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, ...

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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 ...

exports data, which is sequentially by RRA, from oldest to newest data points within each RRA. Data points are overwritten if they exceed the maximum allowed threshold or if they do not reach the minimum required threshold.. Spikekill will cease overwriting data points for any individual RRA when it has reached the value of Kills Per RRA, counting all DSes of that RRA together. It will then begin the process again on the next RRA.. This means that for any given RRA, older spikes will always be overwritten before newer spikes. However, newer spikes in one RRA can still be overwritten before older spikes in a different RRA, since the thresholds are different per RRA:DS pair.. ...

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.

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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 ...

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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.. ...