PD-102,807 is a drug which acts as a selective antagonist for the muscarinic acetylcholine receptor M4.[1][2][3] It is used in scientific research for studying the effects of the different muscarinic receptor subtypes in the body and brain.[4][5][6][7]

PD-102,807
Identifiers
  • ethyl 3,6a,11,14-tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H24N2O4
Molar mass392.455 g·mol−1
3D model (JSmol)
  • CCOC(=O)c1c(C)[nH]c(c1c3C5)ccc3OC2N5CCc4c2ccc(OC)c4
  • InChI=1S/C23H24N2O4/c1-4-28-23(26)20-13(2)24-18-7-8-19-17(21(18)20)12-25-10-9-14-11-15(27-3)5-6-16(14)22(25)29-19/h5-8,11,22,24H,4,9-10,12H2,1-3H3 checkY
  • Key:VDDUJINYXKGZLV-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

See also

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References

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  1. ^ Olianas MC, Onali P (1999). "PD 102807, a novel muscarinic M4 receptor antagonist, discriminates between striatal and cortical muscarinic receptors coupled to cyclic AMP". Life Sciences. 65 (21): 2233–40. doi:10.1016/S0024-3205(99)00488-9. PMID 10576595.
  2. ^ Varoli L, Andreani A, Burnelli S, Granaiola M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Bedini A, Fazio N, Spampinato S (May 2008). "Diphenidol-related diamines as novel muscarinic M4 receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 18 (9): 2972–6. doi:10.1016/j.bmcl.2008.03.061. PMID 18395442.
  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. PMID 12086495.
  4. ^ Pujol Lereis VA, Hita FJ, Gobbi MD, Verdi MG, Rodriguez MC, Rothlin RP (March 2006). "Pharmacological characterization of muscarinic receptor subtypes mediating vasoconstriction of human umbilical vein". British Journal of Pharmacology. 147 (5): 516–23. doi:10.1038/sj.bjp.0706654. PMC 1616972. PMID 16444291.
  5. ^ Hogan K, Markos F (February 2007). "Muscarinic type 1 receptors mediate part of nitric oxide's vagal facilitatory effect in the isolated innervated rat right atrium". Nitric Oxide: Biology and Chemistry. 16 (1): 110–7. doi:10.1016/j.niox.2006.05.005. PMID 16843016.
  6. ^ Myslivecek J, Klein M, Novakova M, Ricny J (July 2008). "The detection of the non-M2 muscarinic receptor subtype in the rat heart atria and ventricles". Naunyn-Schmiedeberg's Archives of Pharmacology. 378 (1): 103–16. doi:10.1007/s00210-008-0285-8. PMID 18443764.
  7. ^ Lau BK, Vaughan CW (November 2008). "Muscarinic modulation of synaptic transmission via endocannabinoid signalling in the rat midbrain periaqueductal gray". Molecular Pharmacology. 74 (5): 1392–8. doi:10.1124/mol.108.045872. PMID 18678620.