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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
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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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7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
Antidepressants - Current and Future Targets
Written by P. Skolnich et al
'Antidepressants - Current and Future Targets' provides an overview of the current and future targets for the treatment of major depressive disorder.
Therapeutic Strategies in Schizophrenia
Written by J. Lieberman
'Schizophrenia - Emerging Targets and Therapeutic Strategies' provides a summary of the targets and pathways representing the most promising strategies to pursue for novel drug development.
Neurobiology of Parkinson's Disease
Written by A. Schapira
'Neurobiology and Therapeutics of Parkinson's Disease' highlights the neurobiology of Parkinson's disease and summarizes current and novel therapeutic interventions.
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