Identification and characterization of m4 selective muscarinic antagonists.
Article Details
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Augelli-Szafran CE, Jaen JC, Moreland DW, Nelson CB, Penvose-Yi JR, Schwarz RD
Identification and characterization of m4 selective muscarinic antagonists.
Bioorg Med Chem Lett. 1998 Aug 4;8(15):1991-6.
- PubMed ID
- 9873472 [ View in PubMed]
- Abstract
Our interest in the area of m4 muscarinic antagonists had led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7 nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Carbamoylcholine Muscarinic acetylcholine receptor M1 IC 50 (nM) 10000 N/A N/A Details Carbamoylcholine Muscarinic acetylcholine receptor M2 IC 50 (nM) 3.8 N/A N/A Details Carbamoylcholine Muscarinic acetylcholine receptor M3 IC 50 (nM) 880 N/A N/A Details Carbamoylcholine Muscarinic acetylcholine receptor M4 IC 50 (nM) 0.4 N/A N/A Details Methscopolamine bromide Muscarinic acetylcholine receptor M1 IC 50 (nM) 1.8 N/A N/A Details Methscopolamine bromide Muscarinic acetylcholine receptor M2 IC 50 (nM) 4.3 N/A N/A Details Methscopolamine bromide Muscarinic acetylcholine receptor M3 IC 50 (nM) 1.1 N/A N/A Details