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PD-0298029

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Chemical compound

Pharmaceutical compound
PD-0298029
Identifiers
IUPAC name
  • ethyl 3,6a,11,14-tetrahydro-9-methoxy-2-propyl-3,5-dimethyl-(12H)-isoquinopyrrolobenzoxazine-1-carboxylate
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H32N2O4
Molar mass448.563 g·mol
3D model (JSmol)
SMILES
  • CCCc1c(c2c(n1C)cc(c3c2CN4CCc5cc(ccc5C4O3)OC)C)C(=O)OCC

  • CCCc1n(C)c5cc(C)c3OC4c2ccc(OC)cc2CCN4Cc3c5c1C(=O)OCC
InChI
  • InChI=1S/C27H32N2O4/c1-6-8-21-24(27(30)32-7-2)23-20-15-29-12-11-17-14-18(31-5)9-10-19(17)26(29)33-25(20)16(3)13-22(23)28(21)4/h9-10,13-14,26H,6-8,11-12,15H2,1-5H3
  • Key:MTMZSGQXRVRKSY-UHFFFAOYSA-N
  (verify)

PD-0298029 is a drug which acts as a selective antagonist for the muscarinic acetylcholine receptor M4. It was developed for the treatment of Parkinson's disease, but poor bioavailability and rapid metabolism in animal studies have meant its use is largely limited to in vitro research into the M4 and other muscarinic receptors.

See also

References

  1. Böhme TM, Augelli-Szafran CE, Hallak H, Pugsley T, Serpa K, Schwarz RD (July 2002). "Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors". Journal of Medicinal Chemistry. 45 (14): 3094–3102. doi:10.1021/jm011116o. PMID 12086495.
  2. Boehme TM, Angelli-Szafran CE, Corinne E, Hallak H, Schwarz RD (January 2002). "Analogs of M4 selective synthetic muscarinic receptor antagonists: Synthesis, binding and pharmacokinetic properties". Medicinal Chemistry Research. 11 (8): 423–433.
  3. Eglen RM (2005). "Muscarinic receptor subtype pharmacology and physiology". Progress in Medicinal Chemistry. 43. Amsterdam London: Elsevier Science: 105–136 (128). doi:10.1016/S0079-6468(05)43004-0. ISBN 978-0-444-51572-8. PMID 15850824.
Muscarinic acetylcholine receptor modulators
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(and prodrugs)
See also
Receptor/signaling modulators
Nicotinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators


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