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Short description: Chemical compound
PD-0298029 |
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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
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| ChemSpider | |
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| Chemical and physical data |
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| Formula | C27H32N2O4 |
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| Molar mass | 448.563 g·mol−1 |
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| 3D model (JSmol) | |
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CCCc1c(c2c(n1C)cc(c3c2CN4CCc5cc(ccc5C4O3)OC)C)C(=O)OCC
CCCc1n(C)c5cc(C)c3OC4c2ccc(OC)cc2CCN4Cc3c5c1C(=O)OCC
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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  YKey:MTMZSGQXRVRKSY-UHFFFAOYSA-N Y
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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
- ↑ "Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors". Journal of Medicinal Chemistry 45 (14): 3094–102. July 2002. 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
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| mAChRs | | Agonists | |
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| Antagonists |
- 3-Quinuclidinyl benzilate
- 4-DAMP
- Aclidinium bromide (+formoterol)
- Abediterol
- AF-DX 250
- AF-DX 384
- Ambutonium bromide
- Anisodamine
- Anisodine
- Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, [[Chemistry:Dimetdimetindene, Diphenhydramine|diphenhydramine]], doxylamine, meclizine, mepyramine (pyrilamine), mequitazine, perlapine, phenindamine, pheniramine, Phenyltoloxamine|Phenyltoloxamine]]]], promethazine, propiomazine, triprolidine)
- AQ-RA 741
- Atropine
- Atropine methonitrate
- Atypical antipsychotics (e.g., clozapine, Chemistry:Fluperlapine
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Precursors
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 | Original source: https://en.wikipedia.org/wiki/PD-0298029. Read more |
