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Table 1 Maximal efficacies (Emax) and potencies (EC50) of MRS2179, MRS2279 and MRS2500 on P2Y1-R-dependent Gαq protein activation and β-arrestin 2 recruitment

From: Platelet P2Y1 receptor exhibits constitutive G protein signaling and β-arrestin 2 recruitment

G protein signaling

 

Emax ± s.e.m.

EC50 (M)

pEC50 ± s.e.m.

MRS2179

115.7 ± 5.057

1.525e−005

4.817 ± 0.0671

MRS2279

154.3 ± 13.86

2.638e−005

4.579 ± 0.1247

MRS2500

127.2 ± 3.892

7.716e−007

6.113 ± 0.07237

β-Arrestin 2 signaling

 

Emax ± s.e.m

EC50 (M)

pEC50 ± s.e.m

MRS2179

− 103.3 ± 6.549

5.055e−006

5.296 ± 0.153

MRS2279

− 102.8 ± 14.98

1.943e−005

4.712 ± 0.2838

MRS2500

− 89.95 ± 2.887

4.755e−008

7.323 ± 0.1193

  1. Data were obtained from experiments shown in Fig. 4a, b and represent the Emax ± s.e.m, EC50 (M), and pEC50 ± s.e.m. on P2Y1-R-dependent Gαq protein and β-arrestin 2 constitutive signaling