Mardepodect

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 PDE_10A subtype.^[1]

Mardepodect

Clinical data
Other names	PF-2545920
ATC code	None
Legal status
Legal status	Investigational
Identifiers
IUPAC name 2-(4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)phenoxymethyl)quinoline
CAS Number	898562-94-2 N
PubChem CID	11581936
DrugBank	DB08387 N
ChemSpider	9756702 N
UNII	R9Y8EY0G42
KEGG	D11171
ChEMBL	ChEMBL1642569 N
CompTox Dashboard (EPA)	DTXSID001025873
Chemical and physical data
Formula	C25H20N4O
Molar mass	392.462 g·mol−1
3D model (JSmol)	Interactive image
SMILES n3c1ccccc1ccc3COc5ccc(cc5)-c2nn(C)cc2-c4ccncc4
InChI 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
NY (what is this?)  (verify)

The PDE_10A 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 PDE_10A inhibitors such as papaverine have been shown to produce antipsychotic effects in animal models,^[3] and more potent and selective PDE_10A inhibitors are a current area of research for novel antipsychotic drugs which act through a different pathway to conventional dopamine or 5-HT_2A antagonist drugs and may have a more favourable side effects profile.^[4]

Mardepodect is currently one of the furthest advanced PDE_10A 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

• Balipodect
• MK-8189