jun 27. PMID: 22750078.
