Radioligand-receptor binding

Carpenter, J.W. et al. 2002. Configuring radioligand receptor binding assays for HTS using scintillation proximity assay technology. Meth. Mol. Biol. 190, 31—49. 

M Zhu, NG Bowery, PM Greengrass, JD PhiUipson. Application of radioligand receptor binding assays in the search for CNS active principles from Chinese medicinal plants. J Ethnopharmacol 54 153—164, 1996. 

Neonicotinoids do not act as a homogenous class of insecticides. Radioligand receptor binding assays revealed two classes of neonicotinoids described here as competitive and non-competitive , respectively, relative to [ H]imidacloprid. Differences in affinity, mode of displacement, number of binding sites and temperature sensitivity suggest that thiamethoxam binds in a way unique among the commercial neonicotinoids. Metabolic transformation is not relevant for its insecticidal effects. 

The Langmuir adsorption isotherm for radioligand binding [A ] to a receptor to form a radioligand-receptor complex [A R] can be rewritten in terms of one where it is not assumed that receptor binding produces a negligible effect on the free concentration of ligand ([A free]) ... 

Allosteric modulators affect the interaction of the receptor and probe molecules (i.e., agonists or radioligands) by binding to separate sites on the receptor. 

Aim To measin e the binding of a radioligand (or ligand that is traceable by other means) to a receptor. The object is to obtain an estimate of the equilibrium dissociation constant of the radioligand-receptor complex (denoted Kd) and the maximal number of binding sites (denoted Umax)-... 

Gatley SJ, Lan R, Volkow ND, Papas N, King P, Wong CT, Gilford AN, Pyatt B, Dewey SL, Makriyannis A. Imaging of the brain marijuana receptor—Development of a radioligand that binds to cannabinoid CB1 receptors in vivo. J Neurochem 1998 70 417 423. 

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