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Fluoxymesterone
Profile by Type-IIx
An 11β-hydroxylated orally administered AAS. 5α-reducible and relatively nonestrogenic.
Potently androgenic. Therapeutic use obtains efficacy from this feature of its design.
Exerts a potent antiglucocorticoid effect. Also, weakly binds the GR [2], whether exerting agonist or antagonist action is unknown. The antiglucorticoid action occurs via 11β-HSD2 inhibition [3]:
11β-HSD2: enzyme that controls the oxidation of cortisol. Its inhibition leads to glucocorticoid-mediated MR activation, potassium excretion, sodium and water retention, and increased blood pressure (Ferrari, 2010; Ferrari et al., 2001; Serra et al., 2002) [3]. Halotestin competitively inhibits 11β-HSD2, thereby leading to glucocorticoid-mediated MR activation [3]. AAS that inhibit this enzyme may aggravate atherosclerosis via MR activation and inflammatory processes in the vascular endothelium (Glazer, 1991; Thompson et al., 1989) [3].
Mechanisms in promoting aggression/strength and anti-adpogenic/hardening effects
Mechanism in aggression/strength: competitive inhibition of cortisol oxidation [3]. Compared with cortisol, fluoxymesterone ~3-5x less efficiently converted to its 11-oxo form, resembling the conversion of dexamethasone [3]. The presence of an 11-oxo group tends to promote tissue-specific cortisol modulation which may lead to greater visceral fat loss and increased glycogen deposition.
Mechanism in anti-adipogenic/lipolytic ("hardening") effect: { Link to Compounds: Anti-adipogenic mechanisms }
… [analogous to DHT] inhibits adipogenic differentiation of hMSCs and human preadipocytes through an AR-mediated pathway, but it does not affect the proliferation of either hMSCs or preadipocytes. Androgen effects on fat mass represent the combined effect of decreased differentiation of fat cell precursors, increased lipolysis, and reduced lipid accumulation. [4].
Practical
Used frequently by strength athletes for its potent raw strength/power augmentation ("peaking"). Its relative toxicity is a consideration for dose/duration. A typical course may be 30mg daily x 4 weeks, with 40-60mg a day the last few days before competition. May also be used during a strength cycle in a pulsed fashion, to peak for PR/PB attempts. Bodybuilders use frequently for its "hardening" (anti-adipogenic) effect at the end of a prep cycle, typically after cutting out injectables. Doses may scale up based on body mass. May be used by combat athletes prior to a fight for its aggression-promoting effects and for focus/clarity (anecdotally), though { Link to Cheque drops/mibolerone } may be preferred under the assumption of its being relatively undetectable in urine post-fight (anecdotally).
Practical consequences
Impaired corticosteroid metabolism and activation of minerolocorticoid receptor (MR) has been associated with cardiovascular disease (Briet and Chiffrin, 2010; Hadoke et al., 2009; Lastra et al., 2010) [3].
__________
References:
[1] Vida, J. Androgens and anabolic agents (1969).
[2] Houtman, C. J., Sterk, S. S., van de Heijning, M. P. M., Brouwer, A., Stephany, R. W., van der Burg, B., & Sonneveld, E. (2009). Detection of anabolic androgenic steroid abuse in doping control using mammalian reporter gene bioassays. Analytica Chimica Acta, 637(1-2), 247–258. doi:10.1016/j.aca.2008.09.037
[3] Furstenberger, C., Vuorinen, A., Da Cunha, T., Kratschmar, D. V., Saugy, M., Schuster, D., & Odermatt, A. (2012). The Anabolic Androgenic Steroid Fluoxymesterone Inhibits 11 -Hydroxysteroid Dehydrogenase 2-Dependent Glucocorticoid Inactivation. Toxicological Sciences, 126(2), 353–361. doi:10.1093/toxsci/kfs022
[4] Gupta, V., Bhasin, S., Guo, W., Singh, R., Miki, R., Chauhan, P., … Jasuja, R. (2008). Effects of dihydrotestosterone on differentiation and proliferation of human mesenchymal stem cells and preadipocytes. Molecular and Cellular Endocrinology, 296(1-2), 32–40. doi:10.1016/j.mce.2008.08.019
Profile by Type-IIx
An 11β-hydroxylated orally administered AAS. 5α-reducible and relatively nonestrogenic.
Potently androgenic. Therapeutic use obtains efficacy from this feature of its design.
[1]
Exerts a potent antiglucocorticoid effect. Also, weakly binds the GR [2], whether exerting agonist or antagonist action is unknown. The antiglucorticoid action occurs via 11β-HSD2 inhibition [3]:
[3]
11β-HSD2: enzyme that controls the oxidation of cortisol. Its inhibition leads to glucocorticoid-mediated MR activation, potassium excretion, sodium and water retention, and increased blood pressure (Ferrari, 2010; Ferrari et al., 2001; Serra et al., 2002) [3]. Halotestin competitively inhibits 11β-HSD2, thereby leading to glucocorticoid-mediated MR activation [3]. AAS that inhibit this enzyme may aggravate atherosclerosis via MR activation and inflammatory processes in the vascular endothelium (Glazer, 1991; Thompson et al., 1989) [3].
Mechanisms in promoting aggression/strength and anti-adpogenic/hardening effects
Mechanism in aggression/strength: competitive inhibition of cortisol oxidation [3]. Compared with cortisol, fluoxymesterone ~3-5x less efficiently converted to its 11-oxo form, resembling the conversion of dexamethasone [3]. The presence of an 11-oxo group tends to promote tissue-specific cortisol modulation which may lead to greater visceral fat loss and increased glycogen deposition.
Mechanism in anti-adipogenic/lipolytic ("hardening") effect: { Link to Compounds: Anti-adipogenic mechanisms }
… [analogous to DHT] inhibits adipogenic differentiation of hMSCs and human preadipocytes through an AR-mediated pathway, but it does not affect the proliferation of either hMSCs or preadipocytes. Androgen effects on fat mass represent the combined effect of decreased differentiation of fat cell precursors, increased lipolysis, and reduced lipid accumulation. [4].
Practical
Used frequently by strength athletes for its potent raw strength/power augmentation ("peaking"). Its relative toxicity is a consideration for dose/duration. A typical course may be 30mg daily x 4 weeks, with 40-60mg a day the last few days before competition. May also be used during a strength cycle in a pulsed fashion, to peak for PR/PB attempts. Bodybuilders use frequently for its "hardening" (anti-adipogenic) effect at the end of a prep cycle, typically after cutting out injectables. Doses may scale up based on body mass. May be used by combat athletes prior to a fight for its aggression-promoting effects and for focus/clarity (anecdotally), though { Link to Cheque drops/mibolerone } may be preferred under the assumption of its being relatively undetectable in urine post-fight (anecdotally).
Practical consequences
Impaired corticosteroid metabolism and activation of minerolocorticoid receptor (MR) has been associated with cardiovascular disease (Briet and Chiffrin, 2010; Hadoke et al., 2009; Lastra et al., 2010) [3].
__________
References:
[1] Vida, J. Androgens and anabolic agents (1969).
[2] Houtman, C. J., Sterk, S. S., van de Heijning, M. P. M., Brouwer, A., Stephany, R. W., van der Burg, B., & Sonneveld, E. (2009). Detection of anabolic androgenic steroid abuse in doping control using mammalian reporter gene bioassays. Analytica Chimica Acta, 637(1-2), 247–258. doi:10.1016/j.aca.2008.09.037
[3] Furstenberger, C., Vuorinen, A., Da Cunha, T., Kratschmar, D. V., Saugy, M., Schuster, D., & Odermatt, A. (2012). The Anabolic Androgenic Steroid Fluoxymesterone Inhibits 11 -Hydroxysteroid Dehydrogenase 2-Dependent Glucocorticoid Inactivation. Toxicological Sciences, 126(2), 353–361. doi:10.1093/toxsci/kfs022
[4] Gupta, V., Bhasin, S., Guo, W., Singh, R., Miki, R., Chauhan, P., … Jasuja, R. (2008). Effects of dihydrotestosterone on differentiation and proliferation of human mesenchymal stem cells and preadipocytes. Molecular and Cellular Endocrinology, 296(1-2), 32–40. doi:10.1016/j.mce.2008.08.019
