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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 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.
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.
The most commonly prescribed class of antidepressants in the USA today are the selective serotonin reuptake inhibitors (SSRIs). These drugs inhibit the uptake of the neurotransmitter 5-HT by blocking the SERT, thus increasing its synaptic concentration, and have shown to be efficacious in the treatment of depression, however sexual dysfunction ...
Levodopa is a precursor to the neurotransmitter dopamine, which is administered to increase its levels in the central nervous system.However, most levodopa is decarboxylated to dopamine before it reaches the brain, and since dopamine is unable to cross the blood–brain barrier, this translates to little therapeutic gain with strong peripheral side effects.
Administration can prevent common side-effects, such as nausea and vomiting, as a result of interaction with D 2 receptors in the vomiting center (or cheomoreceptor trigger zone) located outside the blood–brain barrier. [2] Examples of extracerebral decarboxylase inhibitors include carbidopa and benserazide.
Medifoxamine (Cledial, Gerdaxyl) is an antidepressant that appears to act as an SDRI as well as a 5-HT 2 receptor antagonist. [3] Sibutramine (Reductil, Meridia, Siredia, Sibutrex) is a withdrawn anorectic that itself as a molecule in vitro is an SNDRI but preferentially an SDRI, with 18.3- and 5.8-fold preference for inhibiting the reuptake of serotonin and dopamine over norepinephrine ...
PRX-14040 is a selective dopamine reuptake inhibitor that was developed by Prexa Pharmaceuticals. [1] [2] [3] It has 28-fold selectivity for the dopamine transporter over the norepinephrine transporter. [2]
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