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Table 3 Activation of muscarinic M1 receptors as measured by BRET-2

From: Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands

 

BRET-2

Compound

pEC50

%Efficacy

Carbachol

4.6 ± 0

100 ± 0

Oxotremorine-M

5.6 ± 0.2

100 ± 12

Pilocarpine

5.4 ± 0.3

16 ± 3*

NDMC

NA

 

AC-42

5.4 ± 0.6

12 ± 0.7*

AC-260584

6.2 ± 0.14

26 ± 6*

Xanomeline

7.2 ± 0.3

16 ± 6*

  1. M1 BRET-2 assays were performed to determine potency and efficacy of agonists to stimulate β-arrestin-1 recruitment. Data presented are mean ± S.D. from 2-3 independent experiments carried out in triplicate. Statistically significant difference compared to no drug, * = p < 0.001, (Student t-test, GraphPad, Prism). Based on student t-test, efficacies for AC-42, AC-260584, xanomeline and pilocarpine were not statistically different, p > 0.5. NA: No measurable agonist activity.
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BMC Pharmacology

ISSN: 1471-2210