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Determine the specific muscarinic receptor subtypes responsible for mediating contractile responses in human detrusor smooth muscle in vitro.

October 1, 2001Journal of Autonomic Pharmacology

The minor population of M3‐receptors mediate contraction of human detrusor muscle in vitro

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Authors

RCRuss Chess‐WilliamsBond University CCChristopher R. ChappleForest Institute TYTomonori YamanishiDokkyo Medical University

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Implication

In vitro study demonstrates that M3 receptors solely mediate contraction in human detrusor muscle strips, indicating that functional bladder contraction relies on a minor receptor population.

Key Points

Determine the specific muscarinic receptor subtypes responsible for mediating contractile responses in human detrusor smooth muscle in vitro.
Assessed in vitro contractile responses of human detrusor muscle strips to carbachol with and without subtype-selective antagonists (pirenzepine, methoctramine, 4-DAMP, tropicamide) and nonselective agents (oxybutynin, tolterodine).
Calculated antagonist affinity values (pKB) using Schild analysis and correlated them with published affinities from cloned human muscarinic receptor subtypes.
The M3-selective antagonist 4-DAMP demonstrated high affinity (pKB 9.5), whereas M1- (pirenzepine, pKB 6.8), M2- (methoctramine, pKB 6.9), and M4-selective antagonists (tropicamide, pKB 6.5) exhibited low affinities, with all Schild plot slopes equal to unity.
Oxybutynin and tolterodine acted as competitive antagonists with pKB values of 7.6 and 8.1, respectively, producing an overall pharmacological profile that correlated best with cloned m3 and m5 receptor subtypes.

Cite This Study

Chess‐Williams et al. (2001) studied this question.

synapsesocial.com/papers/6a8695cb012b2ba690512eca https://doi.org/10.1046/j.1365-2680.2001.00231.x

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Implication

In vitro study demonstrates that M3 receptors solely mediate contraction in human detrusor muscle strips, indicating that functional bladder contraction relies on a minor receptor population.

The minor population of M3‐receptors mediate contraction of human detrusor muscle in vitro

Discussion

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Implication

Key Points

Cite This Study

The minor population of M3‐receptors mediate contraction of human detrusor muscle in vitro

Discussion

Member takes

Implication

Key Points

Cite This Study

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