Dopamine Receptors

Dopamine is the major catecholamine neurotransmitter present in the mammalian brain where it is responsible for a variety of functions, including locomotion, neuroendocrine secretion, cognition and emotion. Dopamine also plays a role in the periphery where it regulates a range of other processes, including catecholamine release, hormone secretion, and gastrointestinal motility.

Dopamine Receptor Target Files

Related Categories

The application of molecular cloning techniques to the study of dopamine receptors has expanded the classical dopamine D1/D2 classification scheme to include five dopamine receptor subtypes. These may be divided into D1-like (D1 and D5) and D2-like (D2, D3 and D4 receptors) based on their predicted transmembrane topologies, and functional and pharmacological properties. Dysregulation of dopamine transmission causes a variety of conditions such as Parkinson's disease, Tourette's syndrome, schizophrenia and hyperprolactemia.

Receptor Subtype D1-like Receptors D2-like Receptors
D1 D5 D2 D3 D4
G protein Gs Gs Gi/o Gi/o Gi/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 Ki 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)-(-)-Sulpiride (0895)
~ 170
~ 80
-
> 10000
18000
-
~ 350
~ 45000
~ 330
~ 100
-
> 10000
-
-
~ 3500
77000
~ 230
1.2
0.06
217
1.8
~ 300
0.06
~ 15
~ 170
~ 7
0.3
1.4
3.5
~ 1600
0.6
~ 13
21
2.3
0.15
> 5000
2400
~ 2800
0.08
1000

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