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Table 1 Radioligand binding and functional activities of different compounds*

From: Agonist signalling properties of radiotracers used for imaging of dopamine D2/3 receptors

  cAMP ?-arrestin-2
Compound pKiD2-high Potency Efficacy Potency Efficacy
   pEC50 % pEC50 %
Dopamine 6.97¿ 9.22¿ 100¿ 6.97 100
NPA 10.13¿ 10.31 118 9.67 103
PHNO 9.47¿ 11.03 114 9.39 99
11a 8.69¿ 9.16¿ 86¿ 8.26 81
12a 8.26¿ 9.42¿ 96¿ 8.36 88
12d 8.30¿ 9.82¿ 94¿ 8.61 88
IBZM 6.99¿ 9.08 Inverse agonist - Neutral antagonist
  1. *pKi, pEC50 and Emax values are the average of at least two duplicate experiments with standard deviations (SD) values that were less than a third of the mean.
  2. ¿Parts published earlier in van Wieringen et al, 2014 [19].
  3. ¿For IBZM no high-affinity state was detected; pKi value represents affinity for the total number of D2 receptors.