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Chemical compound
PD-0298029
ethyl 3,6a,11,14-tetrahydro-9-methoxy-2-propyl-3,5-dimethyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-carboxylate
ChemSpider
Formula C 27 H 32 N 2 O 4
Molar mass 448.563 g·mol−1 3D model (
JSmol )
CCCc1c(c2c(n1C)cc(c3c2CN4CCc5cc(ccc5C4O3)OC)C)C(=O)OCC
CCCc1n(C)c5cc(C)c3OC4c2ccc(OC)cc2CCN4Cc3c5c1C(=O)OCC
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
Y Key:MTMZSGQXRVRKSY-UHFFFAOYSA-N
Y
(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.
[1]
[2]
[3]
See also
References
^ 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): 3094–102.
doi :
10.1021/jm011116o .
PMID
12086495 .
^ 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.
^ Progress in Medicinal Chemistry 43. (2005). Chapter 4, Muscarinic Receptor Subtype Pharmacology and Physiology, by Richard M Eglen. pp 128-129.
ISBN
0-444-51572-0
mAChRs Tooltip Muscarinic acetylcholine receptors
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PBID
PD-102,807
PD-0298029
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WIN-2299
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Precursors (and
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