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La formebolona (nombres comerciales Esicle … La formebolona (nombres comerciales Esiclene, Hubernol, Metanor), también conocida (confusamente) como formildienolona, así como 2-formil-11α-hidroxi-17α-metil-δ1-testosterona, es un anabólico-androgénico esteroide (AAS) activo por vía oral. Descripto como un fármaco anabólico y anticatabólico que se comercializa o se ha comercializado en España e Italia Como AAS, muestra cierta actividad anabólica, aunque es inferior a la testosterona en términos de potencia, pero se dice que prácticamente no tiene actividad androgénica. La Formebolona contrarresta los efectos catabólicos (control del balance de nitrógeno) o glucocorticoides potentes como el fosfato de dexametasona. Un análogo cercano, la roxibolona (y su variante de éster de acción prolongada, la decilroxibolona), muestra una actividad antiglucocorticoide similar a la de la formbolona pero, por el contrario, carece de actividad como AAS. No se ha encontrado que la roxibolona se una al receptor de glucocorticoides, y se ha sugerido que la actividad antiglucocorticoide de la roxibolona y la formbelona puede estar mediada por la modulación de los procesos enzimáticos. De hecho, se sabe que la 11α- y la 11β-hidroxiprogesterona (la formebolona y la roxibolona están 11α- y 11β-hidroxiladas (respectivamente) de manera similar) son potentes inhibidores de la 11β-hidroxiesteroide deshidrogenasa (11β-HSD), que es responsable de la biosíntesis de la potente glucocorticoides endógenos cortisol y corticosterona (de los precursores desoxicortisol y desoxicorticosterona, respectivamente) Sin embargo, se encontró que la formebolona es un inhibidor muy débil de la 11β-HSD tipo 2 (IC50 10 μM), aunque esta isoenzima específica de la 11β-HSD es responsable de la inactivación de los glucocorticoides en lugar de su producción.ucocorticoides en lugar de su producción.
, Formebolone (INN, BAN) (brand names Esicle … Formebolone (INN, BAN) (brand names Esiclene, Hubernol, Metanor), also known as formyldienolone, as well as 2-formyl-11α-hydroxy-17α-methyl-δ1-testosterone, is an orally active anabolic-androgenic steroid (AAS) described as an anticatabolic and anabolic drug that is or has been marketed in Spain and Italy. As an AAS, it shows some anabolic activity, though it is inferior to testosterone in terms of potency, but is said to have virtually no androgenic activity. Formebolone counteracts the catabolic effects (control of nitrogen balance) of potent glucocorticoids like dexamethasone phosphate. A close analogue, roxibolone (and its long-acting ester variant ), shows similar antiglucocorticoid activity to formebolone but, in contrast, is devoid of activity as an AAS. Roxibolone has been found not to bind to the glucocorticoid receptor, and it has been suggested that the antiglucocorticoid activity of roxibolone and formebolone may instead be mediated by modulation of enzymatic processes. Indeed, 11α- and 11β-hydroxyprogesterone (formebolone and roxibolone being 11α- and 11β-hydroxylated (respectively) similarly) are known to be potent inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD), which is responsible for the biosynthesis of the potent endogenous glucocorticoids cortisol and corticosterone (from the precursors deoxycortisol and deoxycorticosterone, respectively). However, formebolone was found to be a very weak inhibitor of 11β-HSD type 2 (IC50 > 10 μM), although this specific isoenzyme of 11β-HSD is responsible for the inactivation of glucocorticoids rather than their production.cocorticoids rather than their production.
, Il formebolone (conosciuto anche come form … Il formebolone (conosciuto anche come formildienolone) è un derivato del testosterone, sintetizzato e studiato per ottenere un composto dotato di una estrogenicità inferiore rispetto a testosterone stesso. È uno steroide anabolizzante.Il suo utilizzo in molti paesi è sottoposto a controllo e potrebbe determinare violazione di norme di legge. In Italia formebolone fu posto in vendita dalla società farmaceutica , sia nella forma farmaceutica di compresse che in soluzione iniettabile, con il nome commerciale di Esiclene. Attualmente in questo paese l'utilizzo di steroidi anabolizzanti è regolamentato dalla legge in materia antidoping numero 376 del 14 dicembre 2000.ntidoping numero 376 del 14 dicembre 2000.
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Esiclene, Hubernol, Metanor
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Ball-and-stick model of the formebolone molecule
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Formyldienolone; 2-Formyl-11α-hydroxy-17α-methyl-δ1-testosterone
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| rdfs:comment |
Il formebolone (conosciuto anche come form … Il formebolone (conosciuto anche come formildienolone) è un derivato del testosterone, sintetizzato e studiato per ottenere un composto dotato di una estrogenicità inferiore rispetto a testosterone stesso. È uno steroide anabolizzante.Il suo utilizzo in molti paesi è sottoposto a controllo e potrebbe determinare violazione di norme di legge. In Italia formebolone fu posto in vendita dalla società farmaceutica , sia nella forma farmaceutica di compresse che in soluzione iniettabile, con il nome commerciale di Esiclene. Attualmente in questo paese l'utilizzo di steroidi anabolizzanti è regolamentato dalla legge in materia antidoping numero 376 del 14 dicembre 2000.ntidoping numero 376 del 14 dicembre 2000.
, Formebolone (INN, BAN) (brand names Esicle … Formebolone (INN, BAN) (brand names Esiclene, Hubernol, Metanor), also known as formyldienolone, as well as 2-formyl-11α-hydroxy-17α-methyl-δ1-testosterone, is an orally active anabolic-androgenic steroid (AAS) described as an anticatabolic and anabolic drug that is or has been marketed in Spain and Italy. As an AAS, it shows some anabolic activity, though it is inferior to testosterone in terms of potency, but is said to have virtually no androgenic activity. Formebolone counteracts the catabolic effects (control of nitrogen balance) of potent glucocorticoids like dexamethasone phosphate. A close analogue, roxibolone (and its long-acting ester variant ), shows similar antiglucocorticoid activity to formebolone but, in contrast, is devoid of activity as an AAS.contrast, is devoid of activity as an AAS.
, La formebolona (nombres comerciales Esicle … La formebolona (nombres comerciales Esiclene, Hubernol, Metanor), también conocida (confusamente) como formildienolona, así como 2-formil-11α-hidroxi-17α-metil-δ1-testosterona, es un anabólico-androgénico esteroide (AAS) activo por vía oral. Descripto como un fármaco anabólico y anticatabólico que se comercializa o se ha comercializado en España e Italia Como AAS, muestra cierta actividad anabólica, aunque es inferior a la testosterona en términos de potencia, pero se dice que prácticamente no tiene actividad androgénica. La Formebolona contrarresta los efectos catabólicos (control del balance de nitrógeno) o glucocorticoides potentes como el fosfato de dexametasona. Un análogo cercano, la roxibolona (y su variante de éster de acción prolongada, la decilroxibolona), muestra una actgada, la decilroxibolona), muestra una act
|
| rdfs:label |
Formebolone
, Formebolona
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