Dopamine GPCR Family Subtypes and Products

What Are Dopamine Receptors?

Dopamine receptors are a family of G protein-coupled receptors (GPCRs) which are responsible for a large number of central nervous system functions, such as attention, cognitive functions, cardiovascular functions, motivation and positive reinforcement and motor activity. There are five different subtypes of dopamine receptors: D1, D2, D3, D4, and D5. Defects in any one of these transmitters has a potentially large effect on the central nervous system in the form of neurological and psychiatric disorders. These disorders include Tourette’s syndrome, Parkinson’s disease, schizophrenia, ADHD, substance abuse, and social phobias.

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Dopamine Receptor Information

Clickable Text Interaction

D1

D2

D2 Ghrelin

D3

D4

D5

The human dopamine receptor D1 (DRD1 or D1) is a G-protein- coupled receptor. It is expressed most abundantly in the brain areas such as caudate, nucleus accumbens and olfactory tubercle. The D1 receptor regulates neuronal growth and development, mediates some behavioral responses, and modulates dopamine receptor D2-mediated events.

The human dopamine receptor DRD2 (D2) is a G protein-coupled receptor for dopamine. It can be found on postsynaptic dopaminergic neurons that are centrally involved in reward-mediating mesocorticolimbic pathways. Signaling through dopamine D2 receptors governs physiological functions related to locomotion, hormone production, and drug abuse.

The concept of dimerization of G protein-coupled receptor (GPCR) has opened a new insight regarding physiological function regulation. One of the example is heterodimerization of Ghrelin(GHSR) and dopamine(DRD2) receptor. Recent experiments have showed that GHSR:DRD2 heterodimers allosterically modifies canonical DRD2 dopamine signaling resulting in Gβγ subunit-dependent mobilization of Ca2+ independent of GHSR basal activity. Independently, agonist activation of GHSR results in coupling to Gαq and DRD2 transmits dopamine signal through Gαi/o coupling by inhibiting activity of adenylate cyclase and decreasing cAMP level in dose dependent manner.

The human dopamine receptor DRD3 (D3) is a G protein-coupled receptor for dopamine. D3 receptor belongs to the D2-like family of dopamine receptors which are widely expressed in the central nervous system. D3 is involved in movement coordination, cognition, emotion, affects memory and the regulation of prolactin secretion by the pituitary. Alterations in D3 pathways can cause pathogenesis of neurological, neuropsychiatric and hormonal disorders, including Parkinson’s Disease, schizophrenia and hyperprolactinemia.

The human dopamine receptor D4 is a D2-like receptor that inhibits adenylyl cyclase activity and activates K+ channels. D4 receptor antagonists show great potential in the treatment of human personality and psychiatric disorders, such as ADHD (Attention deficit hyperactivity disorder), schizophrenia, alcoholism, and drug addiction.

The human dopamine receptor D5 is a D1-like receptor and its activation stimulates adenylyl cyclase activity. It has a 10-fold higher affinity for dopamine than the D1 receptor. The D5 receptor is expressed in neurons in the limbic regions of the brain, and has been implicated in ADHD and addiction disorders.

Dopamine Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
DopamineD1humanHEK293TC1335DC1335MC1335
D1humanHEK293TH1335DH1335MH1335
D2humanHEK293TC1336DC1336MC1336
D2humanHEK293TC1336aDC1336aMC1336a
D2 GhrelinhumanHEK293TC1514DC1514MC1514
D3humanHEK293T Gqi5CG1337DCG1337MCG1337
D4humanHEK293TC1338DC1338MC1338
D4humanHEK293T Gαqi5CG1338DCG1338MCG1338
D5humanHEK293TC1339DC1339MC1339

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