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. 2023 Mar 6;24(5):5042. doi: 10.3390/ijms24055042

Table 1.

(A) Dopamine receptor agonists. The main dopamine receptors on which the commonly used dopamine receptor agonist acts are listed here in five columns. Dopamine is an agonist at all dopamine receptors, albeit with varying affinities. One would predict in the heart that first high-affinity dopamine receptors, and thereafter, low-affinity receptors, will be stimulated by dopamine. Note that there is no drug currently available that allows for distinguishing between D1-dopamine and D5-dopamine receptors. Usually, antagonists do not distinguish between D2-, D3-, D4-dopamine receptors. Moreover, at higher concentrations, for instance, fluphenazine antagonizes also at the D1-dopamine receptors. Moreover, antagonists usually are not dopamine receptor-selective. For instance, metoclopramide also acts antagonistically on cardiac 5-HT4-serotonin receptors and domperidon on cardiac potassium channels. (B) Dopamine receptor antagonists. The main dopamine receptors on which commonly used dopamine receptor antagonists act are listed here in five columns. Note that there is no antagonist that is currently available that allows to distinguish between D1-dopamine and D5-dopamine receptors. Usually, antagonists do not distinguish between D2-, D3-, D4-dopamine receptors. Moreover, at higher concentrations, for instance, fluphenazine antagonizes also at D1-dopamine receptors. Moreover, antagonists usually are not dopamine receptor-selective. For instance, metoclopramide also acts antagonistically on cardiac 5-HT4-serotonin receptors, and domperidon acts antagonistically on cardiac potassium channels. Superscript numbers indicate which drug was used in which reference. Ki indicates the half maximum concentration to inhibit a function and pKi represents its negative decadic logarithm.

(A) Dopamine Receptor Agonists
D1 D2 D3 D4 D5 Reference
dopamine
pKi: 4.3–5.6
dopamine
pKi: 4.3–5.6
dopamine
pKi: 6.3–7.4
dopamine
pKi: 7.6
dopamine
pKi: 6.6
Myslivecek 2022 [1]
1 SKF-38393 2 MLS1547 1 SKF-38393 1 Ding et al. 2008 [2]
2 Myslivecek 2022 [1]
AT77636 rotigotine rotigotine rotigotine AT77636 Myslivecek 2022 [1]
1SKF-81297 1 ropinirole 1 ropinirole 2 quinpirole 1 SKF-81297 1 Myslivecek 2022 [1]
2 Yamaguchi et al., 1997 [3]
1 SKF-83959 1,2 pramipexol 1,2 pramipexol 2 pramipexol 1 SKF-83959 1 Myslivecek 2022 [1]
2 Piercey et al., 1996 [4]
fenoldopam
(=SKF 82526)
2 PD 128907 PD 128907 fenoldopam
(=SKF 82526)
Myslivecek 2022 [1]
2A68930 1 PD16077 1PD16077 1 Myslivecek 2022 [1]
2 DeNinno et al., 1990 [5]
2 chloro APB 1 A412997 1A412997 1 A412997 1 Myslivecek 2022 [1]
2 Neumeyer et al., 1991 [6]
dihydrexidine Salmi et al., 2004 [7]
apomorphine Myslivecek 2022 [1]
propylbutyl-dopamine Zhao et al. 1990 [8]
SKF81297 Rashid et al., 2007 [9]
quinpirole Rashid et al., 2007 [9]
bromocriptine
0.1 µM (as Ki)
bromocriptine Kvernmo et al., 2008 [10]
pergolide
0.6 µM (as Ki)
pergolide Kvernmo et al., 2008 [10]
(B) Dopamine Receptor Antagonists
D1 D2 D3 D4 D5 Reference
2 haloperidol 2 haloperidol 2 S33084 2 L745870 2 Myslivecek 2022 [1]
1 SCH-38390 2 pipotiazine 2 SB277011-A 2 sonepiprazole 1 SCH-39390 1 Ding et al. 2008 [2]
2,3 SKF-83566 2 perospirone 2 perospirone 2 perospirone 2 SKF-83566 2 Myslivecek 2022 [1]
3 Kopia and Valocik 1989 [11]
2 ecopipam 2 raclopride 2 raclopride 2 A-381393 2 ecopipam 2 Myslivecek 2022 [1]
2 SCH23982 2 ML321 2 sulpiride 2 sulpiride 2 Myslivecek 2022 [1]
1 odapipam
(=NNC 756
Ki: 0.17 nM)
1 odapipam
(Ki: 942 nM)
2 prochlorperazine
2 prochlorperazine 2 prochlorper-azine 1 Andersen et al., 1992 [12]
2 Myslivecek 2022 [1]
NGB 2904 NGB 2904 NGB 2904 Myslivecek 2022 [1]
metoclopramide S14297 S14297 Myslivecek 2022 [1]
domperidon Myslivecek 2022 [1]
pimozide pimozide pimozide Lumley et al., 1977 [13]
fluphenazine fluphenazine Vettel et al., 2014 [14]
melperone Lencesova et al., 2017 [15]
cabergoline cabergoline Myslivecek 2022 [1]

Pergolide and bromocriptine have an affinity of 0.1 µM (as Ki) or 0.6 µM at D1-dopamine receptors; therefore, they can act as agonists at D1-dopamine receptors.