Tag: NaSSA: Noradrenergic and Specific Serotonergic Antidepressant

What is Aptazapine?

Published on by Andrew MarshallLeave a comment

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 an Noradrenergic and Specific Serotonergic Antidepressant?

Published on by Andrew Marshall4 Comments

Introduction

Noradrenergic and specific serotonergic antidepressants (NaSSAs) are a class of psychiatric drugs used primarily as antidepressants.

They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, 5-HT6, and/or 5-HT7 in some cases. By blocking α2-adrenergic autoreceptors and heteroreceptors, NaSSAs enhance adrenergic and serotonergic neurotransmission in the brain involved in mood regulation, notably 5-HT1A-mediated transmission. In addition, due to their blockade of certain serotonin receptors, serotonergic neurotransmission is not facilitated in unwanted areas, which prevents the incidence of many side effects often associated with selective serotonin reuptake inhibitor (SSRI) antidepressants; hence, in part, the “specific serotonergic” label of NaSSAs.

List of NaSSAs

The NaSSAs include the following agents:

  • Aptazapine (CGS-7525A)
  • Esmirtazapine (ORG-50,081)
  • Mianserin (Bolvidon, Norval, Tolvon)
  • Mirtazapine (Norset, Remeron, Avanza, Zispin)
  • Setiptiline/teciptiline (Tecipul)

Notably, all of these compounds are analogues and are also classified as tetracyclic antidepressants (TeCAs) based on their chemical structures.

S32212, a structurally novel NaSSA with an improved selectivity profile (e.g., no antihistamine effects, etc.), was reported in 2012. It has completed preliminary preclinical research and may go on to undergo clinical trials.

This page is based on the copyrighted Wikipedia article < https://en.wikipedia.org/wiki/Noradrenergic_and_specific_serotonergic_antidepressant >; 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.