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Background
Tropisetron is an α7 nicotinic partial agonist with superior effects to GTS-21, which was shown to enhance cognition in healthy people [1]. Additionally it is a 5-HT3 antagonist which have a long history of benefits to mental health. Acting synergistically, 5-HT3 antagonism prevents nausea induced by α7 nicotinic partial agonism, while simultaneously giving it a dual nootropic effect. α7 nicotinic receptor partial agonism is neuroprotective and non-addictive, with literature suggesting the cognition enhancement by nicotine may be owed to this receptor, without the euphoric effects. This receptor is also responsible for the anti-inflammatory effects of nicotine, and more selective agonists for a7 such as GTS-21 (or Tropisetron) are much stronger.
Outside of the US, Tropisetron is a pharmaceutical. As such it has a wealth of human data, where it was shown repeatedly to be well tolerated, with little to no side effects. It is normally prescribed for chemotherapy-induced nausea in cancer patients, however it has been used experimentally with success as an analgesic in Fibromyalgia [2] and general treatment for Schizophrenia [3], where it was found to be quite successful. Tropisetron was also successful when tested for OCD [4]. Tropisetron trends to decrease anxiety in some studies, but with less efficacy than a benzodiazepine [5].
Its potential benefits to ADHD and depression are yet to be elucidated, but some preclinical data hint it may be advantageous. We hope to encourage such research by allowing researchers to buy Tropisetron.
Pharmacology
α7 nicotinic partial agonism increases calcium influx, but simultaneously prevents hyperactivation of the receptor, giving Tropisetron neuroprotective and pro-cognitive abilities. Increasing acetylcholine potentiates the nootropic effect of Tropisetron, and increasing cAMP potentiates its theoretical antidepressant effects in animal models. 5-HT3 antagonism produces a nootropic effect, in part by increasing acetylcholine release.
Pharmacokinetics
Tropisetron has superior pharmacokinetics with 60% oral bioavailability and a 6hr half life but duration that supersedes that.
References
[1] GTS-21 improves cognition in healthy people: https://www.nature.com/articles/1300028
[2] Tropisetron as an analgesic for Fibromyalgia: https://pubmed.ncbi.nlm.nih.gov/11028833/
[3] Tropisetron improves negative and cognitive symptoms in Schizophrenia: https://www.nature.com/articles/s41386-020-0685-0
[4] Tropisetron pilot study for OCD: https://pubmed.ncbi.nlm.nih.gov/31575326/
[5] Tropisetron mildly helps anxiety: https://pubmed.ncbi.nlm.nih.gov/7871001/
Disclaimer
Scientific discussion is purely for educational purposes. This is not medical advice.
