Some science behind the scenes

SAs

An SA is a serotonin antagonist,  a drug used to inhibit the action at serotonin (5-HT) receptors.  Within this class are a large number of research chemicals, used to counteract the effects of agonists in such things as clinical trials.  Ketanserin for example is frequently used in scientific research to study the serotonin system; specifically, the 5-HT2A receptor.

  • 5-HT2A antagonists tend to be used as atypical antipsychotics.  In the typical anti-psychotics agonists tend to be used
  • The 5-HT2A/2C antagonists are used as antihypertensives, antipsychotics and anti-depressants. 
  • The antagonists of the 5-HT3 receptors are usually anti-emetics or IBS drugs. The  5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they are used to treat post-operative and cytotoxic drug nausea & vomiting.

Other antagonists also exist.  Bufotenine is, according to the IUPHAR database an 5-HT1D and 5-HT2A antagonist [contradicting the Wikipedia entry].  For more details see Smoking toad venom!  Yohimbine is also an antagonist.  Many Serotonin antagonists also have antihistamine action

  • Atypical antipsychotics –including the older drugs such as clozapine and other drugs such as  risperidone.  Ziprasidone (marketed as Geodon, Zeldox) is marketed for depression, bipolar maintenance, and PTSD
  • Anti-anxiety drugs – such as Deramciclane
  • Anti-depressants – such as Etoperidone
  • Anti-histamines – such as Periactin
  • Alcohol abuse drugs – such as Metadoxine
  • Beta blockers – such as  alprenolol, cyanopindolol, iodocyanopindolol, oxprenolol, pindobind, pindolol, propranolol, tertatolol
  • Migraine treatments – such as Dotarizine, some of the Ergolines
  • Muscle relaxants – such as Flopropione also known as a spasmolytic or antispasmodic agent
  • PET scanning drugs - MPPF, [ 2'-methoxyphenyl-(N-2'-pyridinyl)-p-fluoro-benzamidoethyipiperazine] has been used as a radioligand with positron emission tomography
  • Anti-hypertension drugs – such as Bietaserpine, Deserpidine , Ketanserin [the profiling here is very contradictory] and and alpha blockers such as Dibenzyline
  • Anti-emetics - such as Ondansetron
  • IBS drugs – such as Alosetron hydrochloride (initial brand name: Lotronex)
  • Alzheimers drugs – such as Memantine which acts as a non-competitive antagonist at the 5-HT3 receptor, as an incidental action
  • Tetracyclic antidepressants  - such as  amoxapine, mianserin, mirtazapine
  • Volatiles/gases – such as  nitrous oxide, sevoflurane, and xenon
  • Serenics or antiaggression agents – only one appears to exist – Eltoprazine. It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor

Observations

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