Glucocorticoid Receptor Research

With this early success the further evolution of the first-generation steroidal glucocorticoids was started, and the stage for later syntheses of potent synthetic steroids such as prednisolone, dexamethasone and fluocortolon was set [13]. 

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DeAngelo AB, Chavis C. 1990. Phthalate ester inhibition of glucocorticoid receptor (GR) binding activity in B6C3F1 mouse liver [abstract]. Proceedings of the Annual Meeting of the American Association for Cancer Research 31 86. 

Eidridge, J.C. Landfield, P.W. Cannabinoid Interactions with Glucocorticoid Receptors in Rat Hippocampus Brain Research (1990) 534 135-141... 

Lopez, J. F., Chalmers, D. T., Little, K, Y. and Watson, S. J. A. E. Bennett Research Award. Regulation of serotonin 1 A, glucocorticoid, and mineralocorticoid receptor in rat and human hippocampus implications for the neurobiology of depression. Biol. Psych. 43 547-573,1998. 

It has been hypothesized that depression could arise from a pathological enhancement of 5-HT2 receptor function. This view would concur with the observations that the functional activity of 5-HT2 receptors on the platelet membrane is enhanced in depression and the increase in the density of 5-HT2 receptors in the frontal cortex of brains from suicide victims. It is possible that enhanced 5-HT2 receptor function is associated primarily with anxiety, a common feature of depression, and that the increased activity of the 5-HT2 receptors results in an attenuation of the functioning of S-HT receptors thereby resulting in the symptoms of depression. Whether this change in the activity of S-HT receptors is due to direct effects of the altered 5-HT2 receptor function is uncertain. There is evidence that hypercortisolaemia, which is a characteristic feature of depression, reduces the activity of these receptors probably through central glucocorticoid type 2 receptors. Clearly further research is needed to determine the precise interaction between the 5-HT2 and 5-HTi receptor types. 

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