Identification and characterization of m4 selective muscarinic antagonists.

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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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
CarbamoylcholineMuscarinic acetylcholine receptor M1IC 50 (nM)10000N/AN/ADetails
CarbamoylcholineMuscarinic acetylcholine receptor M2IC 50 (nM)3.8N/AN/ADetails
CarbamoylcholineMuscarinic acetylcholine receptor M3IC 50 (nM)880N/AN/ADetails
CarbamoylcholineMuscarinic acetylcholine receptor M4IC 50 (nM)0.4N/AN/ADetails
Methscopolamine bromideMuscarinic acetylcholine receptor M1IC 50 (nM)1.8N/AN/ADetails
Methscopolamine bromideMuscarinic acetylcholine receptor M2IC 50 (nM)4.3N/AN/ADetails
Methscopolamine bromideMuscarinic acetylcholine receptor M3IC 50 (nM)1.1N/AN/ADetails