5-HT1A receptor-mediated G protein activation assessed by [35S]GTPγS binding in rat cerebral cortex

Add time:08/08/2019    Source:sciencedirect.com

To date, 5-hydroxytryptamine1A (5-HT1A) receptor-mediated functional assays (adenylyl cyclase inhibition, high-affinity GTPase activity and [35S]guanosine-5′-O-(γ-thio)-triphosphate ([35S]GTPγS) binding) have been performed mainly in hippocampal membranes. In the current study, 5-HT-stimulated G protein activation assays were carried out in rat cerebral cortical membranes. High-affinity GTPase activity was stimulated by 5-HT, but not by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). By contrast, 5-HT- and 8-OH-DPAT-stimulated [35S]GTPγS binding displayed sufficient dynamic range enough to warrant further pharmacological analysis. Under standard conditions, which were determined precisely in terms of the concentrations of GDP, MgCl2 and NaCl, the profile of 5-HT-stimulated [35S]GTPγS binding investigated using a series of 5-HT receptor agonists and antagonists clearly indicated the involvement of the 5-HT1A receptor subtype. There appeared to be no evidence supporting the presence of regional heterogeneity in coupling efficiency between 5-HT1A and G proteins in the hippocampus or cortex. This method is a useful tool for investigating functional coupling between postsynaptic 5-HT1A receptors and G proteins in cerebral cortical membranes.

We also recommend Trading Suppliers and Manufacturers of 5-METHOXY-3-(1,2,5,6-TETRAHYDRO-4-PYRIDINYL)-1H-INDOLE HEMISUCCINATE (cas 107008-28-6). Pls Click Website Link as below: cas 107008-28-6 suppliers

Prev:Correlation between low/high affinity ratios for 5-HT1A receptors and intrinsic activity
Next:Effects of atropine and azaprophen (cas 107010-27-5) on matching and detection in rhesus monkeys)