Date published: 2026-3-31

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PD 102807 (CAS 23062-91-1)

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Alternate Names:
3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-carboxylic acid, ethyl ester
Application:
PD 102807 is a selective mAChR M4 antagonist
CAS Number:
23062-91-1
Purity:
≥98%
Molecular Weight:
392.45
Molecular Formula:
C23H24N2O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.

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PD 102807, identified as a highly specific antagonist targeting the mAChR M4 muscarinic receptor, stands out due to its remarkable selectivity in binding interactions. This compound is characterized by its differential inhibition potency across various subtypes of muscarinic acetylcholine receptors (mAChRs), as evidenced by its IC50 values: 91 nM for mAChR M4, 6559 nM for mAChR M1, 3441 nM for mAChR M2, 950 nM for mAChR M3, and 7412 nM for mAChR M5. These values illuminate PD 102807′s pronounced affinity for the M4 receptor over other muscarinic receptor subtypes, showcasing its utility in dissecting the roles and mechanistic actions of M4 receptors in physiological and pathophysiological processes. The specificity of PD 102807 for the M4 subtype provides a critical tool in the investigation of muscarinic receptor pharmacology, enabling researchers to elucidate the distinct functions and signaling pathways mediated by M4 receptors apart from those modulated by M1, M2, M3, and M5 receptors. This selective antagonism is instrumental in advancing our comprehension of the nuanced regulatory roles that muscarinic receptors play in neurotransmission and cellular signaling, thereby enhancing the exploration of targeted interventions in research applications where precise modulation of receptor activity is paramount.


PD 102807 (CAS 23062-91-1) References

  1. Characterization of the muscarinic receptor in isolated uterus of sham operated and ovariectomized rats.  |  Choppin, A., et al. 1999. Br J Pharmacol. 127: 1551-8. PMID: 10455309
  2. PD 102807, a novel muscarinic M4 receptor antagonist, discriminates between striatal and cortical muscarinic receptors coupled to cyclic AMP.  |  Olianas, MC. and Onali, P. 1999. Life Sci. 65: 2233-40. PMID: 10576595
  3. Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.  |  Böhme, TM., et al. 2002. J Med Chem. 45: 3094-102. PMID: 12086495
  4. Pharmacological characterization of muscarinic receptor subtypes mediating vasoconstriction of human umbilical vein.  |  Pujol Lereis, VA., et al. 2006. Br J Pharmacol. 147: 516-23. PMID: 16444291
  5. Muscarinic type 1 receptors mediate part of nitric oxide's vagal facilitatory effect in the isolated innervated rat right atrium.  |  Hogan, K. and Markos, F. 2007. Nitric Oxide. 16: 110-7. PMID: 16843016
  6. The detection of the non-M2 muscarinic receptor subtype in the rat heart atria and ventricles.  |  Myslivecek, J., et al. 2008. Naunyn Schmiedebergs Arch Pharmacol. 378: 103-16. PMID: 18443764
  7. Betel quid extract promotes oral cancer cell migration by activating a muscarinic M4 receptor-mediated signaling cascade involving SFKs and ERK1/2.  |  Chiu, CC., et al. 2010. Biochem Biophys Res Commun. 399: 60-5. PMID: 20638369
  8. Contribution of muscarinic M1 receptors to the cholinergic suppression of synaptic responses in layer II of the entorhinal cortex.  |  Barrett, SG. and Chapman, CA. 2013. Neurosci Lett. 554: 11-5. PMID: 24012918
  9. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.  |  Croy, CH., et al. 2016. Eur J Pharmacol. 782: 70-6. PMID: 27085897
  10. Autoradiography of 3H-pirenzepine and 3H-AFDX-384 in Mouse Brain Regions: Possible Insights into M1, M2, and M4 Muscarinic Receptors Distribution.  |  Valuskova, P., et al. 2018. Front Pharmacol. 9: 124. PMID: 29515448
  11. Novel regulatory systems for acetylcholine release in rat striatum and anti-Alzheimer's disease drugs.  |  Muramatsu, I., et al. 2019. J Neurochem. 149: 605-623. PMID: 30968952
  12. Central muscarinic receptor subtypes (M1 and M3) involved in carbacol-induced hypophagia in neonatal broiler chicken.  |  Zendehdel, M., et al. 2020. Int J Neurosci. 130: 204-211. PMID: 31517560
  13. Muscarinic acetylcholine receptor regulates self-renewal of early erythroid progenitors.  |  Trivedi, G., et al. 2019. Sci Transl Med. 11: PMID: 31554738
  14. Striatal and nigral muscarinic type 1 and type 4 receptors modulate levodopa-induced dyskinesia and striato-nigral pathway activation in 6-hydroxydopamine hemilesioned rats.  |  Brugnoli, A., et al. 2020. Neurobiol Dis. 144: 105044. PMID: 32798726
  15. PD 102807 Induces M3 mAChR-Dependent GRK-/Arrestin-Biased Signaling in Airway Smooth Muscle Cells.  |  Tompkins, E., et al. 2022. Am J Respir Cell Mol Biol. 67: 550-561. PMID: 35944139

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PD 102807, 1 mg

sc-203659
1 mg
$202.00
US: Only available in the US

PD 102807, 10 mg

sc-203659A
10 mg
$950.00
US: Only available in the US