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Table 2 Recycling of muscarinic receptors after treatment with various ligands

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

 

No recycle

3 h recycle

No drug

100

100

Carbachol

48 ± 4*

102 ± 10

Oxotremorine-M

60 ± 2*

97 ± 1

Xanomeline

65 ± 5*

69 ± 7*

AC-42

63 ± 3*

69 ± 1*

AC-260584

59 ± 2*

64 ± 3*

  1. HEK-293 cells expressing hM1 were treated with various ligands for 30 minutes as indicated in the table. Concentrations of ligands used were as follows; carbachol, 100 μM; oxotremorine-M, 1 μM; xanomeline, 100 μM; AC-42, 10 μM; and AC-260584, 1 μM and similar to concentration used in the internalization assays. Values presented are % receptors on the cells surface. Data presented is the average from 2 independent experiments carried out in triplicate. Statistically significant difference compared to no drug, * = p < 0.05, (Student t-test, GraphPad, Prism).
  2. No recycling could be observed after treatment with NDMC (1 μM), 71% cell surface receptor after 3 hours of recycling (n = 1).