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Dopamine receptors are implicated in many neurological processes, including motivational and incentive salience, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling. Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. [2]
D 1 receptor has a high degree of structural homology to another dopamine receptor, D 5, and they both bind similar drugs. [13] As a result, none of the known orthosteric ligands is selective for the D 1 vs. the D 5 receptor, but the benzazepines generally are more selective for the D 1 and D 5 receptors versus the D 2-like family. [12]
Dopamine receptor D 2, also known as D 2 R, is a protein that, in humans, is encoded by the DRD2 gene.After work from Paul Greengard's lab had suggested that dopamine receptors were the site of action of antipsychotic drugs, several groups, including those of Solomon H. Snyder and Philip Seeman used a radiolabeled antipsychotic drug to identify what is now known as the dopamine D 2 receptor. [5]
A dopamine molecule consists of a catechol structure (a benzene ring with two hydroxyl side groups) with one amine group attached via an ethyl chain. [14] As such, dopamine is the simplest possible catecholamine, a family that also includes the neurotransmitters norepinephrine and epinephrine. [15]
The similarity between the dopamine structure and the ergoline ring in bromocriptine is likely the cause for its action on the dopamine receptors. [35] It has shown to have equal affinity for D 2 - and D 3 -receptor and much lower affinity for D 1 -receptor.
D 5 receptor is a subtype of the dopamine receptor that has a 10-fold higher affinity for dopamine than the D 1 subtype. [6] The D 5 subtype is a G-protein coupled receptor, which promotes synthesis of cAMP by adenylyl cyclase via activation of Gα s/olf family of G proteins. [7] [8] Both D 5 and D 1 subtypes activate adenylyl cyclase.
The dopamine receptor D 4 is a dopamine D2-like G protein-coupled receptor encoded by the DRD4 gene on chromosome 11 at 11p15.5. [5] The structure of DRD4 has been reported in complex with the antipsychotic drug nemonapride. [6] As with other dopamine receptor subtypes, the D 4 receptor is activated by the neurotransmitter dopamine.
Dopamine receptor D 3 is a protein that in humans is encoded by the DRD3 gene. [5] [6] This gene encodes the D 3 subtype of the dopamine receptor. The D 3 subtype inhibits adenylyl cyclase through inhibitory G-proteins. This receptor is expressed in phylogenetically older regions of the brain, suggesting that this receptor plays a role in ...