Nomenclature |
D3
receptor
|
D4
receptor
|
D5
receptor
|
HGNC, UniProt |
DRD3, P35462
|
DRD4, P21917
|
DRD5, P21918
|
Endogenous
agonists |
dopamine
(pK
i 6.4–7.3) [245, 545, 1653, 1778] |
dopamine
(pK
i 7.6) [1940] |
dopamine
(pK
i 6.6) [1823] |
Agonists |
pramipexole
(pK
i 8.4–8.7) [1273, 1653], bromocriptine
(Partial agonist) (pK
i 7.1–8.2) [545, 1279, 1653], ropinirole
(pK
i 7.7) [732], apomorphine
(Partial agonist) (pK
i 6.1–7.6) [245, 545, 1279, 1653, 1776] |
apomorphine
(Partial agonist) (pK
i 8.4) [1279] |
– |
(Sub)family‐selective agonists |
quinpirole
(pK
i 6.4–8) [245, 1273, 1281, 1473, 1653, 1776, 1778, 1940] |
quinpirole
(pK
i 7.5) [1279, 1473, 1940] |
A68930
(pEC50 6.6) [1381] |
Selective
agonists |
PD 128907
(pK
i 7.6–7.7) [1539, 1653] |
PD168,077
(Partial agonist) (pK
i 8.8) [995] – Rat,
A412997
(pK
i 8.1) [1319] – Rat,
A412997
(pK
i 8.1) [1319] |
– |
Antagonists |
perospirone
(pK
i 9.6) [1776], sertindole
(pK
i 8–8.8) [60, 1675, 1691],
prochlorperazine
(pK
i 8.4) [68], (‐)‐sulpiride
(pK
i 6.7–7.7) [545, 1776, 1860], loxapine
(pK
i 7.7) [1691], domperidone
(pK
i 7.1–7.6) [545, 1776], promazine
(pK
i 6.8) [246] |
perospirone
(pK
i 10.1) [1694], sertindole
(pK
i 7.8–9.1) [246, 1691,
1693, 1694], sonepiprazole
(pK
i 8.9) [1668], loxapine
(pK
i 8.1) [1693] |
– |
(Sub)family‐selective antagonists |
haloperidol
(pK
i 7.5–8.6) [545, 1711, 1776, 1885] |
haloperidol
(pK
i 8.7–8.8) [1033, 1711, 1885] |
SCH‐23390
(pK
i 7.5–9.5) [1823], SKF‐83556
(pK
i 9.4) [1823], ecopipam
(pK
i 8.3) [1823] |
Selective
antagonists |
S33084
(pK
i 9.6) [1278], nafadotride
(pK
i 9.5) [1654], PG01037
(pK
i 9.2) [656], NGB 2904
(pK
i 8.8) [2055], SB 277011‐A
(pK
i 8) [1569], (+)‐S‐14297
(pK
i 6.9–7.9) [1275, 1281] |
L745870
(pK
i 9.4) [1020], A‐381393
(pK
i 8.8) [1361], L741742
(pK
i 8.5) [1609], ML398
(pK
i 7.4) [138] |
– |
Selective
allosteric modulators |
SB269652
(Negative) (pK
i∼9) [558] |
– |
– |
Labelled
ligands |
– |
[3H]spiperone (Antagonist)
(pK
d 9.5) [749, 1940] |
[3H]SCH‐23390 (Antagonist)
(pK
d 9.2) [1580] |
Labelled
ligands |
[3H]spiperone (Antagonist)
(pK
d 9.9) [767, 2125] – Rat,
[3H]7‐OH‐DPAT (Agonist) (pK
d 9.6) [1581], [3H]PD128907 (Agonist) (pK
d 9) [27] |
[125I]L750667 (Antagonist)
(pK
d 9.8) [1473], [3H]NGD941 (Antagonist) (pK
d 8.3) [1533] |
[125I]SCH23982 (Antagonist)
(pK
d 9.1) – Unknown |