Chemistry:Mardepodect
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| Other names | PDF-2545920 |
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| Formula | C25H20N4O |
| Molar mass | 392.462 g·mol−1 |
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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]
References
- ↑ "Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia". Journal of Medicinal Chemistry 52 (16): 5188–96. August 2009. doi:10.1021/jm900521k. PMID 19630403.
- ↑ , Patrick Robert & Caroline Proulx"Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl) phenoxy)methyl)quinoline" C CA patent 2673435 C, published 2008-07-17
- ↑ "Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis". Neuropharmacology 51 (2): 386–96. August 2006. doi:10.1016/j.neuropharm.2006.04.013. PMID 16780899.
- ↑ "Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia". The Journal of Pharmacology and Experimental Therapeutics 325 (2): 681–90. May 2008. doi:10.1124/jpet.107.132910. PMID 18287214. http://jpet.aspetjournals.org/content/jpet/325/2/681.full.pdf.
- ↑ Drahl, C (15 September 2008). "Rethinking Schizophrenia". Chemical & Engineering News 86 (37): 38–40. doi:10.1021/cen-v086n037.p038.
- ↑ "Mardepodect". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800025561.
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