Regulation of monoamine receptors in the brain: dynamic changes during stress.

Monoamine receptors are membrane-bound receptors that are coupled to G-proteins. Upon stimulation by agonists, they initiate a cascade of intracellular events that guide biochemical reactions of the cell. In the central nervous system, they undergo diverse regulatory processes, among which are receptor desensitization, internalization into the cell, and downregulation. These processes vary among different types of monoamine receptors. alpha 2-Adrenoceptors are often downregulated by agonists, and beta-adrenoceptors are internalized rapidly. Others, such as serotonin1A-receptors, are controlled tightly by steroid hormones. Expression of these receptors is reduced by the "stress hormones" glucocorticoids, whereas gonadal hormones such as testosterone can counterbalance the glucocorticoid effects. Because of this, the pattern of monoamine receptors in certain brain regions undergoes dynamic changes when there are elevated concentrations of agonists or when the hormonal milieu changes. Stress is a physiological situation accompanied by the high activity of brain monoaminergic systems and dramatic changes in peripheral hormones. Resulting alterations in monoamine receptors are considered to be in part responsible for changes in the behavior of an individual.