Binding studies receptor

Receptor binding studies have shown that H-LSD labels 5-HT2 receptors in neuronal tissue (Peroutka 1987). LSD has also been shown to bind with high affinity to a subtype of the 5-HTj receptor (5-HTjq), a site that also displays a high affinity for 5-HT (Glennon et al. 1986 Peroutka 1987). 

Hulme, E. C. and Birdsall, N. J. M., Strategy and tactics in receptor binding studies, in Receptor-Ligand Interactions A Practical Approach, Hulme, E. G, Ed., IRL Press, Oxford, 1992, chap. 4. 

Tahtaoui C, Guillier F, Klotz P, Galzi JL, Flibert M, Ilien B (2005) On the use of nonfluo-rescent dye labeled ligands in FRET-based receptor binding studies. J Med Chem 48 7847-7859... 

Consistent with receptor binding studies, k receptor mRNA is expressed in the claustrum and interpeduncular nucleus as well as the ventral tegmental area. High levels of k receptor mRNA levels are expressed in the substantia nigra pars compacta, suggestive that k receptors may be expressed in dopaminergic neurons with a presynaptic location. 

S. Langermann, el al., Receptor binding studies disclose a novel class of high-affinity inhibitors of the Escherichia coli FimH adhesin, Mol. Microbiol., 55 (2005) 441 155. 

The metabolism of heroin is of interest in connection with its pharmacological activities. Earlier opiate -receptor binding studies led to the belief that heroin is a prodrug acting through its metabolites 6-acetylmorphine and morphine [95]. However, heroin is now known to activate (5-receptors, whereas morphine activates -receptor and 6-acetylmorphine acts at both receptor types [96]. Thus, the pharmacodynamic profile of heroin results from both direct and metabolite-mediated effects. 

Finally, a thorough receptor binding study by Raffa and colleagues (1998) showed that hypericin extracts had no effect at adrenergic (alpha or beta), adenosine, angiotensin, benzodiazepine, dopamine, bradykinin, neuropeptide Y, PCP, NMDA, opioid, cholecystokinin A, histamine HI, or nicotinic ACh receptors. Although comprehensive, this study did not look at the binding of any other hypericum constituents. 

Computation of data obtained by enzyme kinetic experiments, or receptor binding studies using sophisticated software, are state of... 

The main plots used in enzyme kinetics and receptor binding studies are the Scatchard plot, the Lineweaver-Burk plot, and the linearization for estimation of the Hill coefficient. This chapter gives a short survey of these transformations of enzyme kinetics or receptor binding data. 

Holzl, J. and Godau, P. (1989) Receptor binding studies with Valeriana officinalis on the benzodiazepine receptor. Planta Med 55 642. 

When using QSAR calculations to optimize a drug for the pharmacodynamic phase, it is important to use relevant biological activities. If in vivo activities are used, the bioactivities will be influenced by pharmacokinetic and pharmaceutical factors. In order for QSAR calculations to reflect the pharmacodynamic phase, the bioactivities should be based on in vitro data — optimally, receptor binding studies. 

Receptor-Binding Studies. Risperidone (Risperdal) is a benzisoxazole derivative that has a relatively high 5-HT " tio and relatively fewer and milder EPS than neuroleptics at its clinically effective doses. Receptor-binding studies of risperidone and its active metabolite, 9-OH-risperidone, in comparison with other novel antipsychotics revealed that ... 

Receptor-Binding Studies. Quetiapine (Seroquel) is also a dibenzothiazepine derivative produced by altering the structure of clozapine. This agent has an affinity for multiple brain receptors, a low propensity to evoke EPS in preclinical tests considered predictive of antipsychotic activity, and does not produce sustained plasma prolactin levels. 

Receptor-Binding Studies. Among the newer atypical antipsychotics, ziprasidone (Geodon) has a distinctive pharmacological profile ( Fig. 5-2). Binding studies indicate that ziprasidone has a high affinity for D 2 receptors, approximately equal to that of risperidone. In vitro, ziprasidone ... 

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