PF-2545920, also known as Mardepodect, is a phosphodiesterase inhibitor selective for the PDE10A subtype, which is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. PDE10A inhibitors have shown behavioral effects in rodent models that predict antipsychotic efficacy. PF-2545920 is active in a range of antipsychotic models, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.
Chemical Formula: C25H20N4O
Exact Mass: 392.16371
Molecular Weight: 392.0
Elemental Analysis: C, 76.51; H, 5.14; N, 14.28; O, 4.08
MP 10, Mardepodect
Chemical Name: 2-(4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)phenoxymethyl)quinoline
InChi Code: InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3
Appearance: Solid powder
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, not in water
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
In the conditioned avoidance response assay (CAR), PF-2545920 is active with an ED50 of 1 mg/kg. Administration of PF-2545920 to mice causes a dose dependent increase in striatal cGMP.
Hamaguchi W, Masuda N, Samizu K, Mihara T, Takama K, Watanabe T.Synthesis and in vivo evaluationof novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-13. PubMed PMID: 25450629.
Lin SF, Labaree D, Chen MK, Holden D, Gallezot JD, Kapinos M, Teng JK, Najafzadeh S, Plisson C, Rabiner EA, Gunn RN, Carson RE, Huang Y. Further evaluation of [11C]MP-10 as a radiotracer for phosphodiesterase 10A: PET imaging study in rhesus monkeys and brain tissue metabolite analysis. Synapse. 2015 Feb;69(2):86-95. doi: 10.1002/syn.21792. Epub 2014 Dec 11. PubMed PMID: 25450608; PubMed Central PMCID: PMC4275380.
Natesan S, Ashworth S, Nielsen J, Tang SP, Salinas C, Kealey S, Lauridsen JB, Stensbøl TB, Gunn RN, Rabiner EA, Kapur S. Effect of chronic antipsychotic treatment on striatal phosphodiesterase 10A levels: a [¹¹C]MP-10 PET rodent imaging study with ex vivo confirmation. Transl Psychiatry. 2014 Apr 1;4:e376. doi: 10.1038/tp.2014.17. PubMed PMID: 24690597; PubMed Central PMCID: PMC4012281.
Uthayathas S, Masilamoni GJ, Shaffer CL, Schmidt CJ, Menniti FS, Papa SM. Phosphodiesterase 10A inhibitor MP-10 effects in primates: comparison with risperidone and mechanistic implications. Neuropharmacology. 2014 Feb;77:257-67. PubMed PMID: 24490227; PubMed Central PMCID: PMC3934827.
Bleickardt CJ, Kazdoba TM, Jones NT, Hunter JC, Hodgson RA. Antagonism of the adenosine A2A receptor attenuates akathisia-like behavior induced with MP-10 or aripiprazole in a novel non-human primate model. Pharmacol Biochem Behav. 2014 Mar;118:36-45. doi: 10.1016/j.pbb.2013.10.030. Epub 2013 Nov 8. PubMed PMID: 24211858.
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