Noradrenergic and specific serotonergic antidepressant

Class of antidepressants
Chemical structure of the prototypical NaSSA mirtazapine (original brand name Remeron)

Noradrenergic and specific serotonergic antidepressants (NaSSAs) are a class of psychiatric drugs used primarily as antidepressants.[1] They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C,[1] but also 5-HT3,[1] 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,[1] notably 5-HT1A-mediated transmission.[2] 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;[1][3] hence, in part, the "specific serotonergic" label of NaSSAs.[2]

List of NaSSAs

The NaSSAs include the following agents:

  • Aptazapine (CGS-7525A)
  • Esmirtazapine (ORG-50,081)
  • Mianserin (Bolvidon, Norval, Tolvon)[4]
  • Mirtazapine (Norset, Remeron, Avanza, Zispin)[4]
  • 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.[5][6] It has completed preliminary preclinical research and may go on to undergo clinical trials.

See also

References

  1. ^ a b c d e Robert M. Julien (17 September 2004). A Primer Of Drug Action: A Comprehensive Guide To The Actions, Uses, And Side Effects Of Psychoactive Drugs. Macmillan. p. 286. ISBN 978-0-7167-0615-1. Retrieved 23 April 2012.
  2. ^ a b Robert E. Hales; Narriman C. Shahrokh; Alan F. Schatzberg; Charles B. Nemeroff (28 April 2009). Study Guide to Psychopharmacology: A Companion to the American Psychiatric Publishing Textbook of Psychopharmacology, Fourth Edition. American Psychiatric Pub. p. 202. ISBN 978-1-58562-354-9. Retrieved 23 April 2012.
  3. ^ Bentham Science Publishers (August 1998). Current Pharmaceutical Design. Bentham Science Publishers. p. 298. Retrieved 23 April 2012.
  4. ^ a b Roland A. Carlstedt (14 December 2009). Handbook of Integrative Clinical Psychology, Psychiatry, and Behavioral Medicine: Perspectives, Practices, and Research. Springer Publishing Company. p. 290. ISBN 978-0-8261-1094-7. Retrieved 23 April 2012.
  5. ^ Millan MJ, Mannoury la Cour C, Chanrion B, et al. (March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization". The Journal of Pharmacology and Experimental Therapeutics. 340 (3): 750–64. doi:10.1124/jpet.111.187468. PMID 22178752. S2CID 8546314.
  6. ^ Dekeyne A, Brocco M, Loiseau F, et al. (March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and electrophysiological characterization". The Journal of Pharmacology and Experimental Therapeutics. 340 (3): 765–80. doi:10.1124/jpet.111.187534. PMID 22178753. S2CID 11363664.

Further reading

  • Kent JM (March 2000). "SNaRIs, NaSSAs, and NaRIs: new agents for the treatment of depression". Lancet. 355 (9207): 911–8. doi:10.1016/S0140-6736(99)11381-3. PMID 10752718. S2CID 27686300.

External links

  • Media related to Noradrenergic and specific serotonergic antidepressants at Wikimedia Commons
  • v
  • t
  • e
SSRIsTooltip Selective serotonin reuptake inhibitors
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors
NRIsTooltip Norepinephrine reuptake inhibitors
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants
SARIsTooltip Serotonin antagonist and reuptake inhibitors
SMSTooltip Serotonin modulator and stimulators
Others
TCAsTooltip Tricyclic antidepressants
TeCAsTooltip Tetracyclic antidepressants
Others
Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
Miscellaneous
  • v
  • t
  • e
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
  • See also: Receptor/signaling modulators
  • Dopaminergics
  • Serotonergics
  • Monoamine reuptake inhibitors
  • Monoamine releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins
  • v
  • t
  • e
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins