The receptor binding and cellular growth responses to exogenous epidermal growth factor (EGF) were studied using the DiFi cell line established from a familial adenomatous polyposis patient. The number of cell membrane EGF receptors on DiFi cells, as measured by competitive radioligand binding assays and Scatchard analysis of 125I-EGF binding isotherms, was calculated to be 4.8 x 10(6) receptor...

BACKGROUND AND PURPOSE The P2X(7) receptor exhibits complex pharmacological properties. In this study, binding of a [(3)H]-labelled P2X(7) receptor antagonist to human P2X(7) receptors has been examined to further understand ligand interactions with this receptor. EXPERIMENTAL APPROACH The P2X(7) receptor antagonist, N-[2-({2-[(2-hydroxyethyl)amino]ethyl}amino)-5-quinolinyl]-2-tricyclo[3.3.1....

Radioligand binding assays remain a common method for quantifying the effects of allosteric modulators at G protein-coupled receptors. The allosteric ternary complex model (ATCM) is the simplest model applied to derive estimates of modulator affinity (K(B)) and cooperativity (alpha), which are necessary for understanding structure-activity relationships. However, the increasing drive toward ass...

The interaction of human growth hormone with human lymphocytes from an established culture (IM-9) was studied using lz51-human growth hormone. The binding of l*51human growth hormone was rapid; with human growth hormone at 0.1 no a steady state was observed in 90 min at 30”. Bound labeled human growth hormone was dissociated rapidly by addition of excess unlabeled human growth hormone. Binding ...

Radioligand-binding assays can be used to obtain information about the binding characteristics of a ligand to its receptor or the general location of binding sites within a tissue or even provide evidence for the existence of a specific receptor. In the case of the cannabinoid receptor system, radioligand binding has been instrumental for each of these applications. While receptor binding can p...

The presence of a folate binding protein of high-affinity type (affinity constant 3.10(10) M-1, maximum folate binding 1.4 nM) in human semen was demonstrated in equilibrium dialysis experiments (37 degrees C, pH 7.4) with the radioligand 3H-folate. Radioligand dissociation from the binding protein was slow at pH 7.4, but rapid at pH 3.5. By use of rabbit antibodies against 25 kDa human milk fo...

In this work, we present a case study to explore the challenges associated with finding novel molecules for a receptor that has been studied in depth and has a wealth of chemical information available. Specifically, we apply a previously described protocol that incorporates explicit water molecules in the ligand binding site to prospectively screen over 2.5 million drug-like and lead-like compo...

To obtain drugs which are more selective at benzodiazepine (BZD) receptors, design and synthesis of functionally selective ligands for BZD receptors is the current strategy of our pharmaceutical chemistry department. The affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. Based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3, 4-oxadiazolo[a,2,3]-pyrimi...

In order to determine whether or not alpha-adrenoceptors are present in adrenal glands, radioligand receptor binding assay was performed in both Sprague-Dawley (SD) rat and human adrenal gland membranes. Radioligand binding assay using 3H-prazosin as an alpha 1-adrenoceptor ligand and 3H-yohimbine as an alpha 2-adrenoceptor ligand, clearly demonstrated alpha 1 and alpha 2 receptors present in b...