[Pharmacological study of neuroreceptors and implications in neurological and psychiatric therapeutics].
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.
Maloteaux
J M
JM
D002478:Cells, Cultured; D006801:Humans; D007473:Ion Channels / Q000378:metabolism; D009419:Nerve Tissue Proteins / Q000378:metabolism; D010766:Phosphorylation; D011494:Protein Kinases / Q000378:metabolism; D015290:Second Messenger Systems / Q000502:physiology; D011984:Sensory Receptor Cells / Q000187:drug effects* / Q000378:metabolism; D013268:Stimulation, Chemical
C029152:G-substrate; D007473:Ion Channels; D009419:Nerve Tissue Proteins; D011494:Protein Kinases