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Dexamethasone – a synthetic glucocorticoid binds more powerfully to the glucocorticoid receptor than cortisol does. Dexamethasone is based on the cortisol structure but differs at three positions (extra double bond in the A-ring between carbons 1 and 2 and addition of a 9-α-fluoro group and a 16-α-methyl substituent).
Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones.Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are involved in a wide range of physiological processes, including stress response, immune response, and regulation of inflammation, carbohydrate metabolism ...
The glucocorticoid receptor (GR or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind. The GR is expressed in almost every cell in the body and regulates genes controlling the development , metabolism , and immune response .
Cortisol is a steroid hormone in the glucocorticoid class of hormones and a stress hormone.When used as medication, it is known as hydrocortisone.. It is produced in many animals, mainly by the zona fasciculata of the adrenal cortex in an adrenal gland. [1]
[7] mGRs appear to be partially involved in the anti-inflammatory and immunosuppressant effects of glucocorticoids. [3] [5] [14] mGRs are present in and appear to regulate many major bodily systems and organs, including the cardiovascular, immune, endocrine, and nervous systems, smooth and skeletal muscle, the liver, and fat tissue.
However, in humans, cortisol is the primary glucocorticoid that is produced primarily in the zona fasciculata of the adrenal cortex. Corticosterone has only weak glucocorticoid and mineralocorticoid potencies in humans and is important mainly as an intermediate in the steroidogenic pathway from pregnenolone to aldosterone.
Glucocorticoids also are in effect during times of stress for the sympathoadrenal system, but provide an inhibitory function for the protection of the body from its own immune system. The glucocorticoids work to inhibit reactions produced from the immune system during times of stress that could cause damage within the body. [4]
In some receptor systems (e.g. acetylcholine at the neuromuscular junction in smooth muscle), agonists are able to elicit maximal response at very low levels of receptor occupancy (<1%). Thus, that system has spare receptors or a receptor reserve. This arrangement produces an economy of neurotransmitter production and release. [12]