ARIMISTANE
Posted: Sun Sep 20, 2020 10:47 am
Arimistane (Androsta-3,5-diene-7,17-dione) is a metabolite of 7-Keto DHEA, not subject to conversion to Testosterone or Estrogen.
In fact, just like Exemestane (Aromasin), Arimistane is a steroid suicidal aromatase inhibitor (AI), and therefore exerts its action by irreversibly binding with covalent bond to aromatase producing enzymatic inactivation.
In addition, this compound has been shown to reduce Cortisol, increase LH (Luteinizing Hormone) and consequently increase Testosterone levels.
Arimistane acts as a false substrate for the aromatase enzyme and is transformed into an intermediate that irreversibly blocks the active site of the enzyme causing it to inactivate: this mechanism is also known as suicidal inhibition.
In other words, Arimistane, being structurally similar to the target (substrate) of the aromatase enzyme, binds irreversibly to this enzyme, thus preventing it from carrying out its action, that is, the conversion of androgens into estrogens.
The half-life of Arimistane is approximately 2.5 hours. It reaches peak plasma concentrations in approximately 2 hours and has a half-life of 2.5 hours without accumulation with repeated doses.
Given the short half-life, it is advisable to take the daily dosage divided into at least 2-3 equal doses to be taken away from meals, given its steroid structure.
Side effects attributed to the use of Arimistane are linked to an excessive drop in estrogen levels (if abused) and include joint pain, mood swings and decreased libido.
https://pubchem.ncbi.nlm.nih.gov/bioass ... ction=Topù
https://pubmed.ncbi.nlm.nih.gov/8035427/
In fact, just like Exemestane (Aromasin), Arimistane is a steroid suicidal aromatase inhibitor (AI), and therefore exerts its action by irreversibly binding with covalent bond to aromatase producing enzymatic inactivation.
In addition, this compound has been shown to reduce Cortisol, increase LH (Luteinizing Hormone) and consequently increase Testosterone levels.
Arimistane acts as a false substrate for the aromatase enzyme and is transformed into an intermediate that irreversibly blocks the active site of the enzyme causing it to inactivate: this mechanism is also known as suicidal inhibition.
In other words, Arimistane, being structurally similar to the target (substrate) of the aromatase enzyme, binds irreversibly to this enzyme, thus preventing it from carrying out its action, that is, the conversion of androgens into estrogens.
The half-life of Arimistane is approximately 2.5 hours. It reaches peak plasma concentrations in approximately 2 hours and has a half-life of 2.5 hours without accumulation with repeated doses.
Given the short half-life, it is advisable to take the daily dosage divided into at least 2-3 equal doses to be taken away from meals, given its steroid structure.
Side effects attributed to the use of Arimistane are linked to an excessive drop in estrogen levels (if abused) and include joint pain, mood swings and decreased libido.
https://pubchem.ncbi.nlm.nih.gov/bioass ... ction=Topù
https://pubmed.ncbi.nlm.nih.gov/8035427/