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Reuptake inhibitor: Difference between revisions
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'''Reuptake''' is a required aspect of neurological activity which regulates the amount of neurotransmitter present in a synapse after the transmission of a neural signal. Neurotransmission occurs by transporting information across neurons by an electrical impulse called an action potential. When an action potential reaches the synapse between two neurons, the pre-synaptic neuron releases neurotransmitters to transport the chemical signal across the synapse by binding to receptors on the post-synaptic neuron. Reuptake is achieved by transporter proteins which reabsorb the extracellular neurotransmitter back into the pre-synaptic neurone for reuse. Reuptake can determine the extent, duration, and spatial domain of receptor activation. | [[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone]]'''Reuptake''' is a required aspect of neurological activity which regulates the amount of neurotransmitter present in a synapse after the transmission of a neural signal. Neurotransmission occurs by transporting information across neurons by an electrical impulse called an action potential. When an action potential reaches the synapse between two neurons, the pre-synaptic neuron releases neurotransmitters to transport the chemical signal across the synapse by binding to receptors on the post-synaptic neuron. Reuptake is achieved by transporter proteins which reabsorb the extracellular neurotransmitter back into the pre-synaptic neurone for reuse. Reuptake can determine the extent, duration, and spatial domain of receptor activation. | ||
A '''reuptake inhibitor''', also known as a transporter blocker, is a drug that inhibits the reuptake of a [[neurotransmitter]] from the synapse into the presynaptic neurone, leading to an increase in the extracellular concentrations of the neurotransmitter. The increased synaptic concentration of a neurotransmitter results in Various drugs utilize reuptake inhibition to exert their psychological and physiological effects, including many [[antidepressants]] and [[stimulants]]. | A '''reuptake inhibitor''', also known as a transporter blocker, is a drug that inhibits the reuptake of a [[neurotransmitter]] from the synapse into the presynaptic neurone, leading to an increase in the extracellular concentrations of the neurotransmitter. The increased synaptic concentration of a neurotransmitter results in Various drugs utilize reuptake inhibition to exert their psychological and physiological effects, including many [[antidepressants]] and [[stimulants]]. | ||
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==Mechanism of action== | ==Mechanism of action== | ||
Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question.<ref> Ravna AW, Sylte I, Dahl SG (2003). "Molecular mechanism of citalopram and cocaine interactions with neurotransmitter transporters.". J Pharmacol Exp Ther. 307 (1): 34–41. | https://www.ncbi.nlm.nih.gov/pubmed/12944499</ref> 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.<ref>Dunn, Michael F(Apr 2010) Protein–Ligand Interactions: General Description. In: eLS. John Wiley & Sons Ltd, Chichester. http://www.els.net [doi: 10.1002/9780470015902.a0001340.pub2]</ref> | Standard reuptake inhibitors are believed to function by binding directly to the transporter protein of the [[neurotransmitter]] in question.<ref> Ravna AW, Sylte I, Dahl SG (2003). "Molecular mechanism of citalopram and cocaine interactions with neurotransmitter transporters.". J Pharmacol Exp Ther. 307 (1): 34–41. | https://www.ncbi.nlm.nih.gov/pubmed/12944499</ref> 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.<ref>Dunn, Michael F(Apr 2010) Protein–Ligand Interactions: General Description. In: eLS. John Wiley & Sons Ltd, Chichester. http://www.els.net [doi: 10.1002/9780470015902.a0001340.pub2]</ref> | ||