What question did this study set out to answer?

Characterize the pharmacological properties and specific subtypes of muscarinic receptors responsible for muscle contraction in male mouse isolated urinary bladder smooth muscle.

August 1, 2001British Journal of PharmacologyOpen Access

Pharmacological characterization of muscarinic receptors in mouse isolated urinary bladder smooth muscle

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Authors

ACAgnès ChoppinDélégation Paris 7 RERichard M. EglenPerkinElmer (United States)

Discussion

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Implication

In vitro pharmacological study demonstrates that M3 receptors mediate contractile responses in mouse bladder smooth muscle, indicating their predominant functional role in urination.

Key Points

Characterize the pharmacological properties and specific subtypes of muscarinic receptors responsible for muscle contraction in male mouse isolated urinary bladder smooth muscle.
Assessed concentration-dependent contractions of isolated bladder smooth muscle strips (n=4) using agonists including (+)-cis-dioxolane, oxotremorine-M, acetylcholine, carbachol, and pilocarpine.
Determined antagonistic potency (pKB values) across 10 selective and non-selective muscarinic antagonists, correlating findings with human recombinant M1–M5 receptor affinities and recontraction assays designed to isolate M2 receptor activity.
Agonists produced concentration-dependent contractions with potency values (pEC50) of 6.6 +/- 0.1 for (+)-cis-dioxolane, 6.9 +/- 0.1 for oxotremorine-M, 6.7 +/- 0.1 for acetylcholine, 5.8 +/- 0.1 for carbachol, and 5.8 +/- 0.1 for pilocarpine.
Tissue antagonist affinity (pKB) correlated most strongly with human recombinant M3 receptor binding affinities, and methoctramine retained M3-like affinity (pKB = 6.23 +/- 0.14; pA2 = 6.16 +/- 0.03) under M3-depleted conditions optimized for M2 activation.

Cite This Study

Choppin et al. (2001) studied this question.

synapsesocial.com/papers/6a82c6501d8eddfbf50f7401 https://doi.org/10.1038/sj.bjp.0704165

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August 1, 2001British Journal of PharmacologyOpen Access

Pharmacological characterization of muscarinic receptors in mouse isolated urinary bladder smooth muscle

View Full Paper

Ask AI

Bookmark

Authors

ACAgnès ChoppinDélégation Paris 7 RERichard M. EglenPerkinElmer (United States)

Discussion

Member takes

Implication

In vitro pharmacological study demonstrates that M3 receptors mediate contractile responses in mouse bladder smooth muscle, indicating their predominant functional role in urination.

Key Points

Characterize the pharmacological properties and specific subtypes of muscarinic receptors responsible for muscle contraction in male mouse isolated urinary bladder smooth muscle.
Assessed concentration-dependent contractions of isolated bladder smooth muscle strips (n=4) using agonists including (+)-cis-dioxolane, oxotremorine-M, acetylcholine, carbachol, and pilocarpine.
Determined antagonistic potency (pKB values) across 10 selective and non-selective muscarinic antagonists, correlating findings with human recombinant M1–M5 receptor affinities and recontraction assays designed to isolate M2 receptor activity.
Agonists produced concentration-dependent contractions with potency values (pEC50) of 6.6 +/- 0.1 for (+)-cis-dioxolane, 6.9 +/- 0.1 for oxotremorine-M, 6.7 +/- 0.1 for acetylcholine, 5.8 +/- 0.1 for carbachol, and 5.8 +/- 0.1 for pilocarpine.
Tissue antagonist affinity (pKB) correlated most strongly with human recombinant M3 receptor binding affinities, and methoctramine retained M3-like affinity (pKB = 6.23 +/- 0.14; pA2 = 6.16 +/- 0.03) under M3-depleted conditions optimized for M2 activation.

Cite This Study

Choppin et al. (2001) studied this question.

synapsesocial.com/papers/6a82c6501d8eddfbf50f7401 https://doi.org/10.1038/sj.bjp.0704165

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