Ad vocem fizjologicznych funkcji 5-HT3:
Since 5-HT3 receptor activation in the brain leads to dopamine release and 5-HT3 receptor antagonists produce central effects comparable to those of antipsychotics and anxiolytics, 5-HT3 receptor involvement in schizophrenia and anxiety was considered. 5-HT3 receptor antagonists have also been reported to induce cognition enhancing effects in rats, suggesting their potential use as memory enhancing agents.
To achieve the full effect of activation of this receptor, heteromeric combination of its two subtypes – 5-HT3A and 5-HT3B is required 5-HT3 antagonists (ondasetron, granisetron, tropisetron etc.) were confirmed for being clinically effective in the treatment of chemotherapy- or radiationinduced nausea and vomiting, whereas they are ineffective against motion sickness and apomorphine induced emesis. There are also indications that they may be effective in the treatment of migraine or migraine associated pain. Preclinical studies suggest that 5-HT3 antagonists may enhance memory and be of benefit in the treatment of anxiety, depression, pain and dementia. Finally, there is evidence that 5-HT3 antagonists may suppress the behavioral consequences of withdrawing chronic treatment with drugs of abuse, including alcohol, nicotine, cocaine, and amphetamine. There is only little evidence about the possible therapeutic application of 5-HT3 agonists; it seems that some partial agonists possess an anxiolytic profile.
-- 20 lip 2015, 13:49 --
Dodać mogę, że mianseryna również jest inhibitorem receptora 5-HT3:
dla enancjomeru (-) Ki=3,47 nM i dla enancjmeru (+) Ki=112,2 nM, uśredniając Ki=57,8 nM (bo mianseryna jest racematem).