PMID: 9004924Jan 1, 1996Paper

Pharmacological study of neuroreceptors and implications in neurological and psychiatric therapeutics

Bulletin et mémoires de l'Académie royale de médecine de Belgique
J M Maloteaux

Abstract

Neuroreceptors may be regulated by their mediators or by agonists, in order to reduce the sensitivity of target cells. The mechanisms of this regulation differ according to the cell type, the intensity and duration of the stimulation. Rapid desensitization may be due to different molecular modifications (conformational changes of ionic channels, phosphorylation, affinity change, reduced efficiency of the coupling with the second messenger...) and may be followed by receptor internalization, recycling (reappearance of the receptors at the cell surface) or degradation when the stimulation is long lasting. The use of different cell types, including transfected cells, and the study of different receptor sub-types, allowed to better characterize the regulation processes and the effects of drugs on these mechanisms.

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