Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.

alpha1-adrenergic receptor subtypes in human peripheral blood lymphocytes. (1/3334)

We investigated the expression of alpha1-adrenergic receptor subtypes in intact human peripheral blood lymphocytes using reverse transcription-polymerase chain reaction (RT-PCR) and radioligand binding assay techniques combined with antibodies against the three subtypes of alpha1-adrenergic receptors (alpha1A, alpha1B, and alpha1D). RT-PCR amplified in peripheral blood lymphocytes a 348-bp alpha1A-adrenergic receptor fragment, a 689-bp alpha1B-adrenergic receptor fragment, and a 540-bp alpha1D-adrenergic receptor fragment. Radioligand binding assay with [3H]prazosin as radioligand revealed a high-affinity binding with a dissociation constant value of 0. 65+/-0.05 nmol/L and a maximum density of binding sites of 175. 3+/-20.5 fmol/10(6) cells. The pharmacological profile of [3H]prazosin binding to human peripheral blood lymphocytes was consistent with the labeling of alpha1-adrenergic receptors. Antibodies against alpha1A-, alpha1B-, and alpha1D-receptor subtypes decreased [3H]prazosin binding to a different extent. This indicates that human peripheral blood lymphocytes express the three alpha1-adrenergic receptor subtypes. Of the three different alpha1-adrenergic receptor subtypes, the alpha1B is the most represented and the alpha1D, the least. Future studies should clarify the functional relevance of alpha1-adrenergic receptors expressed by peripheral blood lymphocytes. The identification of these sites may represent a step for evaluating whether they represent a marker of alpha1-adrenergic receptors in cardiovascular disorders or for assessing responses to drug treatment on these receptors.  (+info)

Kinetic analysis of drug-receptor interactions of long-acting beta2 sympathomimetics in isolated receptor membranes: evidence against prolonged effects of salmeterol and formoterol on receptor-coupled adenylyl cyclase. (2/3334)

The long-acting beta2 sympathomimetics salmeterol and formoterol have been presumed to exert their prolonged action either by binding to an accessory binding site ("exo-site") near the beta2 adrenoceptor or by their high affinity for beta2 adrenoceptors and correspondingly slow dissociation. Whereas most studies with salmeterol had been done in intact tissues, which have slow diffusion and compartmentation of drugs in lipophilic phases, that restrict drug access to the receptor biophase, we used purified receptor membranes from rat lung and disaggregated calf tracheal myocytes as model systems. Binding experiments were designed to measure the slow dissociation of agonists by means of delayed association of (-)-[125I]iodopindolol. Rat lung membranes were pretreated with high concentrations of agonists (salmeterol, formoterol, isoprenaline) before dissociation was induced by 50-fold dilution. Half-times of association of (-)-[125I]iodopindolol remained unchanged compared with untreated controls, indicating that dissociation of agonists occurred in less than 2 min. Adenylyl cyclase experiments were designed to determine the on and off kinetics of agonists to beta2 adrenoceptors by measuring the rate of receptor-induced cyclic AMP (cAMP) formation. Experiments were performed in tracheal membranes characterized by high Vmax values of cAMP formation. Adenylyl cyclase activation occurred simultaneously with the addition of the agonist, continued linearly with time for 60 min, and ceased immediately after the antagonist was added. Similarly, when receptor membranes were preincubated in a small volume with high salmeterol concentrations, there was a linear increase in cAMP formation, which was immediately interrupted by a 100-fold dilution of the reaction mixture. This militates against the exo-site hypothesis. On the other hand, dissociation by dilution was much less when membranes were preincubated with a large volume of salmeterol at the same concentration, indicating that physicochemical effects, and not exo-site binding, underlie its prolonged mode of action.  (+info)

Differential addressing of 5-HT1A and 5-HT1B receptors in epithelial cells and neurons. (3/3334)

The 5-HT1A and 5-HT1B serotonin receptors are expressed in a variety of neurons in the central nervous system. While the 5-HT1A receptor is found on somas and dendrites, the 5-HT1B receptor has been suggested to be localized predominantly on axon terminals. To study the intracellular addressing of these receptors, we have used in vitro systems including Madin-Darby canine kidney (MDCK II) epithelial cells and primary neuronal cultures. Furthermore, we have extended these studies to examine addressing in vivo in transgenic mice. In epithelial cells, 5-HT1A receptors are found on both apical and basolateral membranes while 5-HT1B receptors are found exclusively in intracellular vesicles. In hippocampal neuronal cultures, 5-HT1A receptors are expressed on somatodendritic membranes but are absent from axons. In contrast, 5-HT1B receptors are found on both dendritic and axonal membranes, including growth cones where they accumulate. Using 5-HT1A and 5-HT1B knockout mice and the binary tTA/tetO system, we generated mice expressing these receptors in striatal neurons. These in vivo experiments demonstrate that, in striatal medium spiny neurons, the 5-HT1A receptor is restricted to the somatodendritic level, while 5-HT1B receptors are shipped exclusively toward axon terminals. Therefore, in all systems we have examined, there is a differential sorting of the 5-HT1A and 5-HT1B receptors. Furthermore, we conclude that our in vivo transgenic system is the only model that reconstitutes proper sorting of these receptors.  (+info)

Interactions of high affinity insulin-like growth factor-binding proteins with the type V transforming growth factor-beta receptor in mink lung epithelial cells. (4/3334)

High affinity insulin-like growth factor-binding proteins (IGFBP-1 to -6) are a family of structurally homologous proteins that induce cellular responses by insulin-like growth factor (IGF)-dependent and -independent mechanisms. The IGFBP-3 receptor, which mediates the IGF-independent growth inhibitory response, has recently been identified as the type V transforming growth factor-beta receptor (TbetaR-V) (Leal, S. M., Liu, Q. L., Huang, S. S., and Huang, J. S. (1997) J. Biol. Chem. 272, 20572-20576). To characterize the interactions of high affinity IGFBPs with TbetaR-V, mink lung epithelial cells (Mv1Lu cells) were incubated with 125I-labeled recombinant human IGFBPs (125I-IGFBP-1 to -6) in the presence of the cross-linking agent disuccinimidyl suberate and analyzed by 5% SDS-polyacrylamide gel electrophoresis and autoradiography. 125I-IGFBP-3, -4, and -5 but not 125I-IGFBP-1, -2, and -6 bound to TbetaR-V as demonstrated by the detection of the approximately 400-kDa 125I-IGFBP.TbetaR-V cross-linked complex in the cell lysates and immunoprecipitates. The analyses of 125I-labeled ligand binding competition and DNA synthesis inhibition revealed that IGFBP-3 was a more potent ligand for TbetaR-V than IGFBP-4 or -5. Most of the high affinity 125I-IGFBPs formed dimers at the cell surface. The cell-surface dimer of 125I-IGFBP-3 preferentially bound to and was cross-linked to TbetaR-V in the presence of disuccinimidyl suberate. IGFBP-3 did not stimulate the cellular phosphorylation of Smad2 and Smad3, key transducers of the transforming growth factor-beta type I/type II receptor (TbetaR-I.TbetaR-II) heterocomplex-mediated signaling. These results suggest that IGFBP-3, -4, and -5 are specific ligands for TbetaR-V, which mediates the growth inhibitory response through a signaling pathway(s) distinct from that mediated by the TbetaR-I and TbetaR-II heterocomplex.  (+info)

Proliferative effects of cholecystokinin in GH3 pituitary cells mediated by CCK2 receptors and potentiated by insulin. (5/3334)

1. Proliferative effects of CCK peptides have been examined in rat anterior pituitary GH3 cells, which express CCK2 receptors. 2. CCK-8s, gastrin(1-17) and its glycine-extended precursor G(1-17)-Gly, previously reported to cause proliferation via putative novel sites on AR4-2J and Swiss 3T3 cells, elicited significant dose dependent increases of similar magnitude in [3H]thymidine incorporation over 3 days in serum-free medium of 39 +/- 10% (P < 0.01, n = 20), 37 +/- 8% (P < 0.01, n = 27) and 41 +/- 6% (P < 0.01, n = 36) respectively. 3. CCK-8s and gastrin potentially stimulated mitogenesis (EC50 values 0.12 nM and 3.0 nM respectively), whilst G-Gly displayed similar efficacy but markedly lower potency. L-365,260 consistently blocked each peptide. The CCK2 receptor affinity of G-Gly in GH3 cells was 1.09 microM (1.01;1.17, n = 6) and 5.53 microM (3.71;5.99, n = 4) in guinea-pig cortex. 4. 1 microM G-Gly weakly stimulated Ca2+ increase, eliciting a 104 +/- 21% increase over basal Ca2+ levels, and was blocked by 1 microM L-365,260 whilst CCK-8s (100 nM) produced a much larger Ca2+ response (331 +/- 14%). 5. Insulin dose dependently enhanced proliferative effects of CCK-8s with a maximal leftwards shift of the CCK-8s curve at 100 ng ml(-1) (17 nM) (EC50 decreased 500 fold, from 0.1 nM to 0.2 pM; P < 0.0001). 10 microg ml(-1) insulin was supramaximal reducing the EC50 to 5 pM (P = 0.027) whilst 1 ng ml(-1) insulin was ineffective. Insulin weakly displaced [125I]BHCCK binding to GH3 CCK2 receptors (IC50 3.6 microM). 6. Results are consistent with mediation of G-Gly effects via CCK2 receptors in GH3 cells and reinforce the role of CCK2 receptors in control of cell growth. Effects of insulin in enhancing CCK proliferative potency may suggest that CCK2 and insulin receptors converge on common intracellular targets and indicates that mitogenic stimuli are influenced by the combination of extracellular factors present.  (+info)

[3H]-Mesulergine labels 5-HT7 sites in rat brain and guinea-pig ileum but not rat jejunum. (6/3334)

1. The primary aim of this investigation was to determine whether binding sites corresponding to the 5-HT7 receptor could be detected in smooth muscle of the rat jejunum. Binding studies in rat brain (whole brain minus cerebellum) and guinea-pig ileal longitudinal muscle were also undertaken in order to compare the binding characteristics of these tissues. Studies were performed using [3H]-mesulergine, as it has a high affinity for 5-HT7 receptors. 2. In the rat brain and guinea-pig ileum, pKD values for [3H]-mesulergine of 8.0 +/- 0.04 and 7.9 +/- 0.11 (n = 3) and Bmax values of 9.9 +/- 0.3 and 21.5 +/- 4.9 fmol mg(-1) protein were obtained respectively, but no binding was detected in the rat jejunum. [3H]-mesulergine binding in the rat brain and guinea-pig ileum was displaced with the agonists 5-carboxamidotryptamine (5-CT) > 5-hydroxytryptamine (5-HT) > or = 5-methoxytryptamine (5-MeOT) > sumatriptan and the antagonists risperidone > or = LSD > or = metergoline > ritanserin > > pindolol. 3. Despite the lack of [3H]-mesulergine binding in the rat jejunum, functional studies undertaken revealed a biphasic contractile response to 5-HT which was partly blocked by ondansetron (1 microM). The residual response was present in over 50% of tissues studied and was found to be inhibited by risperidone > LSD > metergoline > mesulergine = ritanserin > pindolol, but was unaffected by RS 102221 (3 microM), cinanserin (30 nM), yohimbine (0.1 microM) and GR 113808 (1 microM). In addition, the agonist order of potency was 5-CT > 5-HT > 5-MeOT > sumatriptan. 4. In conclusion, binding studies performed with [3H]-mesulergine were able to detect 5-HT7 sites in rat brain and guinea-pig ileum, but not in rat jejunum, where a functional 5-HT7-like receptor was present.  (+info)

Selective effects of a 4-oxystilbene derivative on wild and mutant neuronal chick alpha7 nicotinic receptor. (7/3334)

1. We assessed the pharmacological activity of triethyl-(beta-4-stilbenoxy-ethyl) ammonium (MG624), a drug that is active on neuronal nicotinic receptors (nicotinic AChR). Experiments on the major nicotinic AChR subtypes present in chick brain, showed that it inhibits the binding of [125I]-alphaBungarotoxin (alphaBgtx) to the alpha7 subtype, and that of [3H]-epibatidine (Epi) to the alpha4beta2 subtype, with Ki values of respectively 106 nM and 84 microM. 2. MG624 also inhibited ACh elicited currents (I(ACh)) in the oocyte-expressed alpha7 and alpha4beta2 chick subtypes with half-inhibitory concentrations (IC50) of respectively 109 nM and 3.2 microM. 3. When tested on muscle-type AChR, it inhibited [125I]-alphaBgtx binding with a Ki of 32 microM and ACh elicited currents (I(ACh)) in the oocyte-expressed alpha1beta1gammadelta chick subtype with an IC50 of 2.9 microM. 4. The interaction of MG624 with the alpha7 subtype was investigated using an alpha7 homomeric mutant receptor with a threonine-for-leucine 247 substitution (L247T alpha7). MG624 did not induce any current in oocytes expressing the wild type alpha7 receptor, but did induce large currents in the oocyte-expressed L247T alpha7 receptor. The MG624 elicited current (I(MG62)) has an EC50 of 0.2 nM and a Hill coefficient nH of 1.9, and is blocked by the nicotinic receptor antagonist methyllycaconitine (MLA). 5. These binding and electrophysiological studies show that MG624 is a potent antagonist of neuronal chick alpha7 nicotinic AChR, and becomes a competitive agonist following the mutation of the highly conserved leucine residue 247 located in the M2 channel domain.  (+info)

Identification of a region of the C-terminal domain involved in short-term desensitization of the prostaglandin EP4 receptor. (8/3334)

1. The prostaglandin EP4 receptor, which couples to stimulation of adenylyl cyclase, undergoes rapid agonist-induced desensitization when expressed in CHO-K1 cells. 2. Truncation of the 488-amino acid receptor at residue 350 removes the carboxy-terminal domain and abolishes desensitization. 3. To further delineate residues involved in desensitization, the receptor was truncated at position 408, 383 or 369. Receptors truncated at position 408 or 383 underwent PGE2-induced desensitization, whereas the receptor truncated at position 369 displayed sustained activity, indicating that the essential residues for desensitization lie between 370 and 383. 4. The six serines in the 14-amino acid segment between residues 370 and 383 were mutated to alanine, retaining the entire C-terminal domain. Desensitization was absent in cells expressing this mutant. 5. The results indicate involvement of serines located between 370 and 382 in rapid desensitization of the EP4 receptor.  (+info)

A radioligand assay is a type of in vitro binding assay used in molecular biology and pharmacology to measure the affinity and quantity of a ligand (such as a drug or hormone) to its specific receptor. In this technique, a small amount of a radioactively labeled ligand, also known as a radioligand, is introduced to a sample containing the receptor of interest. The radioligand binds competitively with other unlabeled ligands present in the sample for the same binding site on the receptor. After allowing sufficient time for binding, the reaction is stopped, and the amount of bound radioligand is measured using a technique such as scintillation counting. The data obtained from this assay can be used to determine the dissociation constant (Kd) and maximum binding capacity (Bmax) of the receptor-ligand interaction, which are important parameters in understanding the pharmacological properties of drugs and other ligands.

A ligand, in the context of biochemistry and medicine, is a molecule that binds to a specific site on a protein or a larger biomolecule, such as an enzyme or a receptor. This binding interaction can modify the function or activity of the target protein, either activating it or inhibiting it. Ligands can be small molecules, like hormones or neurotransmitters, or larger structures, like antibodies. The study of ligand-protein interactions is crucial for understanding cellular processes and developing drugs, as many therapeutic compounds function by binding to specific targets within the body.

An encyclopedia is a comprehensive reference work containing articles on various topics, usually arranged in alphabetical order. In the context of medicine, a medical encyclopedia is a collection of articles that provide information about a wide range of medical topics, including diseases and conditions, treatments, tests, procedures, and anatomy and physiology. Medical encyclopedias may be published in print or electronic formats and are often used as a starting point for researching medical topics. They can provide reliable and accurate information on medical subjects, making them useful resources for healthcare professionals, students, and patients alike. Some well-known examples of medical encyclopedias include the Merck Manual and the Stedman's Medical Dictionary.

Protein binding, in the context of medical and biological sciences, refers to the interaction between a protein and another molecule (known as the ligand) that results in a stable complex. This process is often reversible and can be influenced by various factors such as pH, temperature, and concentration of the involved molecules.

In clinical chemistry, protein binding is particularly important when it comes to drugs, as many of them bind to proteins (especially albumin) in the bloodstream. The degree of protein binding can affect a drug's distribution, metabolism, and excretion, which in turn influence its therapeutic effectiveness and potential side effects.

Protein-bound drugs may be less available for interaction with their target tissues, as only the unbound or "free" fraction of the drug is active. Therefore, understanding protein binding can help optimize dosing regimens and minimize adverse reactions.

"Competitive binding" is a term used in pharmacology and biochemistry to describe the behavior of two or more molecules (ligands) competing for the same binding site on a target protein or receptor. In this context, "binding" refers to the physical interaction between a ligand and its target.

When a ligand binds to a receptor, it can alter the receptor's function, either activating or inhibiting it. If multiple ligands compete for the same binding site, they will compete to bind to the receptor. The ability of each ligand to bind to the receptor is influenced by its affinity for the receptor, which is a measure of how strongly and specifically the ligand binds to the receptor.

In competitive binding, if one ligand is present in high concentrations, it can prevent other ligands with lower affinity from binding to the receptor. This is because the higher-affinity ligand will have a greater probability of occupying the binding site and blocking access to the other ligands. The competition between ligands can be described mathematically using equations such as the Langmuir isotherm, which describes the relationship between the concentration of ligand and the fraction of receptors that are occupied by the ligand.

Competitive binding is an important concept in drug development, as it can be used to predict how different drugs will interact with their targets and how they may affect each other's activity. By understanding the competitive binding properties of a drug, researchers can optimize its dosage and delivery to maximize its therapeutic effect while minimizing unwanted side effects.

In the context of medical and biological sciences, a "binding site" refers to a specific location on a protein, molecule, or cell where another molecule can attach or bind. This binding interaction can lead to various functional changes in the original protein or molecule. The other molecule that binds to the binding site is often referred to as a ligand, which can be a small molecule, ion, or even another protein.

The binding between a ligand and its target binding site can be specific and selective, meaning that only certain ligands can bind to particular binding sites with high affinity. This specificity plays a crucial role in various biological processes, such as signal transduction, enzyme catalysis, or drug action.

In the case of drug development, understanding the location and properties of binding sites on target proteins is essential for designing drugs that can selectively bind to these sites and modulate protein function. This knowledge can help create more effective and safer therapeutic options for various diseases.

Molecular sequence data refers to the specific arrangement of molecules, most commonly nucleotides in DNA or RNA, or amino acids in proteins, that make up a biological macromolecule. This data is generated through laboratory techniques such as sequencing, and provides information about the exact order of the constituent molecules. This data is crucial in various fields of biology, including genetics, evolution, and molecular biology, allowing for comparisons between different organisms, identification of genetic variations, and studies of gene function and regulation.

Kahl SD, Sittampalam GS, Weidner J (May 2012). "Calculations and Instrumentation used for Radioligand Binding Assays". Assay ... Ligands are radiolabeled using either 3H or 125I, and released into the assay. Since only the radioligands that directly bind ... A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to ... Filter assays are a solid phase ligand binding assay that use filters to measure the affinity between two molecules. In a ...
Schild regression is a radioligand binding assay. It is used for DNA labelling (5' and 3'), leaving the nucleic acids intact. A ...
"Folate receptor expression in carcinomas and normal tissues determined by a quantitative radioligand binding assay". Analytical ...
One of the methods researchers used to guide these alterations was radioligand binding thermostability assay. The assay is ... Biochemical assays require a catalytic activity of the protein in question as well as a specific assay. Circular dichroism and ... The thermofluor assay was the first high-throughput thermal shift assay and its utility and limitations has spurred the ... The radioligand concentration is high enough to saturate the protein. Denatured protein is unable to bind the radioligand and ...
"Folate receptor expression in carcinomas and normal tissues determined by a quantitative radioligand binding assay". Anal. ... These include an invasive tissue-based immunohistochemical assay, and a non-invasive radiodiagnostic approach. The latter ...
In this type of assay, a single concentration of radioligand (usually an agonist) is used in every assay tube. The ligand is ... November 2017). "Assay Operations for SAR Support". Assay Guidance Manual. Eli Lilly & Company and the National Center for ... IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the ... The level of specific binding of the radioligand is then determined in the presence of a range of concentrations of other ...
... displays similar binding affinity toward cells in radio ligand binding assays. Thus, post translational processing may play a ... Scatchard analysis of radio ligand binding data from 125I-OSM binding to a variety of OSM responsive cell lines produced ... As a result, several investigators used human OSM in mouse assays and thus any conclusion drawn from the results of these ... Pro-OSM, although an order of magnitude less efficacious in growth inhibition assays, ...
ISBN 978-3-03788-700-4. Harms A, Ulmer E, Kovar K. Synthesis and 5-HT2A radioligand receptor binding assays of DOMCl and DOMOM ...
... and radioligand and competition assays. BindingDB includes data extracted from the scientific literature by the BindingDB ...
... structure activity relationships of analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays ...
However, radioligand binding assays with human proteins have shown that, contrary to common belief, the drug also does not ...
Dual polarisation interferometry Multi-parametric surface plasmon resonance Ligand binding assay and radioligand binding assay ... Radioligands are radioisotope labeled compounds used in vivo as tracers in PET studies and for in vitro binding studies. The ... ISBN 978-0-12-370599-0. Cabanos, C; Wang, M; Han, X; Hansen, SB (8 August 2017). "A Soluble Fluorescent Binding Assay Reveals ... Wienken CJ, Baaske P, Rothbauer U, Braun D, Duhr S (October 2010). "Protein-binding assays in biological liquids using ...
... for instance in radioligand binding assays. Taken together, (-)-alazocine is a selective partial agonist of the κ-opioid ...
... the range of their bioactivities were measured by radioligand binding assay in order to conclude its potency as an opioid. ... Endomorphin-1 has high affinity and specificity for opioid receptors for behavioral, physiological and pharmacological assays, ...
In the Radioligand binding assay it has shown to have affinities of 0.11nM at the MOR, 0.24nM at the DOR and 0.03nM at the KOR ... and in the Hot- Plate Assay it is shown to be around 20x more potent than morphine. Azido Aryl Analogues of IBNtxA retain ...
... radioligand assay MeSH E01.370.374.750 - thyroid function tests MeSH E01.370.374.750.100 - basal metabolism MeSH E01.370. ... radioligand assay MeSH E01.370.384.730 - radionuclide imaging MeSH E01.370.384.730.050 - absorptiometry, photon MeSH E01.370. ... local lymph node assay MeSH E01.370.750.600 - passive cutaneous anaphylaxis MeSH E01.370.750.610 - patch tests MeSH E01.370. ... local lymph node assay MeSH E01.450.495.750.600 - passive cutaneous anaphylaxis MeSH E01.450.495.750.610 - patch tests MeSH ...
Radioligand displacement assays showed only weak (Ki = 794 nM) binding of collybolide to the human KOR, and functional assays ... Radioligand displacement and functional assays showed collybolide binding to (Ki = 0.9 nM) and activating the human KOR, and an ... and beta-arrestin recruitment assays). Shevick et al. note the presence of surface-modifying agents in the 2016 assay ... Independent chemical synthesis and biological assay of collybolide in 2022 found that it was devoid of opioid activity. ...
The opioid receptor affinity of fentanyl and its analogs was determined from their inhibitory potency in a binding assay with [ ... 3H] fentanyl as the radioligand. The Ki value for butyrfentanyl was Ki=32 ± 4.1 nM. Comparing to fentanyl's Ki (Ki=1.06 ± 0.15 ... Utilization of a radioreceptor assay for the analysis of fentanyl analogs in urine". J Anal Toxicol. 16 (1): 36-41. doi:10.1093 ... Alburges ME, Hanson GR, Gibb JW, Sakashita CO, Rollins DE (1992). "Fentanyl receptor assay. II. ...
With tritium (3H) radioactively labeled ketanserin is used as a radioligand for serotonin 5-HT2 receptors, e.g. in receptor ... binding assays and autoradiography. This radio-labeling has enabled the study of serotonin 5-HT2A receptor distribution in the ...
Testing for Illegal Drugs Radioligand binding assay When multiple assays measure the same target their results and utility may ... DNase footprinting assay Filter binding assay Gel shift assay Bicinchoninic acid assay (BCA assay) Bradford protein assay Lowry ... Chemotaxis assay Secretion assays Apoptosis assays such as the DNA laddering assay, the Nicoletti assay, caspase activity ... MTT assay Cell Counting Kit-8 (WST-8 based cell viability assay) SRB (Sulforhodamine B) assay CellTiter-Glo® Luminescent Cell ...
The 35S labelled radioligand of the compound, 35SGTPγS, is used in autoradiography and G-protein binding studies. Harrison C, ... Strange PG (November 2010). "Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and ... Traynor JR (December 12, 2003). "The [35S]GTPγS binding assay: approaches and applications in pharmacology". Life Sciences. 74 ...
His lab also first developed [125I]-(R)-DOI as a radioligand. Nichols is one of the few people who has published legitimate ... He has done extensive work using the rat model assay of drug discrimination in characterizing hallucinogenic drugs. Although ...
The affinity towards adenosine A3 subtype was measured against the radioligand PSB-11. Ozola V, Thorand M, Diekmann M, Qurishi ... GTPγS binding assay using hA3-CHO-cells indicated that PSB-10 acts as an inverse agonist (IC50 = 4 nM). It has been shown to ... a novel high-affinity antagonist radioligand for human A(3) adenosine receptors". Bioorg Med Chem Lett. 12 (3): 501-3. doi: ...
Binding assays determined that (-)-trans-H2-PAT possessed the strongest binding affinity at the histamine H1 receptor. Booth, ... RG; Moniri, NH; Bakker, RA; Choksi, NY; Nix, WB; Timmerman, H; Leurs, R (July 2002). "A novel phenylaminotetralin radioligand ...
Kolb's lab has developed a blood plasma assay for phospho-217-Tau (p217Tau), which shows potential as a highly accurate ... "Early Clinical PET Imaging Results with the Novel PHF-Tau Radioligand [F-18]-T807". Journal of Alzheimer's Disease. 34 (2): 457 ... sensitivity assay for measuring p217+tau in plasma". Alzheimer's & Dementia: Diagnosis, Assessment & Disease Monitoring. 13 (1 ...
2011) assayed desmethyltrimipramine, 2-hydroxytrimipramine, and trimipramine-N-oxide in addition to trimipramine and found that ... study were due to methodological differences, in particular the use of radioligand binding in isolated membranes (KD) to study ...
In functional antagonist assays, a dose-response curve measures the effect of the ability of a range of concentrations of ... of an antagonist can be determined experimentally using Schild regression or for competitive antagonists in radioligand binding ... Altering the amount of antagonist used in the assay can alter the dose ratio. In Schild regression, a plot is made of the log ( ... In functional assays of non-competitive antagonists, depression of the maximal response of agonist dose-response curves, and in ...
September 2008). "Two fast screening methods (GC-MS and TLC-ChEI assay) for rapid evaluation of potential anticholinesterasic ... "Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies". Brain Research. 571 (2): 242- ...
Waeber C, Schoeffter P, Palacios JM, Hoyer D (June 1988). "Molecular pharmacology of 5-HT1D recognition sites: radioligand ... March 1998). "Standard binding and functional assays related to medications development division testing for potential cocaine ... and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand ...
"Development of homogeneous high-affinity agonist binding assays for 5-HT2 receptor subtypes". ASSAY and Drug Development ... "Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors". Naunyn- ...
Kahl SD, Sittampalam GS, Weidner J (May 2012). "Calculations and Instrumentation used for Radioligand Binding Assays". Assay ... Ligands are radiolabeled using either 3H or 125I, and released into the assay. Since only the radioligands that directly bind ... A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to ... Filter assays are a solid phase ligand binding assay that use filters to measure the affinity between two molecules. In a ...
Affinity DataKi: 0.0200nMAssay Description:Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assayMore ... Affinity DataKi: 0.0316nMAssay Description:Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assayMore ... Affinity DataKi: 0.0398nMAssay Description:Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assayMore ... Affinity DataKi: 0.0398nMAssay Description:Binding affinity to alphaVbeta6 (unknown origin) by radioligand binding assayMore ...
Radioligand Assay, Thyrotropin/blood, Thyrotropin-Releasing Hormone/pharmacology, Thyroxine/blood, Triiodothyronine/blood. in ... Radioligand Assay; Thyrotropin/blood; Thyrotropin-Releasing Hormone/pharmacology; Thyroxine/blood; Triiodothyronine/blood}}, ...
THRX-195518 possesses activity at target muscarinic receptors that was slightly lower (approximately one-third to one-tenth) than revefenacin. ...
Radioassay, Protein-Binding use Radioligand Assay Radioassays, Protein-Binding use Radioligand Assay ... Radioimmunoprecipitation Analyses use Radioimmunoprecipitation Assay Radioimmunoprecipitation Analysis use ...
Radioassay, Protein-Binding use Radioligand Assay Radioassays, Protein-Binding use Radioligand Assay ... Radioimmunoprecipitation Analyses use Radioimmunoprecipitation Assay Radioimmunoprecipitation Analysis use ...
Radioassay, Protein-Binding use Radioligand Assay Radioassays, Protein-Binding use Radioligand Assay ... Radioimmunoprecipitation Analyses use Radioimmunoprecipitation Assay Radioimmunoprecipitation Analysis use ...
Radioassay, Protein-Binding use Radioligand Assay Radioassays, Protein-Binding use Radioligand Assay ... Radioimmunoprecipitation Analyses use Radioimmunoprecipitation Assay Radioimmunoprecipitation Analysis use ...
Radioassay, Protein-Binding use Radioligand Assay Radioassays, Protein-Binding use Radioligand Assay ... Radioimmunoprecipitation Analyses use Radioimmunoprecipitation Assay Radioimmunoprecipitation Analysis use ...
Detection of harmful algal toxins using the radioligand receptor binding assay. A manual of methods. Vienna: International ... Urine and serum samples of cases were collected for ciguatoxin (CTX) testing by radiological and receptor-binding assay. ... of cases were collected and submitted to the Philippines Nuclear Research Institute to detect CTX using receptor-binding assay ... Tabbada and Director Alumanda Dela Rosa of the Philippine Nuclear Research Institute for running the receptor-binding assay. ...
This functional activity was confirmed in radioligand binding assays (pKi = 7.50). This work demonstrates the power of ... In a whole-cell biosensing assay based on detection of dynamic mass redistribution (DMR) as readout for Gq inhibition, FR-6 ... Preliminary screening of QS activity using biosensor reporter assays indicated that C. haemolyticum strain KM2 produces both ...
Each assay was completed in triplicate and repeated three times for reproducibility.. GSH and GSSG assays were performed ... Equilibrium binding of radioligands ERa and ERb proteins in the presence of different concentrations of unlabelled competitors ... Each assay was completed in triplicate and repeated three times for reproducibility.. GSH and GSSG assays were performed ... other: OECD in vivo uterotrophic screening assay. Principles of method if other than guideline:. OECD uterotrophic assay is an ...
Buy 4-CDC online In radioligand binding assays, 4-CDC had very low affinities of 9,410 nM, 28,700 nM, and 19,600 nM for the ... Buy 4-CDC online, In radioligand binding assays, 4-CDC had very low affinities of 9,410 nM, 28,700 nM, and 19,600 nM for the ... In uptake potency assays, 4-CDChad low uptake potencies of 208 nM, 670 nM, and 75.5nM for the DAT, SERT, and NET, respectively ... In drug discrimination assays, 4-CMC i.p. fully substituted (ED50= 4.3mg/kg) for the discriminative stimulus effects of 10 mg/ ...
METHODS: Circulating anti-IFN-2 antibodies were measured by a radioligand binding assay. Whole-exome sequencing, RNA sequencing ... blood mononuclear cells were used to study any patients with levels of anti-IFN-2 autoantibodies exceeding the assays positive ...
Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) ... We also measured NO release from the kidneys using a chemiluminescence assay. AM (10(-10) to 10(-7) mol/L) relaxed the aorta ... To Order Contact us: [email protected] ... Description: A sandwich quantitative ELISA assay kit for detection of Rat ... A sandwich quantitative ELISA assay kit for detection of Human Adrenomedullin (ADM) in samples from serum, plasma .... ...
E5.478.594.410.639.830 Radioligand Assay E1.450.650 E1.370.225.985 E5.200.985 Rectal Prolapse C23.300.842.500.500 C23.300. ... E5.240.550 Plaque Assay E1.370.225.875.970.790 (Replaced for 2012 by Viral Plaque Assay) Plastic Embedding E1.370.225.500. ... E5.478.594.700 Radioimmunoprecipitation Assay E1.450.495.410.380.825 E1.370.225.812.735.840 E1.450.495.410.700.825 E5.200. ... E5.200.812.447 Immunoradiometric Assay E1.450.495.410.700.405 E5.478.566.639.405 E5.478.594.410.639.405 Immunosorbent ...
E5.478.594.410.639.830 Radioligand Assay E1.450.650 E1.370.225.985 E5.200.985 Rectal Prolapse C23.300.842.500.500 C23.300. ... E5.240.550 Plaque Assay E1.370.225.875.970.790 (Replaced for 2012 by Viral Plaque Assay) Plastic Embedding E1.370.225.500. ... E5.478.594.700 Radioimmunoprecipitation Assay E1.450.495.410.380.825 E1.370.225.812.735.840 E1.450.495.410.700.825 E5.200. ... E5.200.812.447 Immunoradiometric Assay E1.450.495.410.700.405 E5.478.566.639.405 E5.478.594.410.639.405 Immunosorbent ...
E5.478.594.410.639.830 Radioligand Assay E1.450.650 E1.370.225.985 E5.200.985 Rectal Prolapse C23.300.842.500.500 C23.300. ... E5.240.550 Plaque Assay E1.370.225.875.970.790 (Replaced for 2012 by Viral Plaque Assay) Plastic Embedding E1.370.225.500. ... E5.478.594.700 Radioimmunoprecipitation Assay E1.450.495.410.380.825 E1.370.225.812.735.840 E1.450.495.410.700.825 E5.200. ... E5.200.812.447 Immunoradiometric Assay E1.450.495.410.700.405 E5.478.566.639.405 E5.478.594.410.639.405 Immunosorbent ...
E5.478.594.410.639.830 Radioligand Assay E1.450.650 E1.370.225.985 E5.200.985 Rectal Prolapse C23.300.842.500.500 C23.300. ... E5.240.550 Plaque Assay E1.370.225.875.970.790 (Replaced for 2012 by Viral Plaque Assay) Plastic Embedding E1.370.225.500. ... E5.478.594.700 Radioimmunoprecipitation Assay E1.450.495.410.380.825 E1.370.225.812.735.840 E1.450.495.410.700.825 E5.200. ... E5.200.812.447 Immunoradiometric Assay E1.450.495.410.700.405 E5.478.566.639.405 E5.478.594.410.639.405 Immunosorbent ...
E5.478.594.410.639.830 Radioligand Assay E1.450.650 E1.370.225.985 E5.200.985 Rectal Prolapse C23.300.842.500.500 C23.300. ... E5.240.550 Plaque Assay E1.370.225.875.970.790 (Replaced for 2012 by Viral Plaque Assay) Plastic Embedding E1.370.225.500. ... E5.478.594.700 Radioimmunoprecipitation Assay E1.450.495.410.380.825 E1.370.225.812.735.840 E1.450.495.410.700.825 E5.200. ... E5.200.812.447 Immunoradiometric Assay E1.450.495.410.700.405 E5.478.566.639.405 E5.478.594.410.639.405 Immunosorbent ...
... and luciferase activity was assayed using the Promega Luciferase assay system and a Monolight 2010 system luminometer. ... In situ hybridization and radioligand binding studies have shown that 5HT3Rs are prominently expressed in a variety of ... Gel mobility shift assays were performed using the entire −219 bp fragment of the5HT3 R proximal promoter and nuclear extracts ... DNaseI protection assays. DNA-protein complexes were formed as described above using 1-7 μg of nuclear extract. Reactions were ...
There is a wide menu of available assay kits compatible with the MESO QuickPlex, and a full line of components and reagents for ... The unit for nuclear medicin at Skåne University Hospital provides radioligands for both experimental and clinical use. Besides ... developing your own assay. Several hundreds of immunoassays for a range of applications including immunology, inflammation, ... oncology, neurobiology, and toxicology, in various assay formats are available.. To learn more, visit the MESO QuickPlex ...
Antipolymer antibody assay: May provide conclusive evidence for a subgroup of people with fibromyalgia; about 50% of ... and the radioligand (11C)PBR28, which binds to the translocator protein (TSPO). Expression of TSPO is low in healthy CNS tissue ...
A Focus on Their Potential Mechanism of Action through Computational and Biochemical Assays (71 views). Biomolecules (ISSN: ... a new dopamine transporter PET radioligand (899 views). Synapse (ISSN: 0887-4476), 2009 Oct; 63(10): 871-880.. Impact Factor: ... Identification of Protease Inhibitors by a Fast Fluorimetric Assay (779 views). Mol Biotechnol (ISSN: 1073-6085, 1559- ...
  • A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to receptors, antibodies or other macromolecules. (wikipedia.org)
  • Specifically, despite the human body's endogenous receptors, hormones, and other neurotransmitters, pharmacologists utilize assays in order to create drugs that are selective, or mimic, the endogenously found cellular components. (wikipedia.org)
  • Radioligands are used to measure the ligand binding to receptors and should ideally have high affinity, low non-specific binding, high specific activity to detect low receptor densities, and receptor specificity. (wikipedia.org)
  • First, researchers evaluate the selectivity of TG4-155 for EP2 receptor against other prostanoid receptors in cell-based functional assays. (immune-system-research.com)
  • In particular, TG4-155 displays a high affinity to human EP2 receptors with a K i of 15 nM in the radioligand binding assay. (immune-system-research.com)
  • Cocaine self-administration, extinction training and drug-induced relapse change metabotropic glutamate mGlu5 receptors expression: Evidence from radioligand binding and immunohistochemistry assays. (krakow.pl)
  • On the other hand, the efficacy of our novel prodrugs was assessed using cutting-edge LC-MS/MS methods (i.e., diaPASEF, QTAP), fluorometric assay, ELISA, and behavioural studies. (uef.fi)
  • Historically, ligand binding assay techniques were used extensively to quantify hormone or hormone receptor concentrations in plasma or in tissue. (wikipedia.org)
  • Urine and serum samples of cases were collected for ciguatoxin (CTX) testing by radiological and receptor-binding assay. (who.int)
  • The maximal peak of receptor production was reached at 72-96 h post infection, and radioligand binding assays on insect cell membranes showed about 7 pmol of active receptor/ mg of membrane protein. (fu-berlin.de)
  • This functional activity was confirmed in radioligand binding assays (pKi = 7.50). (bvsalud.org)
  • The synthesised compounds were evaluated in radioligand binding studies and in functional assays performed in CHO cells stably transfected with human ARs. (unicam.it)
  • Functional studies were carried out using a new Eu-GTP assay which exploits the unique fluorescence properties of lanthanide chelates and provides a powerful alternative to assays that utilise radioisotopes. (unicam.it)
  • Ligand binding assays provide a measure of the interactions that occur between two molecules, such as protein-bindings, as well as the degree of affinity (weak, strong, or no connection) for which the reactants bind together. (wikipedia.org)
  • There are numerous types of ligand binding assays, both radioactive and non-radioactive. (wikipedia.org)
  • As such, ligand binding assays are a superset of radiobinding assays, which are the conceptual inverse of radioimmunoassays (RIA). (wikipedia.org)
  • Ligand binding assays are used primarily in pharmacology for various demands. (wikipedia.org)
  • The ligand-binding assay methodology quantified the concentration of the hormone in the test material by comparing the effects of the test sample to the results of varying amounts of known protein (ligand). (wikipedia.org)
  • The foundations for which ligand binding assay have been built are a result of Karl Landsteiner, in 1945, and his work on immunization of animals through the production of antibodies for certain proteins. (wikipedia.org)
  • The first successful ligand binding assay was reported in 1960 by Rosalyn Sussman Yalow and Solomon Berson. (wikipedia.org)
  • As a direct result of these monumental findings, researchers have continued the advancement of ligand binding assays in many facets in the fields of biology, chemistry, and the like. (wikipedia.org)
  • Essential aspects of binding assays include, but are not limited to, the concentration level of reactants or products (see radioactive section), maintaining the equilibrium constant of reactants throughout the assay, and the reliability and validity of linked reactions. (wikipedia.org)
  • Although binding assays are simple, they fail to provide information on whether or not the compound being tested affects the target's function. (wikipedia.org)
  • The amount of prodrug's cellular kinetics, non-specific protein binding, and bioconversion was conducted by using highly validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) methods or radioligand binding assays. (uef.fi)
  • Key words: 125I-iodoamphetamine, 123I-iodoamphetamine, binding assay, liver, hepatocyte INTRODUCTION 123I-IODOAMPHETAMINE (IMP) is a clinically useful radioactive tracer in assessing brain1,2 or lung perfusion,3-5 because intravenously administered IMP is taken up by these tissues and retained. (jsnm.org)
  • In addition, radioligand binding assays for ER and EGFR were carried out and tumour histological grade was determined. (ox.ac.uk)
  • GSH and GSSG assays were performed according to the methods of Pandey and Katiyar. (europa.eu)
  • In a whole-cell biosensing assay based on detection of dynamic mass redistribution (DMR) as readout for Gq inhibition, FR-6 suppressed Gq signaling with micromolar potency (pIC50 = 5.56). (bvsalud.org)
  • Protein concentrations were determined using protein assay reagents. (europa.eu)
  • Cell culture system - B16 cells from Korean Cell Line bank were cultured in DMEM with 10% FBS and penicillin/streptomycin, in 24 well plates for each assay. (europa.eu)
  • 25% of the meta-phosphoric acid added cell pellets were centrifuged and the supernatant assayed. (europa.eu)
  • There are two common strategies that are adopted for this type of experiment: Increasing the amount of radioligand added while maintaining both the constant specific activity and constant concentration of radioligand, or decreasing the specific activity of the radioligand due to the addition of an unlabeled ligand. (wikipedia.org)
  • For establishing SAR on ligands to be synthesized, it was necessary to establish an in vitro binding assay. (nih.gov)
  • The compounds were synthesized using specially developed synthetic routes, and their biological activity was assessed in the following assays: Ellman's (cholinesterase inhibition), FRET-based (inhibition of betasecretase), thioflavin T / S in vitro and in cellulo (Aβ and tau aggregation), FRAP and ABTS (antioxidant properties) and radio ligand binding assay. (krakow.pl)
  • To identify such transformations, we carried out a comprehensive analysis of all approximately 33,000 compound pairs in the Novartis internal database which have IC 50 values in the dofetilide displacement assay. (biomedcentral.com)
  • Conclusions 177 Lu-BiOncoFAP is a promising candidate for radioligand therapy of cancer, with favorable in vivo tumour-to-organ ratio, long tumour residence time and potent anti-cancer efficacy. (biorxiv.org)
  • Determination of DPM is important for making conversions to calculate molar concentrations of radioligands, and it is also important if a comparison between different instruments is required. (nih.gov)
  • All newly synthesized compounds were evaluated in radioligand competition binding assays, as well as in 5 different functional BRET (bioluminescence energy transfer) assays. (nih.gov)
  • Initially, we followed a literature protocol 79 using synthetic Aβ aggregates as protein source and [ 125 I]TZDM as reference radioligand. (nih.gov)
  • The raw wash is then run through a size exclusion column to separate the ECVs, and the different size samples are either run through a BCA Protein Assay to determine amount of protein in each sample based on an absorbance reading, or run through an SDS-PAGE Protein Gel and treated with antibodies to isolate the aβ protein. (uw.edu)
  • The purpose of this chapter is to 1) describe common calculations used in radioligand binding assays and 2) outline steps for setting up and using microplate scintillation counters (Microbeta Trilux and TopCount). (nih.gov)
  • Microplate scintillation counters, used for reading Scintillation Proximity Assay (SPA) and filtration assays, detect flashes of light (photons) that occur when a released radioactive particle interacts with and excites a fluor molecule. (nih.gov)
  • The GADA assay was based on 125 I-labeled human recombinant GAD65. (medscape.com)
  • The IA-2A assay was based on 35 S-methionine-labeled human recombinant in vitro transcribed-translated intracellular domain of IA-2. (medscape.com)
  • Methods The binding properties of BiOncoFAP and its monovalent OncoFAP analogue were assayed against recombinant hFAP. (biorxiv.org)
  • Activities supported under this FOA include, but are not limited to the in vitro screening of existing ligands against human ADRD brain tissue, medicinal chemistry support for development of new compounds and improvement of existing ligand specificity and selectivity, initial screening of ligands in appropriate animal models, and radioligand formulation and first-in-human testing. (nih.gov)
  • When examined using a reporter gene assay, bisphenol AF was a full agonist for ERα. (nih.gov)
  • Radioligand binding assays are a "work horse" in biological laboratories and have been adapted for HTS and lead optimization support in drug discovery. (nih.gov)
  • The determination will be made on a weight-of-evidence basis taking into account data from the Tier 1 assays and other scientifically relevant information available. (nih.gov)
  • We show that these characteristics of-3H-PCP binding to both GF/B filters and denatured tissue are not shared by other radioligands, such as 3H-D lysergic acid diethylamide (3H-D-LSD) and dH-t+)3-qinuclidinyl benzylate (3H-QNB). (erowid.org)
  • 80 For this radioligand, the concentration of binding sites to Aβ 42 monomer was again low. (nih.gov)
  • We modified an ELISA assay to measure Aβ 42 and Aβ 40 , which in turn allowed us to measure the number of binding sites per Aβ 42 monomer. (nih.gov)
  • This funding opportunity announcement (FOA) supports the development of PET radioligands that identify proteinopathies or pathological processes associated with the human biology of Alzheimer's disease related dementias (ADRDs). (nih.gov)
  • We changed the reference radioligand to [ 3 H]PIB. (nih.gov)
  • The purity of I-LSD was greater than 95% as assayed by high performance liquid chromatography. (erowid.org)
  • Both the sensitivity and specificity of this GADA assay were 100% when compared with a 35 S-GADA assay evaluated in the Diabetes Autoantibody Proficiency Testing Program for GADA (no. 2, 24 samples tested). (medscape.com)
  • In the latest Diabetes Autoantibody Proficiency Testing Program for IA-2A (no. 3, 24 samples tested), this IA-2A assay performed with 100% sensitivity and 100% specificity. (medscape.com)