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Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. [1] Dopamine receptors are therefore common drug targets. Dopamine receptors activate different effectors through not only G-protein coupling, but also signaling through different protein (dopamine receptor-interacting ...
A dopamine antagonist, also known as an anti-dopaminergic and a dopamine receptor antagonist (DRA), is a type of drug which blocks dopamine receptors by receptor antagonism. Most antipsychotics are dopamine antagonists, and have been used in treating schizophrenia , bipolar disorder , and stimulant psychosis . [ 1 ]
Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. [2] Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors.
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron.
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]
Non-ergoline dopamine receptor agonists have higher binding affinity to dopamine D 3-receptors than dopamine D 2-receptors. This binding affinity is related to D 2 and D 3 receptor homology, the homology between them has a high degree of sequence and is closest in their transmembrane domains, were they share around 75% of the amino acid. [37]
Ecopipam is an example of a D 1-like receptor antagonist. At low doses, dopamine D 2 and D 3 receptor antagonists can preferentially block presynaptic dopamine D 2 and D 3 autoreceptors and thereby increase dopamine levels and enhance dopaminergic neurotransmission.
Dopamine therapy is the regulation of levels of the neurotransmitter dopamine through the use of either agonists, or antagonists; and has been used in the treatment of disorders characterized by a dopamine imbalance. Dopamine replacement therapy (DRT) is an effective treatment for patients with decreased levels of dopamine.