Tag: Adrenergic

What is a Norepinephrine Releasing Agent?

Published on by Andrew Marshall1 Comment

Introduction

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. This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine therefore an increase in adrenergic neurotransmission.

A closely related type of drug is a norepinephrine reuptake inhibitor (NRI). Another class of drugs that stimulates adrenergic activity is the adrenergic receptor agonist class.

Refer to Monoamine Releasing Agent.

Uses and Examples

NRAs are used for a variety of clinical indications including the following:

  • For the treatment of attention deficit hyperactivity disorder (ADHD), e.g. amphetamine, methamphetamine, pemoline
  • As anorectics in the treatment of obesity, e.g. amphetamine, phentermine, benzphetamine, phenmetrazine, aminorex
  • As wakefulness-promoting agents in the treatment of narcolepsy, e.g. amphetamine, methamphetamine
  • As nasal decongestants, e.g. levomethamphetamine, propylhexedrine, ephedrine, pseudoephedrine, phenylpropanolamine

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

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

Selective NRAs include ephedrine, pseudoephedrine, phenylpropanolamine, levomethamphetamine, phentermine, and bupropion. These drugs also release dopamine to a much lesser extent, however, and bupropion is also a nicotinic acetylcholine receptor antagonist.

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What is Aptazapine?

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Introduction

Aptazapine (developmental code name CGS-7525A) is a tetracyclic antidepressant (TeCA) that was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed.

Outline

It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine.

Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).

This page is based on the copyrighted Wikipedia article < https://en.wikipedia.org/wiki/Aptazapine >; it is used under the Creative Commons Attribution-ShareAlike 3.0 Unported License (CC-BY-SA). You may redistribute it, verbatim or modified, providing that you comply with the terms of the CC-BY-SA.

What is Adrenergic?

Published on by Andrew Marshall7 Comments

Introduction

Adrenergic means “working on adrenaline (epinephrine) or noradrenaline (norepinephrine)” (or on their receptors). When not further qualified, it is usually used in the sense of enhancing or mimicking the effects of epinephrine and norepinephrine in the body.

Outline

Adrenergic nervous system, a part of the autonomic nervous system that uses epinephrine or norepinephrine as its neurotransmitter

Regarding proteins:

  • Adrenergic receptor, a receptor type for epinephrine and norepinephrine; subtypes include α1, α2, β1, β2, and β3 receptors
  • Adrenergic transporter (norepinephrine transporter), a protein transporting norepinephrine from the synaptic cleft into nerve cells

Regarding pharmaceutical drugs:

  • Adrenergic receptor agonist, a type of drug activating one or more subtypes of adrenergic receptors.
  • This includes drugs regulating blood pressure and antiasthmatic drugs.
  • Adrenergic receptor antagonist, a type of drug blocking one or more subtypes of adrenergic receptors.
  • This mainly includes drugs lowering blood pressure.
  • Adrenergic reuptake inhibitor, a type of drug blocking the norepinephrine transporter.
  • This includes antidepressants and drugs against ADHD.

This page is based on the copyrighted Wikipedia article < https://en.wikipedia.org/wiki/Adrenergic >; it is used under the Creative Commons Attribution-ShareAlike 3.0 Unported License (CC-BY-SA). You may redistribute it, verbatim or modified, providing that you comply with the terms of the CC-BY-SA.