Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback

FASEB J. 2018 Jun;32(6):2903-2910. doi: 10.1096/fj.201700582R. Epub 2018 Jan 17.

Abstract

We have recently identified a cholinergic chemosensory cell in the urethral epithelium, urethral brush cell (UBC), that, upon stimulation with bitter or bacterial substances, initiates a reflex detrusor activation. Here, we elucidated cholinergic mechanisms that modulate UBC responsiveness. We analyzed muscarinic acetylcholine receptor (M1-5 mAChR) expression by using RT-PCR in UBCs, recorded [Ca2+]i responses to a bitter stimulus in isolated UBCs of wild-type and mAChR-deficient mice, and performed cystometry in all involved strains. The bitter response of UBCs was enhanced by global cholinergic and selective M2 inhibition, diminished by positive allosteric modulation of M5, and unaffected by M1, M3, and M4 mAChR inhibitors. This effect was not observed in M2 and M5 mAChR-deficient mice. In cystometry, M5 mAChR-deficient mice demonstrated signs of detrusor overactivity. In conclusion, M2 and M5 mAChRs attenuate the bitter response of UBC via a cholinergic negative autocrine feedback mechanism. Cystometry suggests that dysfunction, particularly of the M5 receptor, may lead to such symptoms as bladder overactivity.-Deckmann, K., Rafiq, A., Erdmann, C., Illig, C., Durschnabel, M., Wess, J., Weidner, W., Bschleipfer, T., Kummer, W. Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback.

Keywords: chemosensory cells; cholinergic; cystometry; overactive bladder syndrome.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation / drug effects
  • Animals
  • Epithelial Cells / metabolism*
  • Epithelial Cells / pathology
  • Mice
  • Mice, Knockout
  • Muscarinic Antagonists / pharmacology*
  • Receptor, Muscarinic M2* / antagonists & inhibitors
  • Receptor, Muscarinic M2* / biosynthesis
  • Receptor, Muscarinic M2* / genetics
  • Receptor, Muscarinic M5* / antagonists & inhibitors
  • Receptor, Muscarinic M5* / biosynthesis
  • Receptor, Muscarinic M5* / genetics
  • Reverse Transcriptase Polymerase Chain Reaction
  • Urethra / metabolism*
  • Urethra / pathology
  • Urethra / physiopathology
  • Urinary Bladder, Overactive / genetics
  • Urinary Bladder, Overactive / metabolism
  • Urinary Bladder, Overactive / pathology
  • Urinary Bladder, Overactive / physiopathology

Substances

  • Muscarinic Antagonists
  • Receptor, Muscarinic M2
  • Receptor, Muscarinic M5