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Biological Data
Biological description | Potent and selective M4 muscarinic receptor antagonist (IC50 = 90.7 nM). Shows 72-, 38-, 10- and 82-fold selectivey for M4 over M1, M2, M3 and M5 receptors respectively. Also promotes erythroid progenitors expansion. |
Solubility & Handling
Storage instructions | Room temperature |
Solubility overview | Soluble in DMSO (100mM) |
Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
Chemical name | 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 |
Chemical structure | |
Molecular Formula | C23H24N2O4 |
PubChem identifier | 4995951 |
SMILES | CCOC(=O)C1=C(NC2=C1C3=C(C=C2)OC4C5=C(CCN4C3)C=C(C=C5)OC)C |
InChi | 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 |
InChiKey | VDDUJINYXKGZLV-UHFFFAOYSA-N |
References for PD 102807
References are publications that support the biological activity of the product
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Muscarinic modulation of synaptic transmission via endocannabinoid signalling in the rat midbrain periaqueductal gray.
Lau BK et al (2008) Mol Pharmacol 74(5) : 1392-8. -
Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.
Bã?hme TM et al (2002) J Med Chem 45(14) : 3094-102. -
A novel muscarinic M(4) receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M(2) receptor sub-type.
Kitaichi K et al (1999) Eur J Pharmacol 383(1) : 53-6. -
Identification and characterization of m4 selective muscarinic antagonists.
Augelli-Szafran CE et al (1998) Bioorg Med Chem Lett 8(15) : 1991-6.
Potent, selective M4 receptor antagonist. Promotes erythroid progenitors expansion.