Dopamine receptor D2

D 2 D 2 receptorDRD2D2 receptorD2dopamine receptor D 2 D2 receptorsD 2 receptorsdopamine D 2 receptordopamine D2 receptors
Dopamine receptor D 2, also known as D2R, is a protein that, in humans, is encoded by the DRD2 gene.wikipedia
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Dopamine receptor

dopaminedopamine receptorsdopaminergic
This gene encodes the D 2 subtype of the dopamine receptor, which is coupled to G i subtype of G protein-coupled receptor.

Dopamine

dopaminergic systemDAdopaminergic
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 Snyder and Philip Seeman) used a radiolabeled antipsychotic drug to identify what is now known as the dopamine D 2 receptor.
These can be postsynaptic dopamine receptors, which are located on dendrites (the postsynaptic neuron), or presynaptic autoreceptors (e.g., the D 2 sh and presynaptic D 3 receptors), which are located on the membrane of an axon terminal (the presynaptic neuron).

Cabergoline

Dostinex
In similar manner, older dopamine agonists used for Parkinson's disease such as bromocriptine and cabergoline are poorly selective for one dopamine receptor over another, and, although most of these agents do act as D 2 agonists, they affect other subtypes as well.
Cabergoline (brand names Dostinex and others), an ergot derivative, is a potent dopamine receptor agonist on D 2 receptors.

C957T

The C957T gene polymorphism is a synonymous mutation located within the 957th base pair of the DRD2 gene.

Piribedil

Piribedil (trade names Pronoran, Trivastal Retard, Trastal, Trivastan, Clarium and others) is an antiparkinsonian agent and piperazine derivative which acts as a D 2 and D 3 receptor agonist.

ANKK1

ANNK1 and addictive behaviors
However, the polymorphism resides in exon 8 of the ANKK1 gene.
This polymorphism, which is commonly referred to Taq1A, was previously believed to be located in the promoter region of the DRD2 gene, since the polymorphism is proximal to the DRD2 gene and can influence DRD2 receptor expression.

Brexpiprazole

Rexulti
It is a dopamine D 2 receptor partial agonist and has been described as a "serotonin–dopamine activity modulator" (SDAM).

Risperidone

RisperdalRisperdal (risperidone)
The structure of DRD2 in complex with the atypical antipsychotic risperidone has been determined.

Quinpirole

Quinpirole is a psychoactive drug and research chemical which acts as a selective D 2 and D 3 receptor agonist.

Sumanirole

Sumanirole (PNU-95,666) is a highly selective D 2 receptor full agonist, the first of its kind to be discovered.

Cariprazine

RGH-188Vraylar
It acts primarily as a D 3 receptor and D 2 receptor partial agonist, with high selectivity for the D 3 receptor.

Dihydrexidine

It has approximately 10-fold selectivity for D 1 and D 5 over the D 2 receptor.

Aplindore

Aplindore (DAB-452) is a drug which acts as a partial agonist selective for the dopamine receptor D2.

Lysergic acid diethylamide

LSDacidLSD-25
The agonism of the D 2 receptor by LSD may contribute to its psychoactive effects in humans.

Domperidone

[3H]domperidoneH-domperidone
It is a peripherally selective dopamine D 2 receptor antagonist and was developed by Janssen Pharmaceutica.

Chlorpromazine

ThorazineLargactilchlorpromazine hydrochloride
Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D 2 receptor, but are, in general, very unselective, at best selective only for the "D 2 -like family" receptors and so binding to D 2, D 3 and D 4, and often also to many other receptors such as those for serotonin and histamine, resulting in a range of side-effects and making them poor agents for scientific research.
Chlorpromazine is a very effective antagonist of D2 dopamine receptors and similar receptors, such as D3 and D5.

Ropinirole

RequipAdartrelropinerole
Ropinirole acts as a D 2, D 3, and D 4 dopamine receptor agonist with highest affinity for D 2.

Quinelorane

Quinelorane is a drug which acts as a dopamine agonist for the D 2 and D 3 receptor.

Aripiprazole

AbilifyAripriprazole
It shows differential engagement at the dopamine receptor (D 2 ).

Itopride

It is a combined D 2 receptor antagonist and acetylcholinesterase inhibitor.

Brilaroxazine

RP5063
Specifically, it acts as a partial agonist of the D 2, D 3, and D 4 receptors and of the 5-HT 1A and 5-HT 2A receptors, and as an antagonist of the 5-HT 6 and 5-HT 7 receptors.

Ligand (biochemistry)

affinityligandbinding affinity
It was observed that either D 2 R agonist or antagonist ligands revealed better binding affinities inside the ligand-binding domain of the active D 2 R in comparison with the inactive state.
Since these early reports, there have been many bivalent ligands reported for various G protein-coupled receptor (GPCR) systems including cannabinoid, serotonin, oxytocin, and melanocortin receptor systems, and for GPCR-LIC systems (D2 and nACh receptors).

Modafinil

ProvigilAlertecList of modafinil analogues
In support of modafinil acting as a dopaminergic agent, its wakefulness-promoting effects are abolished in DAT knockout mice (although it is important to note that DAT knockout mice show D 1 and D 2 receptor and norepinephrine compensatory abnormalities, which might confound this finding), reduced by both D 1 and D 2 receptor antagonists (although conflicting reports exist), and completely blocked by simultaneous inactivation of both D 1 and D 2 receptors.

Haloperidol

HaldolHaloparidolhaloperidol decanoate
Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D 2 receptor, but are, in general, very unselective, at best selective only for the "D 2 -like family" receptors and so binding to D 2, D 3 and D 4, and often also to many other receptors such as those for serotonin and histamine, resulting in a range of side-effects and making them poor agents for scientific research.