Target intelligence / Profile preview

Norepinephrine releasing agent (NRA)

Target
NRA
Molecular classification
Transporter, Catecholaminergic drug
01

Overview

Norepinephrine releasing agents (NRAs) are a class of drugs that induce the release of norepinephrine and epinephrine from pre-synaptic neurons into the synapse. This mechanism increases the extracellular concentrations of these neurotransmitters, enhancing adrenergic neurotransmission throughout the body. NRAs vary in their selectivity, with some also affecting dopamine release to different degrees. Selective NRAs include ephedrine, pseudoephedrine, phenylpropanolamine, and levomethamphetamine, though none are highly selective. These agents are used therapeutically for treating ADHD, obesity, narcolepsy, and as nasal decongestants. A related class of drugs is norepinephrine-dopamine releasing agents (NDRAs), which affect both norepinephrine and dopamine release more equally. NRAs are distinguished from norepinephrine reuptake inhibitors (NRIs), which block the reuptake of norepinephrine rather than stimulating its release.

Other names
Adrenergic releasing agentNoradrenergic releasing agent
02

Mechanism of action

Induces release of norepinephrine and epinephrine from pre-synaptic neurons; Increases extracellular concentrations of norepinephrine and epinephrine; Enhances adrenergic neurotransmission; Some NRAs also release dopamine to varying degrees; Acts on norepinephrine transporters to reverse their normal function

03

Biological functions

NeurotransmissionAdrenergic signalingSympathetic nervous system activationCardiovascular regulation
04

Disease associations

Attention-deficit hyperactivity disorder (ADHD)ObesityNarcolepsyNasal congestionDepression
05

Safety considerations

Cardiovascular effects (increased blood pressure, heart rate)Potential for abuse and dependenceInsomniaAnxietyAppetite suppressionHypertension
06

Interacting drugs

Amphetamine

18 more in the full profile.

07

Biomarkers

Plasma norepinephrine levelsUrinary norepinephrine metabolites

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