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...
35S]GTPγS, α2A-adrenergic receptorG protein activationThe [(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, ...
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 .....
(2003) The [ 35 S]GTPgammaS binding assay: approaches and applications in pharmacology. Life Sci. 74 , 489–508.Harrison C, Traynor JR (2003) The [35S]GTPgammaS binding assay: approaches and applications in pharmacology. Life Sci 74(4):489–508...
G. (2010). "Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors". British Journal of Pharmacology, 161(6), 1238-49. doi:10.1111/j.1476-5381.2010.00963....
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...
The []GTPγS binding assay provides functional information on pertussis toxin-sensitive G-protein activation, complementing radioligand binding assays and conventional second messenger assays.doi:10.1016/S0014-2999(98)00518-4Peltonen, J MPihlavisto, M...
The primary ultra-high-throughput screen of the entire compound collection was accomplished on the Kalypsys (San Diego, CA) robotic platform at a concentration of 8 [micro]M using the 1,536-well [[sup.35]S]GTP[gamma]S SPA binding functional assay. The...
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...
The analgesic efficacy of opioid agonist methadone was quantitatively estimated using the Operational Model of Agonism in the tailflick assay. Methadone appeared to be intermediate in analgesic efficacy when compared to other opioid agonists examined previously. Next, the magnitude of analgesic tolerance ...