Cell-type specific differences in the GTPγS binding assay described above led us to hypothesize the existence of a cell-specific factor that influenced the transfer of signal from R to G or the basal activation state of G independent of receptor. To pursue the latter, we modified the membran...
Strange PG (2010) Use of the GTPγS ([ 35 S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors. Br J Pharmacol 161:1238–1249. : 10.1111/j.1476-5381.2010.00963.x...
Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors (2010) Use of the GTPgammaS ([35S]GTPgammaS and Eu- GTPgammaS) binding assay for analysis of ligand potency and efficacy at G protein-coupled .....
The [(35)S]GTPgammaS binding assay to measure G protein activation following agonist binding to G protein-coupled receptors (GPCRs) remains a powerful molecular technique to substantiate traditional pharmacological values of potency, efficacy, and affinity. The method described uses membrane preparations...
35S]GTPγS bindingCell linesHomogenateNarcolepsyIn vitro functional analyses of hypocretin/orexin receptor systems were performed using [ 125I]hypocretin radioreceptor and hypocretin-stimulated [ 35S]GTPγS binding assay in cell lines expressing human or canine (wild-type and narcoleptic-mutation) ...
independent (constitutive) [[sup.35]S]GTP[gamma]S binding were sensitive to changes in assay concentrations of sodium, magnesium, and the guanine nucleotide GDP; however, the potency of ABT-239 for inhibition of RAMH-stimulated [[sup.35]S]GTP[gam...
[35S]-GTPS) binding assay.2The rate of [35S]-GTPS binding was increased by dopamine in a dose-dependent manner in membranes from CHO cells stably expressing either the D2short or D2long dopamine receptor.3The dopamine-induced stimulation of [35S]-GTPS binding could be inhibited by a ...
This functional assay could provide useful new information about dopamine receptor/G protein coupling in the postmortem human brain, and reveal possible disease related alterations of the interaction between D(2)/D(3) receptors and G proteins. 展开 关键词: Dopamine receptor binding 多巴胺 年份: ...
[35S]GTPS binding to the right and in parallel.5The relative efficacy or intrinsic activity of a compound was affected differently by the differing concentrations of guanosine diphosphate (GDP) in the assay buffer, which should be taken into consideration when determining the relative efficacies of...
The present study demonstrates that agonist stimulated [(35)S]GTPgammaS binding autoradiography could be a suitable technique for the examination of dopamine-D(2)/D(3) receptors in the human brain. This functional assay could provide useful new information about dopamine receptor/G protein coupling...