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{{drugbox {{drugbox
| verifiedrevid = 445907800 | verifiedrevid = 446393243
| IUPAC_name = ethyl 3,6a,11,14-tetrahydro-9-methoxy-2-propyl-3,5-dimethyl-(12H)-isoquinopyrrolobenzoxazine-1-carboxylate | IUPAC_name = ethyl 3,6a,11,14-tetrahydro-9-methoxy-2-propyl-3,5-dimethyl-(12H)-isoquinopyrrolobenzoxazine-1-carboxylate
| image = PD0298029_structure.png | image = PD0298029_structure.png

Revision as of 21:07, 18 September 2011

Pharmaceutical compound
PD-0298029
Identifiers
IUPAC name
  • ethyl 3,6a,11,14-tetrahydro-9-methoxy-2-propyl-3,5-dimethyl-(12H)-isoquinopyrrolobenzoxazine-1-carboxylate
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H32N2O4
Molar mass448.553 g/mol g·mol
3D model (JSmol)
SMILES
  • 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 (2002). "Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors". Journal of Medicinal Chemistry. 45 (14): 3094–102. PMID 12086495. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  2. Boehme TM, Angelli-Szafran CE, Corinne E, Hallak H and Schwarz RD. Analogs of M4 selective synthetic muscarinic receptor antagonists: Synthesis, binding and pharmacokinetic properties. Medicinal Chemistry Research. 2002; 11(8):423–433.
  3. Progress in Medicinal Chemistry 43. (2005). Chapter 4, Muscarinic Receptor Subtype Pharmacology and Physiology, by Richard M Eglen. pp 128-129. ISBN 0444515720
Acetylcholine receptor modulators
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
Nicotinic acetylcholine receptor modulators
nAChRsTooltip Nicotinic acetylcholine receptors
Agonists
(and PAMsTooltip positive allosteric modulators)
Antagonists
(and NAMsTooltip negative allosteric modulators)
Precursors
(and prodrugs)
See also
Receptor/signaling modulators
Muscarinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators
Categories:
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