Table 1.
Receptor | Association or activation(s) |
Dissociation or deactivation(s) |
||||||||
---|---|---|---|---|---|---|---|---|---|---|
α2AAR | β1AR | α2AR | M1R | PTHR | α2AAR | β1AR | α2AR | M1R | PTHR | |
L + R ⇄LR | nd | nd | nd | nd |
Fast 0.17 Slow1.54 |
nd | nd | nd | nd |
Fast 1.40 Slow 28.00 |
LR ⇄LR* | 0.045 | 0.060 | 0.066 | < 0.100 | 1.59 | 2.00 | 2.50 | 4.00 | 0.20 | 58.00 |
LR* + G ⇄LR*G | 0.045 | 0.060 | 0.050 | 0.200 | 1.58 | ≈ 10 | 8 | 15 | 3.70 | 48.00 |
G ⇄G* | ≈1.00 | 0.450 | 0.450 | 2.00 | 2.04 | 38 | 15 | 37 | 35.00 | 121 |
Values represent the time constant (τ).
FRET, Förster resonance energy transfer; GPCR, G protein-coupled receptors; nd, not determined; PTHR, parathyroid hormone type 1 receptor. Ligand (L) and receptor (R) association and dissociation (L + R ⇄LR); receptor activation and deactivation (LR ⇄LR*); receceptor and G protein (G) interaction (LR* + G ⇄LR* G); G activation and deactivation (G ⇄G*). Reactions were recorded from live cells at a saturating concentration of an agonist: PTHrP(1–36) for PTHR; NE for α2AAR and β1AR; adenosine for A2AR; oxotremodine-methiodide for M1R.