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Table 1 Activation of muscarinic M1 receptors as measured by R-SAT® and PI assays

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

 

M1 Agonist RSAT

PI Hydrolysis

 

pEC50

% Efficacy

pEC50

% Efficacy

Carbachol

6.2 ± 0.3

100 ± 10

6 ± 0.1

100 ± 3

Oxotremorine-M

7.4 ± 0.3

105 ± 13

7.0 ± 0.1

106 ± 7

Pilocarpine

5.7 ± 0.2

93 ± 15

6.2 ± 0.9

97 ± 31

Xanomeline

7.4 ± 0.5

120 ± 21

8.4 ± 0.2

99 ± 12

NDMC

7.4 ± 0.2

76 ± 13

7.1 ± 0.4

67 ± 23

AC-42

6.7 ± 0.3

62 ± 14

6.5 ± 0.5

79 ± 14

AC-260584

7.6 ± 0.4

102 ± 21

7.7 ± 0.3

90 ± 17

  1. Activities of compounds on human M1 receptors were compared using two different assay; RSAT in transiently transfected NIH-3T3 cells and PI hydrolysis in stable CHO-M1 cells. Data for each compound is normalized to carbachol for both assays. Values presented are mean ± SD from 2-19 independent experiments carried out in triplicate.