Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Lists of words, usually in alphabetical order, giving information about form, pronunciation, etymology, grammar, and meaning.
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)
A serotonin uptake inhibitor that is effective in the treatment of depression.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of serotonergic neurons. They are different than SEROTONIN RECEPTORS, which signal cellular responses to SEROTONIN. They remove SEROTONIN from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. Regulates signal amplitude and duration at serotonergic synapses and is the site of action of the SEROTONIN UPTAKE INHIBITORS.
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.
Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.
A structurally and mechanistically diverse group of drugs that are not tricyclics or monoamine oxidase inhibitors. The most clinically important appear to act selectively on serotonergic systems, especially by inhibiting serotonin reuptake.
The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.
Databases devoted to knowledge about specific chemicals.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.
A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.
The output neurons of the cerebellar cortex.
An enzyme found predominantly in platelet microsomes. It catalyzes the conversion of PGG(2) and PGH(2) (prostaglandin endoperoxides) to thromboxane A2. EC 5.3.99.5.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).
Physiologically active compounds found in many organs of the body. They are formed in vivo from the prostaglandin endoperoxides and cause platelet aggregation, contraction of arteries, and other biological effects. Thromboxanes are important mediators of the actions of polyunsaturated fatty acids transformed by cyclooxygenase.
A subclass of eicosanoid receptors that have specificity for THROMBOXANE A2 and PROSTAGLANDIN H2.
CXCR receptors with specificity for CXCL12 CHEMOKINE. The receptors may play a role in HEMATOPOIESIS regulation and can also function as coreceptors for the HUMAN IMMUNODEFICIENCY VIRUS.
Cell surface glycoproteins that bind to chemokines and thus mediate the migration of pro-inflammatory molecules. The receptors are members of the seven-transmembrane G protein-coupled receptor family. Like the CHEMOKINES themselves, the receptors can be divided into at least three structural branches: CR, CCR, and CXCR, according to variations in a shared cysteine motif.
CXCR receptors that are expressed on the surface of a number of cell types, including T-LYMPHOCYTES; NK CELLS; DENDRITIC CELLS; and a subset of B-LYMPHOCYTES. The receptors are activated by CHEMOKINE CXCL9; CHEMOKINE CXCL10; and CHEMOKINE CXCL11.
A CXC chemokine that is induced by GAMMA-INTERFERON. It is a chemotactic factor for activated T-LYMPHOCYTES and has specificity for the CXCR3 RECEPTOR.
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.
Adherence of cells to surfaces or to other cells.
CCR receptors with specificity for CHEMOKINE CCL27. They may play a specialized role in the cutaneous homing of LYMPHOCYTES.
A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.
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)
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
A family of heterotrimeric GTP-binding protein alpha subunits that were originally identified by their ability to inhibit ADENYLYL CYCLASES. Members of this family can couple to beta and gamma G-protein subunits that activate POTASSIUM CHANNELS. The Gi-Go part of the name is also spelled Gi/Go.
Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.

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)

Definition of Radioligand assay in the Legal Dictionary - by Free online English dictionary and encyclopedia. What is Radioligand assay? Meaning of Radioligand assay as a legal term. What does Radioligand assay mean in law?
BioAssay record AID 721184 submitted by ChEMBL: Displacement of [3F]FMZ from Wistar rat cerebellum GABAA receptor by competitive radioligand assay.
Hanson J, Rolin S, Reynaud D, Qiao N, Kelley LP, Reid HM, Valentin F, Tippins J, Kinsella BT, Masereel B, Pace-Asciak C, Pirotte B, Dogné JM. In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N-[2-(4-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist. J Pharmacol Exp Ther. 2005 Apr; 313(1):293-301 ...
Significant inhibition of proliferative activity in PC3 human prostate cancer cells by estradiol is reported, accompanied by experimental evidence for a specific estrogen receptor (ER). Radioligand-binding assays revealed the presence of high affinity sites of estrogen binding in the nuclear compartment of PC3 cells. In addition, using a reverse transcriptase-polymerase chain reaction system, we obtained evidence of either normal or a variant ER mRNA; the latter, which lacks the entire exon 4, is coexpressed with normal ER mRNA and has been recently characterized in our laboratories. The likelihood that the inhibitory effect exerted by estradiol could be mediated by an increase of transforming growth factor β (TGFβ) production was also investigated. Use of monoclonal antibodies against TGFβ1 produced a 3-fold increase of growth rate in PC3 cells; this clearly speaks for high levels of endogenous TGFβ1. This effect was almost completely abolished after addition of 100 nm estradiol. However, ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
testing that includes saturation radioligand binding assay to determine receptor concentration (Bmax) and affinity (Kd). Competition binding assays are performed determine affinity (Ki) against known reference agonists and antagonists. GTPγS data is also provided for some of our Gi-coupled receptors.. Membranes are carefully prepared and ready for a variety of HTS applications, including radioligand binding (using either proximitymethods, such as FlashPlate, or classical filtration methods).. Products are packaged as frozen crude membrane preparations. One assay unit is defined as micrograms of protein, defined by competition binding assay (filtration). A complete product description and recommended protocol are included on the Product Information Sheet.. Some of our receptors may be restricted for sale in specified countries. Please inquire.. ...
testing that includes saturation radioligand binding assay to determine receptor concentration (Bmax) and affinity (Kd). Competition binding assays are performed determine affinity (Ki) against known reference agonists and antagonists. GTPγS data is also provided for some of our Gi-coupled receptors.. Membranes are carefully prepared and ready for a variety of HTS applications, including radioligand binding (using either proximitymethods, such as FlashPlate, or classical filtration methods).. Products are packaged as frozen crude membrane preparations. One assay unit is defined as micrograms of protein, defined by competition binding assay (filtration). A complete product description and recommended protocol are included on the Product Information Sheet.. Some of our receptors may be restricted for sale in specified countries. Please inquire.. ...
We submit every batch of receptor to stringent quality control testing that includes saturation radioligand binding assay to determine receptor concentration (Bmax) and affinity (Kd). Competition binding assays are performed determine affinity (Ki) against known reference agonists and antagonists. GTPgS data is also provided for some of our Gi coupled receptors ...
You have selected a print-on-demand product. This publication is printed digitally to order in black and white - colour diagrams are reproduced in black and white. The binding methods will vary from publication to publication.. This publication is usually dispatched within 1-3 working days. Special delivery options are currently unavailable for print-on-demand products which means this publication will dispatched by standard Royal Mail surface mail (for UK customers) or DHL Global Economy (for International customers).. ...
You have selected a print-on-demand product. This publication is printed digitally to order in black and white - colour diagrams are reproduced in black and white. The binding methods will vary from publication to publication.. This publication is usually dispatched within 1-3 working days. Special delivery options are currently unavailable for print-on-demand products which means this publication will dispatched by standard Royal Mail surface mail (for UK customers) or DHL Global Economy (for International customers).. ...
Follitropin (FSH) heterodimers possess two potential N-glycosylation sites on both common α and hormone-specific β subunits. Hypo-glycosylated hFSH isolated from lutropin preparations possessed a partially glycosylated FSHβ subunit decorated with one glycan, while there were two in the hFSHα subunit. Mass spectrometry revealed the presence of oligomannose glycans, which are normally rare in hFSH preparations. Hypo-glycosylated hFSH was 5- to 26-fold more active than fully-glycosylated hFSH in several FSH radioligand assays. In rat testis homogenate, 125I-hypo-hFSH bound receptors immediately, without the 45-60 min lag observed for 125I-fully-glycosylated hFSH. In porcine granulosa cells, short-term incubations revealed an earlier onset of cAMP accumulation, protein kinase A (PKA) activity and CREB phosphorylation. Hypo-glycosylated hFSH increased intracellular cAMP accumulation within one min and PKA-dependent CREB phosphorylation within 5 min; whereas fully-glycosylated hFSH induced CREB ...
Ligand binding assays (LBA) is an assay, or an analytic procedure, whose procedure or method relies on the binding of ligand molecules to receptors, antibodies or other macromolecules. A detection method is used to determine the presence and extent of the ligand-receptor complexes formed, and this is usually determined electrochemically or through a fluorescence detection method. This type of analytic test can be used to test for the presence of target molecules in a sample that are known to bind to the receptor. There are numerous types of ligand binding assays, both radioactive and non-radioactive. As such, ligand binding assays are a superset of radiobinding assays, which are the conceptual inverse of radioimmunoassays (RIA). Some newer types are called mix-and-measure assays because they do not require separation of bound ligands. Ligand binding assays are used primarily in pharmacology for various demands. Specifically, despite the human bodys endogenous receptors, hormones, and other ...
BioAssay record AID 205020 submitted by ChEMBL: Evaluated for affinity at 5-HT uptake site using [3H]paroxetine as radioligand in radioligand binding assay.
Brodde, O.E.; Eymer, T.; Arroyo, J., 1983: 3H-yohimbine binding to guinea-pig kidney and calf cerebral cortex membranes: comparison with human platelets
TY - JOUR. T1 - [63] A Sensitive Radioreceptor Assay for 1α,25-Dihydroxyvitamin D in Biological Fluid. AU - Chandler, John S.. AU - Wesley Pike, J.. AU - Hagan, Laura A.. AU - Haussler, Mark R.. PY - 1980/1/1. Y1 - 1980/1/1. N2 - This chapter discusses a sensitive radioreceptor assay for lα,25-dihydroxyvitamin D in biological fluids. Vitamin D has been recognized as a principal regulator of calcium and phosphate homeostasis in a variety of animal species, including humans. Some studies describe 1α,25-dihydroxyvitamin D [lα,25-(OH)2D] as the hormonal metabolite responsible for mediating intestinal transport of these minerals and hence necessitate development of a precise method for quantitating this sterol in biological fluids, particularly serum. It has been demonstrated that chick intestinal mucosa contained a cytosolic protein that rapidly and specifically bound lα,25-(OH)2D3 both in vivo and in vitro with high affinity. Furthermore, the sterol-protein complex was rapidly translocated to ...
In radioligand binding experiments, MDL 73147EF and MDL 74156 inhibited the binding of [3H]GR65630 to 5-hydroxy-tryptamine3 (5-HT3) binding sites on membranes prepared from NG108-15 neuroblastoma x glioma cells. The calculated dissociation constants (KI) were 20.03 +/- 6.58 and 0.44 +/- 0.18 nM, res …
In the domestic fowl, angiotensin (ANG) II causes a unique vasodepressor response in vivo and vascular relaxation of aortic rings in vitro that appear to be mediated by ANG II receptors. In initial studies using radioligand binding techniques, we identified specific vascular ANG II receptors in the fowl aorta. In the present study, we have characterized fowl vascular ANG II receptors in terms of binding specificity and their modulation by divalent cations and guanine nucleotide, to understand how the fowl receptor might differ from mammalian vascular ANG II receptors that mediate vasoconstriction. Competitive displacement of [125I] ANG II binding by ANG agonist and antagonist analogs revealed a unique pattern of receptor specificity, with the potency rank order: [Asn1, Val5]ANG II greater than [Asp1, Ile5]ANG II greater than [Asp1, Val5, Ser9] ANG I = [Asp1, Val5]ANG II much greater than [Val5]ANG III greater than [sarcosine(Sar)1, Ile5]ANG II greater than [Sar1, Ile8]ANG II much greater than ...
TY - JOUR. T1 - Comparison between single saturating dose ligand binding assay and enzyme immunoassay for low-salt extractable oestrogen and progesterone receptors in breast cancer. T2 - A multicentre study. AU - Gion, Massimo. AU - Dittadi, Ruggero. AU - Leon, Antonette E.. AU - Bruscagnin, Giuliano. AU - Pelizzola, Dario. AU - Giovannini, Gloria. AU - Giganti, Melchiorre. AU - Messeri, Gianni. AU - Quercioli, Massimo. AU - Flamini, Emanuela. AU - Riccobon, Angela. AU - Bozzetti, Cecilia. AU - Benecchi, Magda. AU - De Lena, Mario. AU - Paradiso, Angelo. AU - Ruggeri, Giuseppina. AU - Luisi, Patrizia. AU - Piffanelli, Adriano. PY - 1991. Y1 - 1991. N2 - An excellent correlation between ligand binding assay (LBA) and enzyme immunoassay (EIA) for both oestrogen (ER) and progesterone (PR) receptors has been reported. Nevertheless, considering that the clinical value of any discrepancy between LBA and EIA probably varies with the receptor level, we undertook a collaborative study in which a single ...
Jacqmin, P. ; Lesne, Michel. Measurement of Benzodiazepines By Radioimmuno Assay and Radioreceptor Assay in Biological Samples.In: Annales de Biologie Clinique, Vol. 40, no. 4, p. 480-481 (1982 ...
Membrane Target Systems are quality assured frozen membranes from cells that express recombinant or endogenous receptors.. We submit every batch of receptor to stringent quality control testing that includes saturation radioligand binding assay to determine receptor concentration (Bmax) and affinity (Kd). Competition binding assays are performed determine affinity (Ki) against known reference agonists and antagonists. GTP?S data is also provided for some of our Gi-coupled receptors.. Membranes are carefully prepared and ready for a variety of HTS applications, including radioligand binding (using either proximitymethods, such as FlashPlate, or classical filtration methods).. Products are packaged as frozen crude membrane preparations. One assay unit is defined as micrograms of protein, defined by competition binding assay (filtration). A complete product description and recommended protocol are included on the Product Information Sheet.. Some of our receptors may be restricted for sale in ...
testing that includes saturation radioligand binding assay to determine receptor concentration (Bmax) and affinity (Kd). Competition binding assays are performed determine affinity (Ki) against known reference agonists and antagonists. GTPγS data is also provided for some of our Gi-coupled receptors.. Membranes are carefully prepared and ready for a variety of HTS applications, including radioligand binding (using either proximitymethods, such as FlashPlate, or classical filtration methods).. Products are packaged as frozen crude membrane preparations. One assay unit is defined as micrograms of protein, defined by competition binding assay (filtration). A complete product description and recommended protocol are included on the Product Information Sheet.. Some of our receptors may be restricted for sale in specified countries. Please inquire.. ...
RFC 5389 STUN October 2008 transactions, this transaction ID allows the client to associate the response with the request that generated it; for indications, the transaction ID serves as a debugging aid. All STUN messages start with a fixed header that includes a method, a class, and the transaction ID. The method indicates which of the various requests or indications this is; this specification defines just one method, Binding, but other methods are expected to be defined in other documents. The class indicates whether this is a request, a success response, an error response, or an indication. Following the fixed header comes zero or more attributes, which are Type-Length-Value extensions that convey additional information for the specific message. This document defines a single method called Binding. The Binding method can be used either in request/response transactions or in indication transactions. When used in request/response transactions, the Binding method can be used to determine the ...
We have characterized the binding of a novel radioligand, [3H] FK888, to neurokinin (NK)1 receptors in guinea pig lung membranes and localized its binding in guinea pig lung sections by autoradiography. Lung membranes were incubated with [3H] FK888 at 25 degrees and the assays were terminated by rapid filtration; nonspecific binding was defined as binding in the presence of 1 microM concentrations of the nonpeptide NK1-selective antagonist CP-96,345. Kinetic analysis showed that specific binding of [3H] FK888 (approximately 70% of total binding) was rapid, reaching a plateau by 20 min, and that binding was reversed by addition of 1 microM CP-96,345, giving a kinetic Kd of 0.46 nM. Binding of [3H] FK888 was saturable at approximately 1 nM, and equilibrium binding analysis gave a Kd of 0.32 +/- 0.03 nM and a Bmax of 46.9 +/- 7.1 fmol/mg of protein (four experiments). In competition studies, substance P, CP-96,345, and FK888 competed for [3H] FK888 binding, but NKA, NKB, and NK2-selective ...
We submit every batch of receptor to stringent quality control testing that includes saturation radioligand binding assay to determine receptor concentration (Bmax) and affinity (Kd). Competition binding assays are performed determine affinity (Ki) against known reference agonists and antagonists. GTPgS data is also provided for some of our Gi coupled receptors ...
The in vitro and in vivo binding characteristics of [I-125] iodomethyllycaconitine ([I-125]iodoMLA) were determined in the rat. [I-125]iodoMLA binding to rat cerebral cortex membranes was saturable and reversible and its specific binding represented approximately 70-80% of the total binding. [I-125]iodoMLA labeled a single site with K-d = 1.8 +/- 0.4 nM and B-max = 68 +/- 3 fmol/mg protein. Kinetic analysis revealed a t(1/2) for association and dissociation of 10.5 +/- 3.1 and 10.3 +/- 1.6 min, respectively.
On the basis of extensive radioligand data and more limited functional data, three pharmacological subtypes of alpha 2-adrenergic receptors have been identified. More recently, three human genes or cDNAs for alpha 2-adrenergic receptors have been identified by molecular cloning. The relationship, however, among the pharmacologically defined subtypes and those identified by molecular cloning has not been clear. In order to resolve this issue, we have compared the pharmacological characteristics of the receptors identified by molecular cloning and expressed in COS-7 cells with the characteristics of the pharmacologically defined receptors in their respective prototypic tissue or cell line. The affinities (Ki values) of 12 subtype-selective alpha 2-adrenergic antagonists were determined for the alpha 2 receptor in the six preparations, by radioligand binding. Correlation analyses of the pKi values indicate that the alpha 2A subtype, as defined in the HT29 cell line, the alpha 2B receptor of the ...
In the receptor binding assay, the relative affinity ratios of P-7548 [3-(beta-phenylethyl)-9 beta-methoxy-9 alpha-(m… Expand ...
Radioligand therapy is currently approved for a small number of cancers, but it may have wide applications and could become an important pillar of treatment for many types of cancers and other diseases. As an innovative mode of treatment using nuclear medicine, there are some barriers that need to be addressed in order to realise the potential of radioligand therapy. ...
The latest company information, including net asset values, performance, holding & sectors weighting, changes in voting rights, and directors and dealings.
Radioligands are an innovation driven by our increasing understanding of the molecular biology of cancer and the role of radiation in cancer care. This timeline explores the history and future of radioligand therapy (on the right) alongside other innovations in oncology (on the left). ...
Endolytics offers receptor-binding assays for a number of ligands, as well as custom radioligand receptor-binding assay services.
cis to on Coumadin for to States cases its online category [url=http://ultram.grouply.com/home]buy tramadol overnight delivery[/url] [url=http://ultram.grouply.com/browse]buy tramadol online uk[/url] ain Order your mechanism opioids happentramadol response candays soil I and be [url=http://ultram.grouply.com/page/67]discount tramadol[/url] [url=http://ultram.grouply.com/page/5]generic ultram 100mg[/url] [url=http://ultram.grouply.com/page/10]purchase tramadol online[/url] of alone sleeping analgesic crystallinewas tramadol be placebo alert [url=http://ultram.grouply.com/page/14]tramadol 50mg capsules[/url] [url=http://ultram.grouply.com/page/17]tramadol 50 mg tab[/url] U FFPMANZCA is if require due logo at serotonin tablets [url=http://ultram.grouply.com/page/20]tramadol apap[/url] [url=http://ultram.grouply.com/page/26]tramadol er[/url] canblood administration this pharmacist prescribed tramadol be time and tramadol not [url=http://ultram.grouply.com/page/30]tramadol hcl 100 mg[/url] ...
Background: Pre-pulse inhibition (PPI) is a process in which the motor response to a startling stimulus is inhibited by a less intense stimulus immediately preceding it. Diminished PPI represents one of the many sensory integration impairments observed in patients with schizophrenia and autism. Objectives: The objective of our project is to explore potential neuropharmacological mechanisms of clozapine-mediated PPI improvement. Methods: In the current study 36 female Sprague-Dawley rats were used to study mixed-modal PPI with an acoustic prepulse and a tactile (air-puff) startling stimulus. Animals were chronically administered via osmotic minipump the NMDA glutamate receptor antagonist, dizocilpine (0.15 mg/kg/day), the H1 histamine receptor antagonist, pyrilamine (50 mg/kg/day), the combination of the two drugs or the saline vehicle (N=9/group). Following the completion of these psychopharmacological studies, we performed postmortem radioligand assays on histological sections to determine ...
OBJECTIVE:. To clarify the predictive value of islet cell antibody (ICA) and GAD65 antibody (GADA) present at diagnosis with respect to the need for insulin treatment 6 years after diagnosis in young adults initially considered to have type 2 or unclassifiable diabetes.. RESEARCH DESIGN AND METHODS:. The patient material was representative of the entire Swedish population, consisting of patients who were 15-34 years old at diagnosis of diabetes in 1987-1988 but were not considered to have type 1 diabetes at onset. At follow-up, 6 years after the diagnosis, it was noted whether the patient was treated with insulin. The presence of ICA was determined by an immunofluorescence assay, and GADAs were measured by a radioligand assay.. RESULTS:. Six years after diagnosis, 70 of 97 patients were treated with insulin, and 27 of 97 patients were treated with oral drugs or diet alone. At diagnosis, ICAs and GADAs were present in 41 (59%) of 70 patients and 41 (60%) of 68 patients, respectively, of those now ...
Background. Prostate cancer remains one of the leading causes of mortality amongst men globally with a median incidence rate of 19.5/100 000, which increases with age to reach a peak incidence over the age of 65 years. Despite the lack of reliable cancer registries in Africa, it is believed that the numbers are similar. However, there is a well-documented body of evidence, which suggests that prostate cancer follows a far more aggressive course in African men when compared to European men. African men are 1.6 times more likely to develop prostate cancer when compared to their European counterparts and twice as likely to die from this disease. This disparity is more pronounced than in any other malignancy and has in the past been attributed to factors such as socioeconomic status, access to health care and screening, diet, cultural factors and genetic differences. Convincing recent evidence, however, points to biological, molecular and genetic differences as the major role players in the observed ...
View Notes - L0710ap from BIOS 20182 at UChicago. committed step in a pathway Allosteric regulation (mechanism) Binding of ATP to a non-substrate (allosteric) site on the enzyme causes a
Finnema SJ, Nabulsi NB, Mercier J, Lin SF, Chen MK, Matuskey D, Gallezot JD, Henry S, Hannestad J, Huang Y, Carson RE. Kinetic evaluation and test-retest reproducibility of [11C]UCB-J, a novel radioligand for positron emission tomography imaging of synaptic vesicle glycoprotein 2A in humans ...
Knight AR, Misra A, Quirk K, Benwell K, Revell D, Kennett G, Bickerdike M. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Archives of Pharmacology. 2004;370:114-123. DOI:10.1007/s00210-004-0951-4 PMID 15322733 ...
Example data for receptor function and radioligand binding at wild-type and mutant receptors. (A) Channel function was measured using a voltage-sensitive fluoro
Title compds. represented by the formula I [wherein Q = (hetero)arylalkyl; R1 = OH, halo, alkyl, etc.; R2, R3 = independently H, (halo)alkyl, aminocarbonylalkyl, etc.; n = 0-3; and pharmaceutically acceptable salts, solvates or solvated salts thereof] were prepd. as 5-HT6 modulators. For example, reaction of 2-chloro-4-(4-methylpiperazin-1-yl)quinazoline with N-methyl-4-chlorobenzenesulfonamide gave II in 10% yield. The radioligand binding assay showed II having Ki of 200 nM. Thus, I and their pharmaceutical compns. are useful for the treatment of 5-HT6 mediated disorders, such as Alzheimers disease, schizophrenia, obesity or Parkinsons disease. [on SciFinder(R)]. ...
A series of fourteen methoxy substituted 2-benzoyl-1-benzofuran derivatives were synthesised and their affinities determined for adenosine A1 and A2A receptors via radioligand binding assays to establish the structure ...
Leading chemical binding expert AFFIX Labs has harnessed its global experience in disease prevention to create the first long-lasting surface treatment proven to kill the coronavirus (COVID-19). Now available in Europe and the UAE and launching in new global markets, the surface treatment, known as Si-Quat, combines a safe and well-established disinfectant with the labs proprietary chemical binding technique.
As others have reported, our group also faced difficulties measuring mGluR-mediated Gαi/o activation (Niswender et al., 2008). While establishing that the GloSensor assay to measure mGlu2-, mGlu4-, mGlu6-, and mGlu8-receptor activation was surprisingly straightforward, we encountered challenges establishing an assay for mGlu7 and mGlu3 receptors. Surprisingly, mGlu7-Glo cells showed significant specific binding of the radioligand [3H]LY341495, whereas no measurable specific binding was observed at mGlu4-Glo or mGlu6-Glo cell lines. Previous reports indicate that [3H]LY341495 is not suitable for binding studies using human mGlu4 receptors, probably because of a high Kd value (Wright et al., 2000), and this may be true for rat mGlu4 receptors. Likewise, although the mGlu6-Glo cell line is functional, differences between the Kd values of [3H]LY341495 at human versus rat mGlu6 receptors could explain the lack of specific binding observed in this study. Finally, the calculated Bmax values indicate ...
Booth Profile Eurofins Abraxis, Inc., a respected provider of test kits for over 20 years, offers AbraMag Magnetic Beads for purification of DNA/RNA, antibodies, proteins, antigens, and E. coli.; immunoassay development; and bulk microplate coating. Our environmental and food test kit formats are ELISA, Magnetic Bead, Receptor Binding Assay (RBA), and Enzyme Inhibition. Find out more at www.abraxiskits.com.. ...
The selective dopamine D3 receptor antagonist [3H](+)S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro-naphtho(2,3b)dihydro,2,3- furane]), labelled to high specific activity (145 Ci/mmol), bound to cloned human dopamine D3 receptors but displayed negligible binding to cloned human D2 receptors. [3H](+)S 14297 exhibited rapid association and dissociation, high affinity saturable binding (Kd = 7.0 nM) and a competition binding profile highly correlated with that of [125I]iodosulpride (r = 0.98).. ...
The development of wireless perfect binding has gradually matured. However, in order to achieve the green printing target enterprise as soon as possible, post-press colleagues are still working hard, and in recent years, they have developed a new technology of perfect binding-lock-style bookbinding law. The new process promotes the constant transformation and development of book binding methods, and makes the technology of wireless perfect binding process move towards a more scientific and healthy direction. The following is a brief introduction to the process of the lock-type signature binding method, and to understand the low-carbon energy saving and quality effect it brings to the book binding process. Locking book signature coupling method technology The lock-type book signature coupling method is a wireless binding process method that does not require milling and slotting. It is well reflected after the test and has great promotion value. Recently, several publishing houses and printing ...
The Chemical and Chemical Engineering Resource Guide is the database dedicated to chemical engineers, helping them find the products & services they need.Biolin Scientific,Burg Translations, Inc.,De Gruyter,Labsciences, Inc.,MicroSurfaces, Inc.,Molecular Dimensions,Norgen Biotek Corp.,
The specific aims of our proposal are to develop highly sensitive PCR methods for rapid, specific diagnosis of breast cancers on the basis of their estrogen and progesterone receptor expression. The results we have obtained indicate the feasibility of identifying and quantitating various forms of the hormone receptors in a small amount of tumor tissue by molecular assays.*ANTIBODIES
Sigma receptors, both Sigma‐1(S1R) and Sigma‐2 (S2R), are small molecule‐regulated, primarily endoplasmic reticulum (ER) membrane‐associated sites
Our research group is working on the medicinal-chemical development of subtype selective inhibitors of the four GABA transport proteins mGAT1 - mGAT4. As ligand-receptor interaction generally represents highly specific processes of recognition, our particular emphasis is on the synthesis and biological evaluation of enantiomerically pure compounds. We also develop new methods of synthesis, particularly asymmetric syntheses for the expression of test compound in enantiomerically pure form. The biological screening is conducted with radioligand binding assays and a new method employing mass spectrometry we have developed to assess the ligand-receptor interaction (MS-Binding Studies).The results of the biological assays are employed in molecular modeling to create structure-activity-relationships (SAR) and 3-D bond models, which then serve as a basis for further optimizations. ...
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.: Ro 63-056
Basic saturation binding experiments to determine dissociation constants assume that the concentration of free ligands is about the same greater than 90 as the concentration of ligands added If not the results could be invalid due to ligand depletion A general rule of thumb is to use a starting concentration of protein well below 10 times the estimated and ligand concentrations that bracket the
Regulation of immune responses is tightly controlled through a balance of co-stimulatory and inhibitory checkpoint receptors, often exploited by many cancers. Therefore, therapeutics that block inhibitory receptors or activate immuno-stimulatory checkpoint receptors have proved to be powerful agents to restore anti-tumor immune responses. However, developing drugs targeting these checkpoint proteins has proved to be quite challenging, as cell-based assays used to screen for functional drugs are often difficult to create, involve the use of human primary cells, and have long, complicated protocols. Here, we present data for the new PathHunter® Checkpoint assays that target clinically relevant co-inhibitory and co-stimulatory checkpoint receptors and measure receptor activation and signaling, using the industry-validated Enzyme Fragment Complementation (EFC) technology. These assays facilitate the development of relevant therapeutics, enabling rapid and sensitive screening of biologics and small ...
A graphical method of analysis applicable to ligands that bind reversibly to receptors or enzymes requiring the simultaneous measurement of plasma and tissue radioactivities for multiple times after the injection of a radiolabeled tracer is presented. It is shown that there is a time t after which a …
I have a drug that reduces the level of a certain gene X when compared to control. Now, when I used the antagonist of the drug along with the drug itself, I see a huge increase in the mRNA levels of this gene, even higher than control itself. I know for sure that this antagonist does not have any inverse agonist activity. What other reasons could there be for this effect ...
Armalite AR-10 or RRA LAR?? - posted in Other Weapons - RIFLES (non-AK based): Pondering 308 ARs for next spring with tax check... Armalite AR-10 $1300-1600 or Rock River Arm LAR series $1100-1500. . I know the RRA can use FAL mags but is that a good reason by itself?? Anyone whom has these.. please chime in.. Al
Buy Enzymatic Therapy Resveratrol-Forte® High Potency 60 softgels at the lowest price from NaturalHealthTrust.com! Find other popular Enzymatic Therapy products, Fast delivery, best prices available!
Fish represented stockholders in an appraisal action in the Delaware Court of Chancery brought under Section 262 of the DGCL related to a merger involving Trilogy, Inc. The case settled.. ...
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 ...
"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 ...
"High-throughput screening with a miniaturized radioligand competition assay identifies new modulators of human α2-adrenoceptors ... and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand ...
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 ...
October 1999). "Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS ... binding assays". European Journal of Pharmacology. 383 (2): 209-14. doi:10.1016/s0014-2999(99)00610-x. PMID 10585536. v t e. ...
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 ...
... 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, ...
... structure activity relationships of analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays ...
7,0 7,1 7,2 7,3 7,4 7,5 Anthony P. Davenport; Fraser D. Russel (1996). "Radioligand Binding Assays: Theory and Practice". In ... "Calculations and Instrumentation used for Radioligand Binding Assays". Assay Guidance Manual: 1-21. ... 5,0 5,1 5,2 5,3 5,4 5,5 De Jong, L. A. A.; Uges, D. R. A.; Franke, J. P.; Bischoff, R. (2005). "Receptor-ligand binding assays ... "Assay Acceptance Criteria for Multiwell-Plate-Based Biological Potency Assays". BioProcess International. 12 (1): 30-41. ...
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 ... can not only quantify the affinity from concentration based assays; but also from the kinetics of association and dissociation ...
A radioimmunoassay (RIA), radioligand assay and equilibrium dialysis for determination of plasma and salivary megestrol acetate ...
... for instance in radioligand binding assays. Taken together, (-)-alazocine is a selective partial agonist of the κ-opioid ...
One assay to determine the extent at which a ligand binds to its receptor is the radioligand binding assay (RBA), in which ... While the RBA assay assumes that the tissue prepared has just one molecular target per ligand, in actuality this may not be the ... For example, serotonin binds to many diverse serotonin receptors which makes the RIA assay quite difficult to interpret. ...
... 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 ...
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. ...
This assay is commonly used to calculate the binding constant of molecules to receptors. The transport of the radioligand is ... Examples of radioligands include: 11C-WAY-100635 for the 5-HT1A receptor N(1)-([11C]-methyl)-2-Br-LSD ([11C]-MBL) for 5-HT2 ... A radioligand is a radioactive biochemical substance (in particular, a ligand that is radiolabeled) that is used for diagnosis ... Radioligands are credited with making possible the study of biomolecular behaviour, a previously mysterious area of research ...
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 ...
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 ...
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 ...
This assay is commonly used to calculate binding constant of molecules to receptors. Due to the probable injuries of PET- ... In in vivo systems it is often used to quantify the binding of a test molecule to the binding site of radioligand. The higher ... PET radiotracer is a type of radioligand that is used for the diagnostic purposes via positron emission tomography imaging ... Medicinal radiocompounds List of PET radiotracers Positron emission tomography Medicinal radiochemistry Radioligand Wadsak ...
Methods (Gut bath, Radioligand binding assay, Patch-clamp). Tolerance and resistance. *Drug tolerance ...
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 ...
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 ...
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: ...
用放射性同位素標記的放射性配體(英语:Radioligand)已被用作正電子發射計算機斷層掃描(PET)中的放射性示蹤劑。此外,這種物質還被用於在體外進行的配體-受體結合研究。 ... Protein-binding assays in biological liquids
Radioligands are radioisotope labeled compounds used in vivo as tracers in PET studies and for in vitro binding studies. ... can not only quantify the affinity from concentration based assays; but also from the kinetics of association and dissociation ... "Protein-binding assays in biological liquids using microscale thermophoresis". Nature Communications. 1 (7): 100. Bibcode ...
... binding assays, and functional experiments". Journal of Medicinal Chemistry. 43 (23): 4563-9. doi:10.1021/jm0009989. PMID ... discovery of an inverse agonist radioligand for PET". Journal of Medicinal Chemistry. 51 (6): 1800-10. doi:10.1021/jm701375u. ... "Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor" ...
March 1998). "Standard binding and functional assays related to medications development division testing for potential cocaine ... "Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding" ...
In adenylate cyclase activation assays, CRH-related peptides are 10 times more potent at stimulating CRHR2 beta than CRHR2 ... "Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin". Neuropharmacology. 36 (10): 1439-46. doi: ...
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 ...
... binding assays, and functional experiments". J. Med. Chem. 43 (23): 4563-9. PMID 11087581. doi:10.1021/jm0009989.. ... Discovery of an Inverse Agonist Radioligand for PET". J. Med. Chem. 51 (6): 1800-10. PMID 18307287. doi:10.1021/jm701375u.. ... a novel radioligand for the dopamine D4 receptor". Mol. Pharmacol. 50 (6): 1658-64. PMID 8967990.. ...
... radioligand binding and behavioural studies in two rat models of neuropathic pain". Pain. 132 (3): 289-300. doi:10.1016/j.pain. ... on a neuroendocrine biomarker assay in nonhuman primates with high kappa-receptor homology to humans" (PDF). The Journal of ... GR103545 radioligand showed CUD individuals with higher KOR availability were more prone to stress-induced relapse. A ... interpreted as increased endogenous dynorphin competing with the radioligand at the KOR binding sites. Taken together these ...
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 ...
Kohara A, Toya T, Tamura S, Watabiki T, Nagakura Y, Shitaka Y, Hayashibe S, Kawabata S, Okada M (2005). "Radioligand binding ... In the Morris watermaze test, an assay for learning abilities, those mice needed significantly more time to successfully ... Lavreysen H, Janssen C, Bischoff F, Langlois X, Leysen JE, Lesage AS (2003). "[3H]R214127: a novel high-affinity 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- ...
When compared with MLA in the rat phrenic nerve-diaphragm assay, lycoctonine-18-O-benzoate was also about 10x less potent, and ... a new radioligand for labelling alpha 7-type neuronal nicotinic acetylcholine receptors". Neuropharmacology. 38 (5): 679-90. ... In other functional pharmacological assays, lycoctonine resembled MLA qualitatively but was roughly ten times less potent. When ... in the limited number of assays to which they were subjected. MLA has been used for treating a variety of neurological ...
A single assay is typically completed in minutes and only requires a sample consumption of a few µl. Fluorescence polarization/ ... Björke H, Andersson K (January 2006). "Measuring the affinity of a radioligand with its receptor using a rotating cell dish ... Proximity ligation assay (PLA) in situ is an immunohistochemical method utilizing so called PLA probes for detection of ... A FIDA assay works in complex solutions (e.g. plasma ), and provides information regarding analyte concentration, affinity ...
As shown in Table 1, Adenylyl cyclase and cAMP assays were used in various functional studies to determine the amount of cAMP ... October 1997). "Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin". Neuropharmacology. 36 (10): ...
Binding Assay Neurotransmitter Receptor Synaptic Membrane Ligand Binding Assay Radioreceptor Assay These keywords were added by ... One of the more powerful methods for this purpose has been the radioligand binding assay (Yamamura et al, 1978). With this ... Because of its simplicity and power, the radioligand binding assay has become one of the more popular tools in neurobiological ... Enna S.J. (1984) Radioligand Binding Assays. In: Cattabeni F., Nicosia S. (eds) Principles and Methods in Receptor Binding. ...
What is Radioligand assay? Meaning of Radioligand assay as a legal term. What does Radioligand assay mean in law? ... Definition of Radioligand assay in the Legal Dictionary - by Free online English dictionary and encyclopedia. ... Radioligand assay legal definition of Radioligand assay https://legal-dictionary.thefreedictionary.com/Radioligand+assay ... Assay. (redirected from Radioligand assay). Also found in: Dictionary, Thesaurus, Medical, Financial, Encyclopedia. ASSAY. A ...
Radioligand binding Assay Using cell-line transfected with a neuropeptide GPCR, Ive carried out [125-I] radioligand binding ... Home/ Forums/ Pharmacology and Drug Discovery: Assay Development & Protocols/ Radioligand binding Assay. ... I then looked at the effect of a drug which competitively inhibited radioligand binding to the receptor. Using a fixed [drug ... assays to determine agonist affinity and estimate receptor binding sites on these cells in competitive binding assays using a ...
The non specific binding is low (under 20% of total) and is linear across all the radioligand co... ... Were developing some saturation binding curves for a muscarinic cholinergic receptor binding assay. The specific binding curve ... but then it all of a sudden takes off at higher radioligand concentrations and keeps increasing. ... Saturation curve for radioligand binding assay - posted in Biochemistry: Hi! ...
I and a specific radioreceptor assay for IGF-II following acid-ethanol extraction of the sera to remove the somatomedin binding ... Studies of insulin-like growth factor -I and -II by specific radioligand assays in umbilical cord blood Clin Endocrinol (Oxf). ... I and a specific radioreceptor assay for IGF-II following acid-ethanol extraction of the sera to remove the somatomedin binding ...
Radioligand binding assay Main project page. The experiments of research study on 125I-SI Ang II radioligand binding assay and ... User:Md Rezaul Karim/Notebook/Radioligand binding assay/Entry Base. From OpenWetWare ... Retrieved from "https://openwetware.org/mediawiki/index.php?title=User:Md_Rezaul_Karim/Notebook/Radioligand_binding_assay/Entry ... Applying different ligand-receptor binding assay techniques on the membrane preparations from rat/mouse brain/adrenal glands/ ...
An assay for quantification of drug affinity to the transporter is presented on the basis of the radioligand-binding assay ... a radioligand-binding assay was developed by taking [3H]verapamil and [3H]vinblastine as radioligands and the human intestinal ... radioligand-binding assay. FACS. fluorescence-activated cell sorting. R123. rhodamine 123. BCECF. 2′,7′-bis(2-carboxyethyl)-5(6 ... Data Derived by Radioligand Binding Assay.. One-, two- and three- affinity models were evaluated empirically and the ...
... paroxetine as radioligand in radioligand binding assay. ...
FMZ from Wistar rat cerebellum GABAA receptor by competitive radioligand assay. ...
"Radioligand Assay" by people in this website by year, and whether "Radioligand Assay" was a major or minor topic of these ... "Radioligand Assay" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... Below are the most recent publications written about "Radioligand Assay" by people in Profiles. ... Below are MeSH descriptors whose meaning is more general than "Radioligand Assay". ...
Radioligand-based binding assays. The binding assays of Hood et al.69 were used to assess the direct binding activity to COX-2 ... celecoxib for different COX-2 inhibitors measured by the radioligand-based binding assays. Control: the radioactivity of the ... The supernatant was assayed by the COX fluorescent activity assay kit according to the manufacturers instructions. ... The assay results showed that telmisartan, alendronate and chlorpropamide had IC50 values of 41.97, 90.73 and 223.5 μM for COX- ...
Radioligand-Binding Assay.. The in vitro interaction of CNI-1493 to muscarinic acetylcholine receptors was analyzed by a ... CNI-1493 (10 μM) inhibited specific binding to muscarinic receptors in an in vitro radioligand-binding assay, with highest ... radioligand-binding assay performed by NovaScreen (Hanover, MD). The ability of CNI-1493 (10 μM, duplicate tests) to bind to ...
Radioligand-Binding Assays.. Binding experiments were performed on 20-μg membrane extracts with 1-2 nM [3H]raclopride or 1 nM [ ... GTPγS Assay.. Agonist-mediated [35S]GTPγS incorporation into specific G proteins was assessed as described (21). GDP (final ... Calcium mobilization assays on stable HEK 293 cell lines expressing human D1 and/or D2 receptors (≈1 pmol/mg protein ± 0.2 pmol ... and the assay mixture was incubated on ice for 10 min. The mixture was moved to 30°C and then incubated for 5 min before adding ...
Radioligand binding assays. (−)-[3H]-nicotine competition binding assays: rat brain membranes. P2 membranes (250 μg protein) ... 1 for structures) for its ability to displace the binding of a number of nicotinic radioligands (Fig.2, Table1). Radioligand ... Competition binding assays for [3H]-nicotine binding sites (A) and [125I]-αBgt binding sites (B) in rat brain membranes, [3H]- ... In assays of 86Rb+ efflux from thalamic synaptosomes, a model of an α4β2* nAChR response, (±)-UB-165 was a very weak partial ...
Radioligand assay.. To delineate the recognition sites of the Abs by a fluid phase approach, radiolabeled FH, CFHR1, CFHR2, and ... Radioligand assay. [35S]cysteine-labeled recombinant proteins (Amersham Biosciences, Pantin, France) were produced by an in ... were tested by a radioligand assay (RLA) in the 19 patients. Fig. 5B illustrates the binding of each patients IgG to FH and ... Using ELISA assays, previous studies mapped the dominant epitope of the autoantibodies in the FH C-terminal domains (13, 18-20 ...
We offer a range of tools for receptor-ligand binding assays including radioligands, receptor-transfected cell membranes, and ... We offer a range of tools for receptor ligand binding assays including radioligands, receptor-transfected cell membranes, and ... Simplify the development of your assays and the calculation of your results using our radioligands, receptor-transfected cell ... Alpha chemiluminescent assays, lites luminescence assays, and radiometric detection methods. ...
Radioligand binding assays. Membranes from HEK-293 cells stably expressing the mouse A1AR, A2AAR, or A3AR were used for ... We gratefully acknowledge Melissa Marshall for technical assistance with radioligand binding assays and Rosa Chen for mouse ... Radioligand binding experiments were performed with 25 μg of HEK-293 cell membrane protein in a total volume of 0.1 ml of HE ... Competition binding assays were used to determine the binding affinities of various adenosine analogs at the murine A1AR, A2AAR ...
Radioligand binding was detected using a Wallac MicroBeta counter (PerkinElmer).. The β2-AR radioligand binding assays were ... IP1 HTRF assays. The IP1 HTRF assay was performed as previously described for wild-type or mutant α1B-ARs (41). Assays ... Radioligand binding assays. The affinity of NE and the allosteric antagonist ρ-TIA at the α1B-ARs was determined from [3H] ... and propranolol Ki determined from radioligand binding assays, with Iso efficacy calculated from Iso pEC50 − Iso pKi; Iso EC50 ...
Radioligand binding assays for different receptors. The 5-HT2A/2B/2CR binding assays were provided by the National Institute of ... of four individual assays. (b) Affinity of 3943 to 5HT2CR determined by radioligand binding assay. (c) Inhibition of 5HT2CR ... 10 nM binding affinity to the receptor as determined by the radioligand competition assay. Results from a thermal shift assay ... S3a†). The radioligand competition assay verified potent antagonist binding of 3943 to all three 5-HT2 receptor subtypes in the ...
Radioligand binding competition assay. HEK 293E cells were seeded in Dulbeccos modified Eagles medium supplemented with 10% ... Agarose microdroplet assay. The agarose microdroplet assay was performed to assess U-937 cellular migration, as previously ... Radioligand binding assays were performed 48 hours after transfection. Cells were washed twice in phosphate-buffered saline ( ... F) Binding of WT CXCL12 was measured by radioligand displacement of 125I-CXCL12 from CXCR4WT or CXCR4 (I4E/I6E) in membranes ...
Radioligand Binding Assays.. Competition binding assays against the CB1 receptor antagonist [3H]SR141716A rimonabant were ... 35S]GTPγS Binding Assays.. Assays were performed in triplicate in assay buffer containing 20 mM HEPES, 3 mM MgCl2, 60 mM NaCl, ... the free radioligand concentration was determined by subtraction of total bound radioligand from the added radioligand ... Assay tubes contained 0.5 nM [3H]SR141716A (Kd = 0.53 ± 0.01 nM, n = 3, determined from saturation assay curves) together with ...
Radioligand binding assays.. Assays to assess radioligand binding to CXCR7 were performed as previously described (16). ... Cell apoptosis assay.. Annexin V-FITC (Invitrogen) and propidium iodide (Invitrogen) were added to washed cells (106 cells/ml ... Adhesion assay.. HUVECs were allowed to adhere to 24-well plastic tissue culture plates overnight. The monolayer was treated ... Cell migration assays were performed using a 96-well microchamber (Chemo Tix; NeuroProbes, Inc.). Cells were resuspended in ...
Detection of Harmful Algal Toxins Using the Radioligand Receptor Binding Assay. A Manual of Methods ...
Detection of Harmful Algal Toxins Using the Radioligand Receptor Binding Assay. 2013 ...
Radioligand assay of beta adrenoceptors in lymphocytes isolated from rat spleen. / Ge, Zhi-Dong; Chen, M. Z.; Xu, S. Y. ... Ge, Zhi-Dong ; Chen, M. Z. ; Xu, S. Y. / Radioligand assay of beta adrenoceptors in lymphocytes isolated from rat spleen. In: ... Ge, Z-D., Chen, M. Z., & Xu, S. Y. (1991). Radioligand assay of beta adrenoceptors in lymphocytes isolated from rat spleen. ... Radioligand assay of beta adrenoceptors in lymphocytes isolated from rat spleen. Acta Pharmacologica Sinica. 1991 Jan 1;12(4): ...
Radioligand binding assays The first radio-receptor assay was done in 1970 by Lefkowitz et al, using a radiolabeled hormone to ... "Radioligand binding assays" Lutea A et al, 2005. Receptor-ligand binding assays: Technologies and Applications journal of ... Radioreceptor Assay of Adrenocorticotropic Hormone: New Approach to Assay of Polypeptide Hormones in Plasma Science 170 633 ... A radio-receptor assay requires the separation of the bound from the free ligand. This is done by filtration, centrifugation or ...
Radioligand binding assays. Binding assays were performed using membrane preparations from human embryonic kidney (HEK) 293 ... Thermal shift assay. The protein thermostability of purified DOP constructs was assessed with a thermal shift assay using the ... For Gαi1 biosensor assays, the indicated increasing amount of either DOP WT or BRIL-DOP crystal construct, 40 ng of Gα subunit ... For each assay, data were normalized as percentage of the maximal response for each ligand in the appropriate WT receptor ...
Competition-binding assays showed that 20-meSPX-G fully displaced [3H]epibatidine binding to HEK-293 cells expressing the human ... Binding-Competition Assays between 20-meSPX-G and Radioligands. To obtain further information on the interaction between 20- ... Competition Binding Assays. Competition binding assays with Torpedo nAChRs were performed at equilibrium (incubation during 4 h ... CO2 before collection for binding assays. Cell density was adjusted in order to specifically bind ≤10% of the radioligand. ...
Radioligand Binding Assay. For radioligand binding assays using filtration with a Brandel cell harvester (model M-30; Brandel, ... 2), radioligand binding assays were performed using [3H]kainate and [3H]MG (Fig. 3). Mutations of conserved residues in the ... From the supernatants, membranes were pelleted at 40,000×g for 20 min at 4 °C. For radioligand binding assay, membranes were ... before the radioligand binding assay was carried out. The presence of KAR subunits in membrane samples was confirmed using ...
Radioligand Binding Assays.. Saturation binding isotherms were established after the addition of 1 μg (hM3-R) or 10 μg (hM3- ... ERK1/2 Phosphorylation Assays.. ERK1/2 phosphorylation assays were performed using the AlphaScreen Surefire kit (PerkinElmer ... Ca2+]i Mobilization Assays.. Cells induced to express forms of either hM3-R or hM3-RASSL were plated in black, clear-bottomed ... Tag-Lite Internalization Assays.. Cells were plated on black, poly-d-lysine-coated 96-well plates (105 cells/well), and induced ...
  • Moreover, binding assays have been useful in examining the effects of drugs and disease on neurotransmitter receptors, and the procedure has been adapted for use as a simple and sensitive analytical method for measuring the concentration of neurotransmitters and drugs. (springer.com)
  • A receptor ligand binding assay allows for the study and simple imaging of cell surface receptors for research and diagnostic applications. (iktsm.tw)
  • Finally, CBD acted with only low affinity at cannabinoid CB 1 receptors and displayed no agonist activity in [ 35 S]guanosine 5′- O -(3-thio)triphosphate assays in cortical membranes. (aspetjournals.org)
  • A method that does not require separation is the scintillation proximity assay that relies on the fact that β-particles from 3H travel extremely short distances so the receptors are bound to beads coated with a polyhydroxy scintillant, resulting in only the bound ligands to be detected. (bionity.com)
  • In addition to inhibiting radioligand binding to rat NMDA receptors, gp120 inhibited NMDA-induced currents in Xenopus oocytes, attenuated NMDA-stimulated calcium flux and cytotoxicity in cultured cerebellar granule cells, and provided partial protection against NMDA-induced lethality in vivo. (biomedsearch.com)
  • 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)
  • A series of in vitro binding assays investigated the capacity of GET73 to bind to the GHB binding site and multiple other receptors. (frontiersin.org)
  • Methods and Results - In assays of recombinant canine Ado receptors, ATL-193 and ATL-146e were highly selective for the A 2A over the A 1 and A 3 receptors and were more potent than MRE-0470 and CGS-21680. (ahajournals.org)
  • Radioligand binding studies confirmed that buspirone binds with high affinity to recombinant human D3 and D4 receptors (∼98 and ∼29 nm respectively). (nih.gov)
  • Live cell functional assays also revealed that buspirone, and its metabolites, function as antagonists at both D3 and D4 receptors. (nih.gov)
  • At GVK BIO, we have capabilities for measuring GPCR functional responses by developing cAMP assays for Gs coupled receptors and Ca2+ measurements for Gq coupled receptors. (gvkbio.com)
  • We also have capabilities for performing Guanine nucleotide binding assay ([35S] GTPγS assay) for Gi coupled receptors. (gvkbio.com)
  • The principle of radioligand binding assay is based on labelled radioligand molecules binding to specific receptors, transporters, enzymes or any protein of interest. (gvkbio.com)
  • Biochemical assays for receptors, enzymes, etc. (wuxiapptec.com)
  • And alternatively, a pure biochemical binding assay may not work for certain G-coupled protein receptors, because for example, if you're looking for an agonist response, a binding assay doesn't really help you. (ddw-online.com)
  • Remembers Henry I. "Hank" Yamamura, an eminent neuropharmacologist who pioneered radioligand binding assays, contributing valuable knowledge about neurotransmitter transporters and receptors. (drugabuse.gov)
  • Pharmacology is not my thing at all and I'm stuck in the middle of all this because of these binding assays I did! (scientistsolutions.com)
  • We offer a range of tools for receptor ligand binding assays including radioligands, receptor-transfected cell membranes, and cell lines. (iktsm.tw)
  • 4 Radioligand binding assays, which assess receptor-ligand interactions on cell surfaces, are increasingly restricted due to high production costs and hazards to human health. (rsc.org)
  • 3 Alternative receptor binding assays using fluorescently labeled probes require careful compound design and optimization because of the impact of fluorophore attachment on ligand affinity and efficacy. (rsc.org)
  • Competition-binding assays showed that 20-meSPX-G fully displaced [ 3 H]epibatidine binding to HEK-293 cells expressing the human α3β2 (Ki = 0.040 nM), whereas a 90-fold lower affinity was detected in human α4β2 nAChR. (mdpi.com)
  • Epibatidine binding assays in peripheral blood leukocytes can be used to evaluate an individual's exposure to, and dependence on, nicotine. (google.es)
  • 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)
  • 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)
  • 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)
  • 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)
  • 36. A method for screening of chemical libraries, for catalysis, for facilitating synthesis, for analyte determination using ligand binding assays and/or agglutination assays, for therapeutic purposes, or for controlled release comprising using the molecularly imprinted microspheres according to claim 1. (freepatentsonline.com)
  • The principles of radioligand‐binding assays. (els.net)
  • Membranes from HEK293 cells were prepared and used for radioligand binding assays as described in Method. (nih.gov)
  • In this study, we set out to investigate each compound's protein targets and mechanism of action through prediction of protein targets via a ligand-based target prediction protocol, P rediction I nclu D in G IN actives, and radioligand binding assays. (springer.com)
  • We employ filtration or SPA technologies for the binding assays. (gvkbio.com)
  • Radioligand binding assays are developed for several therapeutic targets. (gvkbio.com)
  • Forty-seven breast cancer tissue samples were available with EGFR values previously determined in radio-ligand binding assays. (hindawi.com)
  • Evotec offers cell membrane preparations in bulk in different purity grades e.g. for ligand binding assays or in vitro transporter activity assays. (evotec.com)
  • Photoaffinity labeling and binding assays using transgenic tobacco ( Nicotiana tabacum ) cells expressing PEPR1 and PEPR2 clearly demonstrated that PEPR1 is a receptor for Pep1-6 and that PEPR2 is a receptor for Pep1 and Pep2. (plantcell.org)
  • All cell lines are screened using immunofluorescence labelling, Western blot, or RT-PCR, and further validated in cell-based assays to confirm the functional expression of the target protein. (evotec.com)
  • Frozen cell are bulk produced from up to 10 billion cells in a batch, validated by help of functional cell-based assays and provided in customised aliquots (e.g. in plates, vials, tubes, or bags). (evotec.com)
  • Today we're going to discuss the current and emerging trends in cell-based assays. (ddw-online.com)
  • We know that cell-based assays now play a fundamental part in a successful lead discovery strategy, and we know that functional approaches open new opportunities to novel targets and to produce results that are more biologically relevant in in vivo studies. (ddw-online.com)
  • So my question is, when should we use cell-based assays? (ddw-online.com)
  • How do you differentiate cell-based assays from biochemical, or biologicalbiochemical assays? (ddw-online.com)
  • I think if you look at biochemical versus cell-based assays, I think historically biochemical assays as mentioned in terms of ligand binding to a membrane that has the GPCR for example, gave very robust straightforward information. (ddw-online.com)
  • And probably cell-based assays have started to merge, because you've got the whole functionality of the cell as it relates to the function of the target. (ddw-online.com)
  • And the second aspect, is and even one of each is insufficient nowadays, given the repertoire of behaviours of different ligands have been found to engender especially as a consequence of functional cell-based assays. (ddw-online.com)
  • Cell-based assays as Richard pointed out provide context, but the context can change from cell to cell. (ddw-online.com)
  • In vitro, 3 and its analogs were potent agonists in [ 35 S]GTP γ S assays at the mu opioid receptor but failed to recruit β -arrestin-2, which is associated with opioid side effects. (pubmedcentralcanada.ca)
  • Somatomedin concentrations in human umbilical sera (n = 206) were measured using a specific radioimmunoassay for insulin-like growth factor (IGF)-I and a specific radioreceptor assay for IGF-II following acid-ethanol extraction of the sera to remove the somatomedin binding proteins. (nih.gov)
  • The preparations were active in a radioligand binding inhibition assay and in a rat liver based radioreceptor assay. (ias.ac.in)
  • Affinity MS-based assays have been developed for screening chemical ligands towards different soluble protein targets, especially enzymes and kinases of therapeutic values. (rsc.org)
  • It is used for preparing and purifying radio-labeled polypeptide ligands, extracting and preparing steroid hormones for assay and receptor protein isolation. (umes.edu)
  • In contrast, (±)-UB-165 and (±)-anatoxin-a were similarly efficacious and similarly sensitive to α-conotoxin-MII in increasing intracellular Ca 2+ in SH-SY5Y cells, a functional assay for native α3-containing nAChR. (jneurosci.org)
  • And a cell-based assay would be a functional assay responding to a secondary messenger signal, or some other cellular response? (ddw-online.com)
  • An assay for quantification of drug affinity to the transporter is presented on the basis of the radioligand-binding assay principle. (aspetjournals.org)
  • The concentration-dependent displacement of the radioligand by nonlabeled substrates for P-gp should be a suitable principle for the determination of drug affinity to the respective binding sites at the human intestinal multidrug transporter P-gp. (aspetjournals.org)
  • None of these assays allow interpretation of the results with respect to drug affinity to P-gp, although direct binding of substrates to P-gp has been shown with the use of photoaffinity labeling analogs of vinblastine and colchicine. (aspetjournals.org)
  • The first radio-receptor assay was done in 1970 by Lefkowitz et al, using a radiolabeled hormone to determine the binding affinity for its receptor. (bionity.com)
  • Using saturation‐binding curves and Scatchard transformation, the affinity of the radioligand for the receptor can be determined. (els.net)
  • Since Ga68 DOTATATE has a high affinity to only sstr2 but no affinity to sstr3 and sstr5, Ga68 DOTANOC has been suggested to be a better radioligand with higher affinity to sstr3 and sstr5 and high affinity to sstr2, as well. (enets.org)
  • Historically, ligand binding assay techniques were used extensively to quantify hormone or hormone receptor concentrations in plasma or in tissue. (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)
  • How do I get from my data which is amount of radioligand bound vs. unlabelled [ligand] to a Hill plot to see if there is any co-operativity between the binding sites? (scientistsolutions.com)
  • 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)
  • Nonhem blot and ribonuclease protection assay were used to identify alpha_2-AR subtypes in human colonic adenocarcinoma (HT29), opossum kidney (OK), and neuroblastoma x glioma rat-mouse hybrid NGlO815 (NG108) cell lines. (nii.ac.jp)
  • For example, receptor functional assays, which measure GPCR downstream signaling effectors, 3 are inadequate for identifying allosteric or biased signaling modulators and often generate hits unsuitable for subsequent optimization. (rsc.org)
  • As an extension to our receptor binding assay platform, we have developed in-house functional assays to screen the GPCR targets. (gvkbio.com)
  • Following treatment with assay reagent (DiscoveRx Inc.), luminescence was measured as described in Method. (nih.gov)
  • Simplify the development of your assays and the calculation of your results using our radioligands, receptor-transfected cell membranes, and cell lines for receptor ligand binding applications. (iktsm.tw)
  • Membranes are prepared from bulk cells, characterized, validated and used in the binding assay for screening of NCEs. (gvkbio.com)
  • In vitro assays in cultured INS-1E β-cells were carried out in order to clarify the mechanism by which β 2 AR deficiency affects glucose metabolism. (diabetesjournals.org)
  • Or else, since I think the drug could be binding to a site distinct from the agonist binding site, could it be that the drug alters the receptor conformation which also changes the configuration of the agonist binding site and so prevents radioligand binding? (scientistsolutions.com)
  • Products available support both agonist and antagonist assays. (iktsm.tw)
  • The RBA and transactivation assay revealed that GTx-822 is an ERβ-selective agonist ( K i = 0.53 nM). (arvojournals.org)
  • We're developing some saturation binding curves for a muscarinic cholinergic receptor binding assay. (protocol-online.org)
  • Also, we cannot exclude the possibility that the epitopes presented by the recombinant cells are not the same with those recognised by the previously reported radioligand assays [7, 18, 21]. (thefreedictionary.com)
  • 2-chloro- N 6 -(3-iodobenzyl)-5′- N -methylcarboxamide (390 ± 160 nM), similar to the potency order to compete for radioligand binding to the recombinant murine A 2A AR but not the A 3 AR. (jimmunol.org)
  • Radioligand binding and fibroblast proliferation assay demonstrated that the peptides were functional. (curehunter.com)
  • For the proliferation assay, cells are plated at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1. (selleckchem.com)
  • METHODS Using 125 I labeled [Leu 15 ] gastrin 17 I as the radioligand, rat gastric parietal cells as the receptor preparations. (bvsalud.org)
  • CONCLUSION The radioligand binding assay of gastrin receptor in rat gastric parietal cell preparations meets the criteria for establishing receptor binding assay. (bvsalud.org)
  • The laboratory is equipped with High Pressure Liquid Chromatography (HPLC) and Enzyme Linked Immunosorbent Assays (ELISA). (umes.edu)
  • We evaluated a newer sandwich ELISA assay (Cisbio US, Bedford, MA, USA) that utilizes two monoclonal antibodies that bind to the mid-region of the CgA protein and allow measurement of intact and fragmented circulating CgA. (enets.org)
  • alpha_2-Adrenoceptor subtype expression was investigated in cultured rat inner medullary collecting duct (IMCD) cells using radioligand binding studies, Nonhem blot analysis, and cAMP assay. (nii.ac.jp)
  • For GPCRs coupled with Gs G-protein, cAMP assay is employed to determine the functionality of the expressed protein. (gvkbio.com)
  • In GVK BIO we employ cAMPGlo assay and Alpha screen technology to perform cAMP assay. (gvkbio.com)
  • Through the development of RIA technology, researchers have been able to move beyond the use of radioactivity, and instead, use liquid- and solid-phase, competitive, and immunoradiometric assays. (wikipedia.org)
  • Levels of radioactivity for a radioligand (per mole) are referred to as the specific activity (SA), which is measured in Ci/mmol. (wikipedia.org)
  • Or maybe you mean, for example, in GPCRs, a biochemical assay would be a receptor binding assay? (ddw-online.com)
  • But back to what Robert was asking earlier, I think ideally you probably want to have a combination of an in vitro cell-based assay and a biochemical assay just to confirm that whatever you identify in a cell-based assay is really acting via the receptor and not some secondary response in an intracellular location. (ddw-online.com)
  • But the binding or the biochemical assay has got to remain as a validation step. (ddw-online.com)
  • One of the more powerful methods for this purpose has been the radioligand binding assay (Yamamura et al, 1978). (springer.com)
  • The receptor (R) preparation and radioligand (L) are incubated to equilibrium. (els.net)
  • Our scientific team with sound technical and analytical skills has developed more than 200 assays against the targets that include GPCRs, Ion channels, transporters and several kinases with a novel methodology. (gvkbio.com)
  • Increasingly, enzymes are being recognized as potential drug targets in drug discovery and GVK BIO offers high quality assay development solutions with various readouts and formats. (gvkbio.com)
  • Immunohistochemical assays, with monoclonal antibodies, are the most commonly used methods for establishing receptor status. (hindawi.com)
  • METHODS: Platelet [3H] paroxetine binding sites were assayed and the m-CPP challenge test was performed in 35 African American cocaine dependent individuals and 33 controls. (duke.edu)
  • Combining expertise in cell sciences and protein production methods with biophysics, functional assays, and HTS Evotec offers clients flexible and efficient platforms for timely delivery of high quality discovery reagents. (evotec.com)
  • To address the need of the hour, we have established various cell lines expressing GPCRs and validated the assays. (gvkbio.com)
  • Ca 2+ release assay is used for GPCRs couple with Gq G-protein. (gvkbio.com)
  • A fluorometric assay using FLIPR is employed to determine the Ca 2+ release by GPCRs. (gvkbio.com)
  • A radio-receptor assay requires the separation of the bound from the free ligand. (bionity.com)
  • The Radioligand Assay Laboratory in Trigg Hall is designed to conduct radio-immunoassays and/or radio receptor assays. (umes.edu)
  • With a flexibility to adapt assays developed at the client's site, we take up the task of screening at our facility. (gvkbio.com)
  • The dedicated facility for radioactive assay readouts enables us to handle assay volumes that range from low to high throughput screening of drug candidates using radiolabeled C, P, H and I reagents. (gvkbio.com)
  • WuXi AppTec's discovery biology services, which are part of our integrated pharmaceutical services, include reagent generation, assay development, screening, biomarker research, custom monoclonal antibody generation, and stable line development, as well as biosafety and adventitious virus testing. (wuxiapptec.com)
  • The actual concentration of a radioligand is determined by the specific stock mix for which the radioligand originated (from the manufactures. (wikipedia.org)
  • The experiments of research study on 125I-SI Ang II radioligand binding assay and angiotensin II receptor subtype quantification. (openwetware.org)
  • GVK BIO offers customized assay development solutions to help you reach your goals quickly and cost effectively. (gvkbio.com)
  • The specific binding curve initially looks as one would expect (i.e. very sharp increase followed by a plateau) but then it all of a sudden takes off at higher radioligand concentrations and keeps increasing. (protocol-online.org)
  • The non specific binding is low (under 20% of total) and is linear across all the radioligand concentrations. (protocol-online.org)
  • 2018. Assay of steroids by liquid chromatography-tandem mass spectrometry in monitoring 21-hydroxylase deficiency. (uib.no)
  • Yes, there's always the issue of whether an in vitro cell-based assay will truly mimic the in vivo response. (ddw-online.com)
  • The results from the assay validation indicative of its overall robustness in terms of sensitivity, specificity, reproducibility, and stability are presented here. (enets.org)
  • Any suggestions for ways to reduce background signal when doing these assays with plate-bound cells? (protocol-online.org)
  • Some newer types are called "mix-and-measure" assays because they do not require separation of bound from unbound ligand. (wikipedia.org)
  • 2017. Simultaneous assay of cortisol and dexamethasone improved diagnostic accuracy of the dexamethasone suppression test. (uib.no)
  • We used the R-CEPIAer endoplasmic reticulum calcium reporter to functionally assay for Gq-coupled receptor signaling, and investigated the bis-quinolinium cyclophanes as antagonists of M3 mACHR activation in transfected CHO cells. (frontiersin.org)
  • We had similar findings in preliminary experiments using the same GAD 65 antigen as in assay 2 in a radioligand assay developed in our laboratory. (thefreedictionary.com)
  • Verapamil was the radioligand of choice for further investigations due to its lower nonspecific binding to the transporter preparation. (aspetjournals.org)
  • Because of the reversible and competitive interaction of numerous substrates with P-gp, a radioligand-binding assay was developed by taking [ 3 H]verapamil and [ 3 H]vinblastine as radioligands and the human intestinal Caco-2 cells, overexpressed with P-gp by culturing in the presence of vinblastine or transfecting with multidrug resistance gene MDR-1 as receptor preparation. (aspetjournals.org)
  • If so could this be due to receptor internalization (assays were all carried out on whole cells at 37degC but without inhibitors of internalization! (scientistsolutions.com)
  • Evotec's cell culture unit has many years expertise producing assay ready frozen cells for our partners from leading pharma and biotech companies. (evotec.com)