1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.

Article Details

Citation

Sonda S, Katayama K, Fujio M, Sakashita H, Inaba K, Asano K, Akira T

1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.

Bioorg Med Chem Lett. 2007 Feb 15;17(4):925-31. Epub 2006 Nov 22.

PubMed ID
17188867 [ View in PubMed
]
Abstract

The structure-activity relationships of novel 1,5-benzodioxepin derivatives as muscarinic M(1)-M(3) receptor antagonists are reported. Some of these compounds were found to possess high binding affinity for the muscarinic M(3) receptor and potent effect on rhythmic increase in bladder pressure in unanesthetized rats following oral administration. These compounds displayed selectivity for the bladder over the salivary gland.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
OxybutyninMuscarinic acetylcholine receptor M1Ki (nM)1N/AN/ADetails
OxybutyninMuscarinic acetylcholine receptor M2Ki (nM)8.1N/AN/ADetails
OxybutyninMuscarinic acetylcholine receptor M3Ki (nM)0.78N/AN/ADetails