Anabolic activity

Quite recently great attention has been focused on steroids involving an isoxazole ring in the 2,3-position because of their anabolic activity. ... 

Another example of resort to heteroatoms to obtain both oral potency and a split between androgenic and anabolic activities Ls tiomestrone (99). Trienone, 98, prepared in much the same way as 23, undergoes sequential 1,6 and 1,4 conjugate addition of thioacetic acid under either irradiation or free radical catalysis to afford the compound containing two sulfur atoms. 

Anabolic activity. The ability of a drug to promote the synthesis of tissue constituents. 

The presence of a 7a-methyl group has been found to potentiate anabolic activity. Acetylation of 19-nortestosterone affords the corresponding 17-acetate... 

GH primarily displays an anabolic activity. It partially stimulates the growth of bone, muscle and cartilage cells directly. Binding of GH to its hepatic receptor results in the synthesis and release of... 

A major function of hGH is the promotion of anabolic activity, that is, bone and tissue growth due to increase in metabolic processes. Other biological effects of hGH are stimulation of protein synthesis, elevation of blood glucose level, and improvement of liver function. 

A number of studies were conducted in order to try and create a drug with high-androgenic and low-anabolic potential however, most attempts were unsuccessful. Because they are structurally similar to testosterone, they exhibit both androgenic and anabolic activity, and are frequently used by athletes for building up muscle mass. At the same time, all of the anabolics currently used have androgenic activity. 

GH primarily displays an anabolic activity. It partially stimulates the growth of bone, muscle and cartilage cells directly. Binding of GH to its hepatic receptor results in the synthesis and release of insulin-like growth factor (IGF-1), which mediates most of GH s growth-promoting activity on, for example, bone and skeletal muscle (Chapter 7). The major effeets mediated by hGH are summarized in Table 8.6. 

Anabolic activities of testosterone, such as increases in amino acid incorporation into protein and in RNA polymerase activity, have been demonstrated in skeletal muscle. Apart from the direct anabolic effects in specific tissue, androgens antagonize the protein catabolic action of glucocorticoids. The androgen compounds with the greatest ratio of protein anabolic effects to virilizing effects are the 19-nortestosterone derivatives. Compounds that are used clinically (Table 63.3) include nandrolone phenpropionate (Durabolin), nandrolone decanoate... 

C) Highly depressed protein anabolic activity in skeletal muscle, bone, and kidney... 

D) Use the androgen receptor to enhance protein anabolic activity... 

Table 40-5 Androgens Preparations Available and Relative Androgenic Anabolic Activity in Animals.

Apart from the antimicrobial growth promoters, there have been some other hormonal-type compounds with anabolic activity that are administered usually... 

Trenbolone acetate is a synthetic steroid with hormonal activity similar to testosterone but with greater anabolic activity. After administration to cattle, trenbolone acetate is rapidly hydrolyzed to its free hydroxylated form (28). The 17 -OH epimer is the major metabolite occurring in the excreta, bile, and liver. 

Ascorbic acid, folic acid, vitamins A and E are synergists with testosterone for maturation of germ cells and increased anabolic activity... 

Sometime in the 80 s athletes found out Zeranabol had anabolic activity. Since it is actually a form of estrogen, the drug increases nitrogen retention. IGF-1, GH, and Insulin secretion increases are also realized for the same reason. The result is some lean mass gain with high water retention. For the most part, users have realize HPTA function suppression at extreme rates, gyno, fat deposits, and head-aches. Oh, did I mention liver damage ... 

Research has shown a rapid and quite strong direct anabolic action from PG s in muscle cells. If PG s such as PGF-2 and PGE-2 are introduced into muscle cells, protein synthesis occurs at an incredible rate. If insulin is introduced into muscle cells with PGF-2 or PGE-2 there is a profound synergistic response. This places certain PG s among the most potent of anabolic activators. Perhaps far more so than anabolic steroids. This also suggests that the powerful anabolic actions of IGF-1, insulin, and amino acids are all mediated in one way or another by PG s. 

Most bodybuilders don t realize that the anabolic effects of Clenbuterol are not due to increased anabolic activity. Clenbuterol is actually effective through a different mechanism. It decreases both protein synthesis and break down. The reason anti-catabolic effects result is simply because it hinders protein break down more which shifts the ratio in favor of anabolism. This means that clenbuterol had significant anti-catabolic effects when stacked with a cortisol inhibitor post or during AAS cycles. Cytadren was an often noted example. Again, since clenbuterol increases thermal genesis, (calories released as heat) the common use of thyroid T-3 or T-4 in a stack with it caused a significant increase in body temperature. This was monitored closely by most. 

The ratio of androgenic to anabolic activity can vary in different molecules. There have been attempts to produce steroids with low androgenic but high anabolic activity to use for various... 

Testosterone This agent is ineffective orally because of inactivation by first-pass metabolism. As with the other sex steroids, testosterone is rapidly absorbed by the liver and other tissues, and is metabolized to relatively or completely inactive compounds that are excreted primarily in the urine but also in the feces. Testosterone and its C-17-esters (for example, testosterone cypi-onate or enanthate) are administered intramuscularly. [Note The addition of the esterified lipid makes the hormone more lipid-soluble, thereby increasing its duration of action.] Testosterone and its esters demonstrate a 1 1 relative ratio of androgenic to anabolic activity. 

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