M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor.

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Citation

Bozkurt TE, Sahin-Erdemli I

M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor.

Pharmacol Res. 2009 May;59(5):300-5. doi: 10.1016/j.phrs.2009.01.013. Epub 2009 Feb 5.

PubMed ID
19416629 [ View in PubMed
]
Abstract

We have investigated the muscarinic receptor subtype(s) mediating the release of urinary bladder-derived relaxant factor that is demonstrated by a coaxial bioassay system. Acetylcholine-induced relaxation of a precontracted anococcygeus muscle mounted within the bladder was considered as an evidence for the release of this factor. M(1)-muscarinic agonist McN-A-343 and the cholinesterase inhibitor physostigmine also elicited relaxation responses in the coaxial bioassay besides acetylcholine. Acetylcholine-induced relaxation was antagonized by the subtype-selective muscarinic antagonists (pK(B)): M(3)-antagonist darifenacin (9.36+/-0.11), M(3)/M(1)-antagonist 4-DAMP (9.30+/-0.11), M(1)-antagonist telenzepine (8.56+/-0.21), M(4)-antagonist tropicamide (6.63+/-0.17) and M(2)-antagonist AF-DX 116 (6.01+/-0.21). The pK(B) values of these antagonists have suggested that stimulation of M(1)- and M(3)-muscarinic receptors in the bladder wall mediates the release of urinary bladder-derived relaxant factor. In addition, McN-A-343, by activating the facilitatory M(1) receptors and physostigmine by inhibiting the acetylcholinesterase may induce the release of this factor through endogenous acetylcholine in the coaxial bioassay system.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
DarifenacinMuscarinic acetylcholine receptor M3ProteinHumans
Yes
Antagonist
Details