CLINICAL PHARMACOLOGY SARM’s exert their anti-anabolic and anabolic effects by inhibiting one or more of the following: The following table summarizes the most common SARM’s.
The table provides a list of SARM’s, their mode of action and potential side effects (as documented by clinical trials) (1). Anabolic effects: The primary (anabolic) effect of an SARM is stimulation of anabolic activity of muscle tissue. The primary effect of blocking of the GH/IGF-1 system is to slow down and reduce the rate of loss of muscle tissue or lean body mass.
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If one were to block the GH/IGF-1 system by inhibiting the binding of IGF-1 to its receptor, this would block the negative feedback effect that blocks the anabolic activity of the GH/IGF-1 system. If the rate of loss of muscle tissue or lean body mass was reduced (e.g., increased rate of loss of lean body mass in a subject with anabolic disease), the negative feedback effect would be reduced and therefore anabolic activity of the GH/IGF-1 system would increase. As the negative feedback effect is reduced, there is an increased production of anabolic hormones (such as IGF-1) by muscle tissue.
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Therefore, a subject in anabolism (e.g., with low rate of loss of lean body mass) may be expected to have more muscle tissue than a subject in anabolism (e.g., with normal rate of loss of lean body mass). The increase in muscle tissue or increase in anabolic hormones is an important basis for the clinical pharmacology evaluation and the clinical profile of an SARM. The increase in anabolic hormones would also be expected to increase lean body mass. Increased lean body mass would be useful to a person in weight loss, to increase overall attractiveness, and to increase self-confidence. Other physiological changes may also be expected due to the increase in anabolic hormones.
One physiological change may be an increase in bone mineral density (BMD). This is beneficial in many subjects (e.g., elderly) who may lose bone tissue. SARMs may be anabolic agents (e.g., in anabolism) or catabolic agents (e.g., in catabolism). The physiological profile of an anabolic agent is different from the physiological profile of a catabolic agent. A catabolic agent will reduce body weight, body mass index (BMI), and/or fat tissue mass. A catabolic agent will also reduce lean body mass and bone mineral density (BMD).
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A typical example of a catabolic agent would be a glucocorticoid (e.g., dexamethasone). Glucocorticoids (e.g., glucocorticoids) are agents which bind to glucocorticoid receptors (e.g., GR receptors). Glucocorticoids are a group of hormones (e.g., cortisol, corticosterone, etc.) that are secreted by the adrenal cortex. There are two types of glucocorticoids (e.g., glucocorticoids): mineralocorticoids and glucocorticoids. Glucocorticoids are primarily responsible for maintaining metabolism, salt, and mineral homeostasis, and regulating the stress response. Glucocorticoids are the most important anabolic and catabolic agents (e.g., hormones). The physiological responses in response to a catabolic agent may also include an increase in muscle mass, but there would also be a decrease in body fat mass. In contrast to a catabolic agent, an anabolic agent is a chemical that causes the growth of tissue, such as bone. Agents which increase lean body mass are also termed anabolic agents.
Anabolic agents would be expected to cause an increase in bone mineral density. Anabolic agents would also be expected to cause an increase in lean body mass. An example of an anabolic agent would be insulin, which is a peptide hormone that functions as a primary regulator of metabolism and can be used to treat diabetes. Another example of an anabolic agent would be the hormone growth hormone, which is a peptide hormone that regulates the anabolism of proteins, carbohydrates, and lipids and plays a key role in postnatal growth and metabolism. Other examples of anabolic agents include the anabolic steroids, which are drugs or chemicals that increase the size and strength of skeletal muscle, although they have also been associated with masculinizing effects and may increase the risk of breast cancer. Anabolic agents are also used for treating muscle wasting associated with AIDS and other diseases. The anabolic drugs include the insulin growth factor and the anabolic steroids, and may be combined with a catabolic agent, such as a glucocorticoid.
The glucocorticoid is a steroid that is made by the body, and is an active agent that can be used to treat a variety of illnesses, such as rheumatoid arthritis, chronic inflammatory airway disease, ulcerative colitis, bronchial asthma and allergies, and osteoarthritis. In certain embodiments, a glucocorticoid and an anabolic agent may be coadministered to treat a condition of the gastrointestinal tract. A glucocorticoid may be used to treat a patient who has been suffering from the symptoms of gastric ulcer or duodenal ulcer. In certain embodiments, the glucocorticoid may be coadministered with a drug or agent