Dopamine Receptor Data

View Dopamine Receptors

Receptor Subtype	D₁-like Receptors		D₂-like Receptors
Receptor Subtype	D₁	D₅	D₂	D₃	D₄

G protein	G_s	G_s	G_i/o	G_i/o	G_i/o
Transduction Mechanism	↑ AC, ↑ PLC, ↑ L-type Ca²⁺ channels	↑ AC	↓ AC, ↑ [Ca²⁺]_i, K⁺ conductance, ↓ Ca²⁺ conductance	↓ AC, activation of MAP kinase	↓ AC, ↓ Ca²⁺ conductance
Localization	Caudate, putamen, nucleus accumbens, olfactory tubercle	Hippocampus, hypothalamus	Caudate, putamen, nucleus accumbens, olfactory tubercle	Nucleus accumbens, olfactory tubercle, islands of Calleja	Frontal cortex, midbrain, amygdala, cardiovascular system
Likely Physiological Roles	Locomotion, reward, reinforcement, learning and memory, renin secretion	Learning and memory	Locomotion, reward, reinforcement, learning and memory	Locomotion, possible role in cognition and emotion	Mostly unknown - possible role in cognition and emotion, hypertension

Key Compounds	K_i Values (nM)

D₁-like Agonists	SKF 38393 (0922) SKF 83822 (2075)	1 3.2	~ 0.5 3.1	~ 150 186	~ 5000 66	~ 1000 335
D₁-like Antagonists	SCH 23390 (0925)	~ 0.2	0.3	~ 1100	~ 800	~ 3000
D₂-like Agonists	Bromocriptine (0427) 7-HydroxyDPAT (0706) Cabergoline (2664)	~ 440 ~ 5000 -	~ 450 - 165	~ 8 10 0.7	~ 5 ~ 1 1.5	~ 290 650 9.0
D₂-like Antagonists	Clozapine (0444) Haloperidol (0931) Nemonapride (1746) NGB 2904 (2635) Raclopride (1810) Remoxipride (0916) Spiperone (0995) (S)-(-)-Sulpride (0895)	~ 170 ~ 80 - > 10000 18000 - ~ 350 ~ 45000	~ 330 ~ 100 - 217 - - ~ 3500 77000	~ 230 1.2 0.06 1.4 1.8 ~ 300 0.06 ~ 15	~ 170 ~ 7 0.3 > 5000 3.5 ~ 1600 0.6 ~ 13	21 2.3 0.15 > 10000 2400 ~ 2800 0.08 1000

All K_i values for agonists were determined at the high-affinity state for all receptors, except for D₃ receptors.

References

Seeman and Van Tol (1994) Dopamine receptor pharmacology. TiPS 15 264. Missale et al (1998) Dopamine receptors: from structure to function. Physiol.Rev. 78 189. O'Sullivan et al (2004) SK&F 83822 distinguishes adenylyl cyclase from phospholipase C-coupled D1-like receptors: behavioural topography. Eur.J.Pharmacol. 486 273. Kvernmo et al (2006) A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin.Ther. 28 1065. Yuan et al (1998) NGB 2904 and NGB 2849: two highly selective dopamine D₃ receptor antagonists. Bioorg.Med.Chem.Lett. 8 2715.