Reuptake inhibitor: Difference between revisions

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Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question. By occupying the transporter, a reuptake inhibitor competitively blocks its respective neurotransmitter from binding to the transporter protein and thus prevents it from being transported from the synapse into the presynaptic neurone. Reuptake inhibitors, like [[agonists]] and [[antagonists]], are an example of ligand-receptor binding.

Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.

Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Allosteric binding may cause a conformational change in the transporter protein that prevents it from reuptaking its respective neurotransmitter. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.

==Types of reuptake inhibitors==

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 Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question. By occupying the transporter, a reuptake inhibitor competitively blocks its respective neurotransmitter from binding to the transporter protein and thus prevents it from being transported from the synapse into the presynaptic neurone. Reuptake inhibitors, like [[agonists]] and [[antagonists]], are an example of ligand-receptor binding.
-Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.
+Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Allosteric binding may cause a conformational change in the transporter protein that prevents it from reuptaking its respective neurotransmitter. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.
 ==Types of reuptake inhibitors==