Skip to Content
Merck
  • Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback.

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

FASEB journal : official publication of the Federation of American Societies for Experimental Biology (2018-02-07)
Klaus Deckmann, Amir Rafiq, Christian Erdmann, Christian Illig, Melanie Durschnabel, Jürgen Wess, Wolfgang Weidner, Thomas Bschleipfer, Wolfgang Kummer
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
VU0238429, solubility: ≥20 mg/mL in DMSO
Sigma-Aldrich
Methoctramine hydrate, ≥97% (NMR), solid
Sigma-Aldrich
Pirenzepine dihydrochloride, ≥98% (TLC), powder
Sigma-Aldrich
4-DAMP, ≥98% (HPLC)