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Serotonin Antagonist and Reuptake Inhibitor Information

Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as anxiolytics and hypnotics. They act by antagonizing serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally, most also act as α1-adrenergic receptor antagonists. The majority of the currently marketed SARIs belong to the phenylpiperazine class of compounds.

Contents

List of SARIs

Vilazodone is a related drug but does not fit into this class as it does not function as a serotonin antagonist, acting as a 5-HT1A receptor partial agonist instead.

Niaprazine is also related to this group but does not inhibit the reuptake of serotonin or the other monoamines, so it does not fit either.

Pharmacology

Binding profile

The affinities (Kd (nM)) of a selection of SARIs have been compared below at an assortment of binding sites:[1][2][3][4]

Compound SERT NET DAT 5-HT1A 5-HT2A α1 α2 D2 H1 mACh
Etoperidone 890 20,000 52,000 85 36 38 570 2,300 3,100 >35,000
Nefazodone 200 360 360 80 26 48 640 910 24,000 11,000
Trazodone 160 8,500 7,400 78 16 39 405 3,650 725 324,000

The selected ligands act as antagonists (or inverse agonists depending on the site in question) at all receptors listed except at 5-HT1A where they are partial agonists,[5] and as inhibitors of all transporters listed.[1][2][3][4]

See also

References

  1. ^ a b Tatsumi M, Groshan K, Blakely RD, Richelson E (December 1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology 340 (2–3): 249–58. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(97)01393-9.
  2. ^ a b Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro". European Journal of Pharmacology 132 (2–3): 115–21. doi:10.1016/0014-2999(86)90596-0. PMID 3816971.
  3. ^ a b Richelson E, Nelson A (July 1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". The Journal of Pharmacology and Experimental Therapeutics 230 (1): 94–102. PMID 6086881. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6086881.
  4. ^ a b Cusack B, Nelson A, Richelson E (May 1994). "Binding of antidepressants to human brain receptors: focus on newer generation compounds". Psychopharmacology 114 (4): 559–65. doi:10.1007/BF02244985. PMID 7855217.
  5. ^ Odagaki Y, Toyoshima R, Yamauchi T (May 2005). "Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35SGTPgammaS binding"]. Journal of Psychopharmacology (Oxford, England) 19 (3): 235–41. doi:10.1177/0269881105051526. PMID 15888508. http://jop.sagepub.com/cgi/pmidlookup?view=long&pmid=15888508.
Antidepressants (N06A)
Specific reuptake inhibitors (RIs), enhancers (REs), and releasing agents (RAs)
Selective serotonin reuptake inhibitors (SSRIs)
Serotonin–norepinephrine reuptake inhibitors (SNRIs)
Serotonin–norepinephrine–dopamine reuptake inhibitors (SNDRIs)
Norepinephrine reuptake inhibitors (NRIs)
Dopamine reuptake inhibitors (DRIs)
Norepinephrine-dopamine reuptake inhibitors (NDRIs)
Norepinephrine-dopamine releasing agents (NDRAs)
Serotonin-norepinephrine-dopamine releasing agents (SNDRAs)
Selective serotonin reuptake enhancers (SSREs)
Others
Receptor antagonists and/or reuptake inhibitors
Serotonin antagonists and reuptake inhibitors (SARIs)
Noradrenergic and specific serotonergic antidepressants (NaSSAs)
Norepinephrine-dopamine disinhibitors (NDDIs)
Serotonin modulators and stimulators (SMSs)
Others
Heterocyclic antidepressants (bi-, tri-, and tetracyclics)
Bicyclics
Tricyclics
Tetracyclics
Monoamine oxidase inhibitors (MAOIs)
Nonselective
MAOA-Selective
MAOB-Selective
Azapirones and other 5-HT1A receptor agonists

: PSO/PSI

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proc(/), drug(/////)
Anxiolytics (N05B)
GABAA PAMs
Benzodiazepine Adinazolam • Alprazolam • Bretazenil • Bromazepam • Camazepam • Chlordiazepoxide • Clobazam • Clonazepam • Clorazepate • Clotiazepam • Cloxazolam • Diazepam • Ethyl Loflazepate • Etizolam • Fludiazepam • Halazepam • Imidazenil • Ketazolam • Lorazepam • Medazepam • Nordazepam • Oxazepam • Pinazepam • Prazepam
Carbamates Emylcamate • Mebutamate • Meprobamate (Carisoprodol, Tybamate) • Phenprobamate • Procymate
Nonbenzodiazepines Abecarnil • Adipiplon • Alpidem • CGS-8216 • CGS-9896 • CGS-13767 • CGS-20625 • Divaplon • ELB-139 • Fasiplon • GBLD-345 • Gedocarnil • L-838,417 • NS-2664 • NS-2710 • Ocinaplon • Pagoclone • Panadiplon • Pipequaline • RWJ-51204 • SB-205,384 • SL-651,498 • Taniplon • TP-003 • TP-13 • TPA-023 • Y-23684 • ZK-93423
Pyrazolopyridines Cartazolate • Etazolate • ICI-190,622 • Tracazolate
Others Chlormezanone • Ethanol (Alcohol) • Etifoxine • Kavalactones (Kava Kava) • Skullcap • Valerenic Acid (Valerian)
α2δ VDCC Blockers Gabapentin • Pregabalin
5-HT1A Agonists Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists Antalarmin • CP-154,526 • Pexacerfont • Pivagabine
NK2 Antagonists GR-159,897 • Saredutant
MCH1 antagonists ATC-0175 • SNAP-94847
mGluR2/3 Agonists Eglumegad
mGluR5 NAMs Fenobam
TSPO agonists DAA-1097 • DAA-1106 • Emapunil • FGIN-127 • FGIN-143
σ1 agonists Afobazole • Opipramol
Others Benzoctamine • Carbetocin • Demoxytocin • Mephenoxalone • Mepiprazole • Oxanamide • Oxytocin • Promoxolane • Tofisopam • Trimetozine • WAY-267,464

: PSO/PSI

(, , , , , , ), /,

proc(/), drug(/////)
Adrenergics
Receptor ligands
α1
α2
β
Reuptake inhibitors
NET
VMAT
Releasing agents
Enzyme inhibitors
Anabolism
PAH
TH
AAAD
DBH
PNMT
  • CGS-19281A
  • SKF-64139
  • SKF-7698
Catabolism
MAO
COMT
Others
Precursors
Cofactors
Others
List of adrenergic drugs
Dopaminergics
Receptor ligands
Agonists
Antagonists
Reuptake inhibitors
Plasmalemmal
DAT inhibitors
Vesicular
VMAT inhibitors
Releasing agents
Allosteric modulators
  • Quinazolinamines: SoRI-9804
  • SoRI-20040
  • SoRI-20041
Enzyme inhibitors
Anabolism
PAH inhibitors
TH inhibitors
AAAD/DDC inhibitors
Catabolism
MAO inhibitors
COMT inhibitors
DBH inhibitors
Others
Precursors
Cofactors
Others
List of dopaminergic drugs
Serotonergics
5-HT1 receptor ligands
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2 receptor ligands
5-HT2A
5-HT2B
5-HT2C
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Reuptake inhibitors
SERT
VMAT
Releasing agents
Enzyme inhibitors
Anabolism
TPH
AAAD
Catabolism
MAO
Others
Precursors
Cofactors
Others

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