View source for Chemistry:Noradrenergic and specific serotonergic antidepressant

{{short description|Class of antidepressants}}
[[File:Mirtazapine.svg|right|thumb|185px|Chemical structure of the prototypical NaSSA [[Chemistry:Mirtazapine|mirtazapine]] (original brand name '''Remeron''').]]

'''Noradrenergic and specific serotonergic antidepressants''' ('''NaSSAs''') are a class of psychiatric drugs used primarily as [[Chemistry:Antidepressant|antidepressant]]s.<ref name="Julien2004">{{cite book | author = Robert M. Julien | title = A Primer Of Drug Action: A Comprehensive Guide To The Actions, Uses, And Side Effects Of Psychoactive Drugs | url = https://books.google.com/books?id=fhNkIsK4y9QC&pg=PA286 | access-date = 23 April 2012 | date = 17 September 2004 | publisher = Macmillan | isbn = 978-0-7167-0615-1 | pages = 286}}</ref> They act by [[Biology:Receptor antagonist|antagonizing]] the α<sub>2</sub>-adrenergic receptor and certain [[Chemistry:Serotonin receptor|serotonin receptor]]s such as [[Biology:5-HT2A receptor|5-HT<sub>2A</sub>]] and [[Biology:5-HT2C receptor|5-HT<sub>2C</sub>]],<ref name="Julien2004" /> but also [[Biology:5-HT3 receptor|5-HT<sub>3</sub>]],<ref name="Julien2004" /> [[Biology:5-HT6 receptor|5-HT<sub>6</sub>]], and/or [[Biology:5-HT7 receptor|5-HT<sub>7</sub>]] in some cases. By blocking α<sub>2</sub>-adrenergic [[Biology:Autoreceptor|autoreceptor]]s and [[Biology:Heteroreceptor|heteroreceptor]]s, NaSSAs enhance [[Biology:Adrenergic|adrenergic]] and [[Chemistry:Serotonin|serotonergic]] [[Biology:Neurotransmission|neurotransmission]] in the [[Biology:Brain|brain]] involved in mood regulation,<ref name="Julien2004" /> notably [[Biology:5-HT1A receptor|5-HT<sub>1A</sub>]]-mediated transmission.<ref name="HalesShahrokh2009">{{cite book | author1 = Robert E. Hales | author2 = Narriman C. Shahrokh | author3 = Alan F. Schatzberg |author4=Charles B. Nemeroff | title = Study Guide to Psychopharmacology: A Companion to the American Psychiatric Publishing Textbook of Psychopharmacology, Fourth Edition | url = https://books.google.com/books?id=--BsJw_A7UwC&pg=PA202 | access-date = 23 April 2012 | date = 28 April 2009 | publisher = American Psychiatric Pub | isbn = 978-1-58562-354-9 | page = 202}}</ref> In addition, due to their blockade of certain serotonin receptors, serotonergic neurotransmission is not facilitated in unwanted areas, which prevents the incidence of many [[Medicine:Side effect|side effect]]s often associated with [[Chemistry:Selective serotonin reuptake inhibitor|selective serotonin reuptake inhibitor]] (SSRI) antidepressants;<ref name="Julien2004" /><ref name="Publishers1998">{{cite book | author = Bentham Science Publishers | title = Current Pharmaceutical Design | url = https://archive.org/details/bub_gb_LjNh9ASGehUC | access-date = 23 April 2012 | date = August 1998 | publisher = Bentham Science Publishers | page = [https://archive.org/details/bub_gb_LjNh9ASGehUC/page/n12 298]}}</ref> hence, in part, the "specific serotonergic" label of NaSSAs.<ref name="HalesShahrokh2009" />

==List of NaSSAs==
The NaSSAs include the following agents:

* [[Chemistry:Aptazapine|Aptazapine]] (CGS-7525A)
* [[Chemistry:Esmirtazapine|Esmirtazapine]] (ORG-50,081)
* [[Chemistry:Mianserin|Mianserin]] (Bolvidon, Norval, Tolvon)<ref name="Carlstedt2009">{{cite book | author = Roland A. Carlstedt | title = Handbook of Integrative Clinical Psychology, Psychiatry, and Behavioral Medicine: Perspectives, Practices, and Research | url = https://books.google.com/books?id=4Tkdm1vRFbUC&pg=PA290 | access-date = 23 April 2012 | date = 14 December 2009 | publisher = Springer Publishing Company | isbn = 978-0-8261-1094-7 | page = 290}}</ref>
* [[Chemistry:Mirtazapine|Mirtazapine]] (Norset, Remeron, Avanza, Zispin)<ref name="Carlstedt2009" />
* [[Chemistry:Setiptiline|Setiptiline/teciptiline]] (Tecipul)

Notably, all of these compounds are [[Chemistry:Structural analog|analogues]] and are also classified as tetracyclic antidepressants (TeCAs) based on their [[Chemistry:Chemical structure|chemical structure]]s.

[[Chemistry:S32212|S32212]], a structurally novel NaSSA with an improved [[Chemistry:Binding selectivity|selectivity]] profile (e.g., no [[Chemistry:Antihistamine|antihistamine]] effects, etc.), was reported in 2012.<ref name="pmid22178752">{{cite journal  |vauthors=Millan MJ, Mannoury la Cour C, Chanrion B, etal | title = S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 340 | issue = 3 | pages = 750–64 |date=March 2012 | pmid = 22178752 | doi = 10.1124/jpet.111.187468 | s2cid = 8546314 }}</ref><ref name="pmid22178753">{{cite journal  |vauthors=Dekeyne A, Brocco M, Loiseau F, etal | title = S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and electrophysiological characterization | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 340 | issue = 3 | pages = 765–80 |date=March 2012 | pmid = 22178753 | doi = 10.1124/jpet.111.187534 | s2cid = 11363664 }}</ref> It has completed preliminary preclinical research and may go on to undergo [[Engineering:Clinical trial|clinical trial]]s.

==See also==
* [[Chemistry:Serotonin antagonist and reuptake inhibitor|Serotonin antagonist and reuptake inhibitor]] (SARI)
* [[Chemistry:Serotonin modulator and stimulator|Serotonin modulator and stimulator]] (SMS)
* Norepinephrine-dopamine disinhibitor (NDDI)
* Tetracyclic antidepressant
* [[Chemistry:Norepinephrine–dopamine reuptake inhibitor|Norepinephrine–dopamine reuptake inhibitor]]
* [[Chemistry:Atypical antidepressant|Atypical antidepressant]]

==References==
{{Reflist}}

==Further reading==
* {{cite journal | author = Kent JM | title = SNaRIs, NaSSAs, and NaRIs: new agents for the treatment of depression | journal = Lancet | volume = 355 | issue = 9207 | pages = 911–8 |date=March 2000 | pmid = 10752718 | doi = 10.1016/S0140-6736(99)11381-3 | s2cid = 27686300 | doi-access = free }}

==External links==

{{Antidepressants}}
{{Adrenergic receptor modulators}}
{{Serotonin receptor modulators}}

[[Category:Alpha-2 blockers]]
[[Category:Serotonin receptor antagonists]]

{{Sourceattribution|Noradrenergic and specific serotonergic antidepressant}}