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]
^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.
PMID12086495.
^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.
ISBN0-444-51572-0
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]
^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.
PMID12086495.
^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.
ISBN0-444-51572-0