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Norepinephrine releasing agent

Catecholaminergic type of drug From Wikipedia, the free encyclopedia

Norepinephrine releasing agent
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A norepinephrine releasing agent (NRA), also known as an adrenergic releasing agent, is a catecholaminergic type of drug that induces the release of norepinephrine (noradrenaline) and epinephrine (adrenaline) from the pre-synaptic neuron into the synapse.[1][2] This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine therefore an increase in adrenergic neurotransmission.[1][2][3][4]

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Ephedrine, one of the most well-known selective NRAs.

A closely related type of drug is a norepinephrine reuptake inhibitor (NRI), for instance reboxetine.[5][6] Another class of drugs that stimulates adrenergic activity is the adrenergic receptor agonist class.[7]

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Uses and examples

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NRAs, frequently as norepinephrine–dopamine releasing agents (NDRAs) rather than as selective NRAs, are used for a variety of clinical indications including the following:[1][2][8][9]

They are also used as recreational drugs, though this is typically reserved only for those that also induce the release of dopamine and/or serotonin, for instance amphetamine, methamphetamine, MDMA, mephedrone, 4-methylaminorex, and MDAI, among others.[19][20][21][22]

Cathine and cathinone are NRAs found naturally in Catha edulis.[23][24] Ephedrine and pseudoephedrine are also found naturally in Ephedra sinica.[23][24][25] Both of these plants are used medicinally (and recreationally as well regarding the former).[23][24][25] The endogenous trace amines phenethylamine and tyramine are NRAs found in many animals, including humans.[26][1][2]

Selective NRAs include ephedrine, pseudoephedrine, phenylpropanolamine, levomethamphetamine, and D-phenylalaninol.[1][2][25][27] These drugs also release dopamine to a much lesser extent however (e.g., ~10- to 20-fold less potently).[1][2][25][27] No highly selective NRAs are currently known.[28] Among the most selective known NRAs is ephedrine, which had about 19-fold higher potency for inducing norepinephrine release over dopamine release in one study.[28][29] Levomethamphetamine has shown about 15-fold higher potency in inducing norepinephrine release over dopamine release.[27][29] D-Phenylalaninol has 13-fold higher potency in inducing norepinephrine release over dopamine release.[27] In contrast to levomethamphetamine, levoamphetamine is an NDRA, with only about 3-fold preference for inducing norepinephrine release over dopamine release in one study (versus dextroamphetamine being roughly equipotent on norepinephrine and dopamine release in the same study).[21] NRAs play a significant role in treating ADHD, obesity, narcolepsy, and as sympathomimetics by enhancing adrenergic signaling.[1][2][8][30]

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Mechanism of action

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References

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