Mardepodect

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Mardepodect
File:PF-2545920.svg
Clinical data
Other namesPF-2545920
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
  • 2-(4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)phenoxymethyl)quinoline
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
E number{{#property:P628}}
CompTox Dashboard (EPA)
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Chemical and physical data
FormulaC25H20N4O
Molar mass392.462 g·mol−1
3D model (JSmol)
  • n3c1ccccc1ccc3COc5ccc(cc5)-c2nn(C)cc2-c4ccncc4
  • 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 N
  • Key:AZEXWHKOMMASPA-UHFFFAOYSA-N N
 NcheckY (what is this?)  (verify)

Mardepodect (developmental code name PF-2545920) is a drug which was developed by Pfizer for the treatment of schizophrenia. It acts as a phosphodiesterase inhibitor selective for the PDE10A subtype.[1]

The PDE10A enzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens and olfactory tubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitive medium spiny neurons in the striatum which are known to be targets of conventional antipsychotic drugs.[2] Older PDE10A inhibitors such as papaverine have been shown to produce antipsychotic effects in animal models,[3] and more potent and selective PDE10A inhibitors are a current area of research for novel antipsychotic drugs which act through a different pathway to conventional dopamine or 5-HT2A antagonist drugs and may have a more favourable side effects profile.[4]

Mardepodect is currently one of the furthest advanced PDE10A inhibitors in development and has progressed through to Phase II clinical trials in humans.[5] In 2017, development of mardepodect for the treatment of schizophrenia and Huntington's disease was discontinued.[6]

See also

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References

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  2. ^ CA 2673435 C, Vorhoest, Patrick Robert & Proulx, Caroline, "Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl) phenoxy)methyl)quinoline", published Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). 
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