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Table 2 The constants of atropine, pirenzepine, darifenacin, and solifenacin with the immobilized M3R by the injection volume-dependent method

From: Two-point immobilization of M3 muscarinic receptor: a method for recognizing receptor antagonists in natural products

Drug

Concentration (μM)

k′nb/(1 + k′) = nt–(1/KA)k′Vm

R2

KA (104 L/mol)

nt (× 10−9 mol/L)

Atropine

250–1000

k′nb/(1 + k′) = 2.42 × 10–8–1.25 × 10–5 k′Vm

0.993

8.00 ± 0.20

2.42 ± 0.60

1250–4000

k′nb/(1 + k′) = 1.41 × 10–7–1.02 × 10–4 k′Vm

0.990

0.98 ± 0.02

141.00 ± 2.83

Pirenzepine

10–150

k′nb/(1 + k′) = 3.75 × 10–9–3.84 × 10–6 k′Vm

0.986

26.04 ± 0.82

3.75 ± 0.12

300–1800

k′nb/(1 + k′) = 3.14 × 10–8–4.27 × 10–5 k′Vm

0.987

2.34 ± 0.07

31.40 ± 0.87

Darifenacin

500–2000

k′nb/(1 + k′) = 2.76 × 10–8–1.29 × 10–5 k′Vm

0.977

7.75 ± 0.20

27.60 ± 0.35

Solifenacin

200–1000

k′nb/(1 + k′) = 4.40 × 10–8–8.33 × 10–6 k′Vm

0.976

12.01 ± 0.08

44.00 ± 0.26