@Mauritio its mostly inhibiting just the variant there (not normal androgen receptors) splice variants lack parts that de-activate them so continually active https://www.nature.com/articles/nrurol.2015.13
ironically depleting androgens in prostate cancer can induce more of them (and more significant amounts in the extracted cells part but idk how much they contribute)
https://aacrjournals.org/clincancerres/article/20/6/1590/211454/Rapid-Induction-of-Androgen-Receptor-Splice
AR-FL (normal receptors) arent getting inhibited much but AR- variants gone
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1 found mild estrogenic activity in vitro in cancered cell lines which doesnt match with the in vivo anti tumor activity,
but mainly on ERRy and ERRa estrogen related receptor, 30% max transcriptional activity of estradiol on estrogen receptors, (maybe displacing estrogens for milder effect lower transcription? but potent on ERRs in these cells)
,
https://www.sciencedirect.com/science/article/abs/pii/S0300483X21001281
They found some hormone reducing effects in fish but idk how relevant to mammals
In adrenocortical cancer cells it reduced hormones production at nM concentration,
https://academic.oup.com/jcem/article/103/10/3706/5056322
- It has a mutagenic effect at higher end dose
humans show lymphocyte abnormalities from treatment at higher end dose. apparently its lethal in 100% of some strains of mice injected at low dose 7.5mg/kg. needs to be transformed in the gastrointestinal tract first & go through the liver https://pubmed.ncbi.nlm.nih.gov/3278217/
orally 60mg/kg ~300mg-400mg human dose starts to give a rise in abnormal sperm
its a mild effect there but thats only with 5 consecutive days
in humans the mutagenic effects on lymphocytes with 1g-2g for a day then 6 days of 500mg increased. (i'd guess red blood cells might be more vulnerable) doi: 10.1016/0165-7992(86)90015-1)
so to be on the safer side i wouldn't take >100mg of this regularly, 25mg has effects. and maybe good to have a few days off a week just incase.
@Mauritio said in Niclosamide reduces serotonin and glutamate:
Didn't you write something about cancer and pH? Niclosamide seems to affect that :
https://pubmed.ncbi.nlm.nih.gov/22474287/
cool thanks , yeah lowering pH to a certain level helps make the apoptosis process more effective