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Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS) and 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.
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.
At low doses dopamine mainly triggers dopamine receptors and β1-adrenergic receptors while at high doses it works via α-adrenergic receptors. [4] Dopamine was first synthesized in a laboratory in 1910 by George Barger and James Ewens in England. [8] It is on the World Health Organization's List of Essential Medicines. [9]
Dopamine receptor flow chart. Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. [1] The D 1-like class of dopamine receptors is coupled to Gα s/olf and stimulates adenylate cyclase production, whereas the D 2-like class is coupled to Gα i/o and thus inhibits adenylate cyclase production.
Although it is important to know that there is a correlation between the two drugs, if l-DOPA doesn't work dopamine agonists are also ineffective. [1] The early dopamine agonists, such as bromocriptine, were ergot derived and activated the D 2-receptor. [7] They induced major side effects such as fibrosis of cardiac valves.
Examples of sympathomimetic effects include increases in heart rate, force of cardiac contraction, and blood pressure. [1] The primary endogenous agonists of the sympathetic nervous system are the catecholamines (i.e., epinephrine [adrenaline], norepinephrine [noradrenaline], and dopamine ), which function as both neurotransmitters and hormones .
Amphetamine, an NDRA and one of the most well-known DRAs. 4-Methylaminorex (4-MAR), the cis- isomer being one of the most dopamine-selective NDRAs known.. A dopamine releasing agent (DRA) is a type of drug which induces the release of dopamine in the body and/or brain.
Methylphenidate, one of the most widely used NDRIs.. A norepinephrine–dopamine reuptake inhibitor (NDRI) is a type of drug that inhibits the reuptake of the monoamine neurotransmitters norepinephrine and dopamine and thereby increases extracellular levels of these neurotransmitters and noradrenergic and dopaminergic neurotransmission. [1]