Radioligand binding
Electrophysiological and radioligand binding characterisation of somatostatin receptors in rat brain and pituitary
... It remains a matter of contention as to whether the endogenously occurring tetradecapeptide and octacosapeptide forms of somatostatin function as separate and independent hormones and neuromodulators, whether they are ...
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PET radioligand binding to translocator protein (TSPO) is increased in unmedicated depressed subjects
... In order to reduce the likelihood of type II errors, we se- lected two regions of interest a priori: the anterior cingu- late cortex (ACC) and the subgenual prefrontal cortex (sgPFC). These regions were selected because ...
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Selectivity of Dobutamine for Adrenergic Receptor Subtypes: IN VITRO ANALYSIS BY RADIOLIGAND BINDING
... FIGuRE 5 Dobutamine open symbols and - epinephrine Because guanine nucleotides do not alter agonist competition filled symbols competition for DHE binding to human curves for [3H]prazosi[r] ...
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Distinct platelet thromboxane A2/prostaglandin H2 receptor subtypes A radioligand binding study of human platelets
... platelet binding site by stable TXA2/PGH2 ...two binding sites; a high-affinity site with Kd of 234 +/- 103 pM, Bmax of ...Parallel binding studies using the TXA2/PGH2 receptor antagonist ...
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Pharmacological characterization of the αvβ6 integrin binding and internalization kinetics of the foot-and-mouth disease virus derived peptide A20FMDV2
... of radioligand binding could be achieved up to 24 ...site binding. This is supported by direct competition at the RGD binding site with SC-68448 not being sufficient to fully reverse ...
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Large-scale functional expression of WT and truncated human adenosine A2A receptor in Pichia pastoris bioreactor cultures
... addition radioligand binding indicated that there was an approximately three and a half times higher functional expression for the bioreactor culture compared to the flask culture (summarised in Table ...
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Defective dopamine 1 receptor adenylate cyclase coupling in the proximal convoluted tubule from the spontaneously hypertensive rat
... by radioligand binding and by adenylate cyclase (AC) ...Specific binding of 125I-SCH 23982 (defined by 10 microM SCH 23390, a DA-1 antagonist) was concentration dependent, saturable, and ...23982 ...
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NMDA receptor subtypes expressed in mammalian cells: A molecular characterisation
... [^H]MK801 radioligand binding to the recombinant receptor populations was initially assayed by full saturation curves as opposed to single point binding since the presence o f the N R la, NR2A and ...
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PubMedCentral-PMC4961583.pdf
... Author Contributions D.P.S and R.T.S conceived the project. Pharmacological assessment of the interactions between Nb60 and Nb80 with the β 2AR were designed, performed and analyzed by D.P.S., R.T.S, B.P., S.A., and A.C. ...
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Kinetic analysis and test-retest variability of the radioligand [11C](R)-PK11195 binding to TSPO in the human brain - a PET study in control subjects
... using radioligand binding to mar- kers of microglia has potential to serve this ...reference radioligand [ 11 C](R)- PK11195 and a subsequent series of radioligands binding to the ...
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Characterisation of the binding of two novel glycine site antagonists to cloned NMDA receptors
... tv^o-site binding models was to analyse the competition binding of pH] MDL105,519 to N Rl-la/N R2A receptors that is operative only for heteromeric ...L-glutamate binding site is localised to the NR2 ...
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Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism
... kinetic radioligand binding assays yielding affinity values and kinetic binding parameters, which resulted in traditional SAR and novel SKR, ...other radioligand binding experiments ...
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A PET imaging agent for evaluating PARP 1 expression in ovarian cancer
... Using the PARP1-KO cell lines along with several nonmodified EOC cell lines, we showed significant differences in the radioligand binding of [125I]KX1 relative to PARP-1 expression Figur[r] ...
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Cessation of anti-VLA-4 therapy in a focal rat model of multiple sclerosis causes an increase in neuroinflammation
... Simplified reference tissue modelling has been used pre- viously to analyse TSPO tracers with contralateral refer- ence input [26]. In the fDTH-EAE-model, the input can be obtained from the contralateral hemisphere due ...
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Potential for imaging the high-affinity state of the 5-HT1B receptor: a comparison of three PET radioligands with differing intrinsic activity
... cacy PET radioligand that has been used in multiple studies over the last decade [16, 20]. [ 11 C]3 is an agonist with some antagonist activity that had previously been studied with PET in NHP at baseline only ...
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Radiolabeled Peptides: Valuable Tools for the Detection and Treatment of Cancer
... application as radiopharmaceuticals since they may be degraded before reaching the intended target. Therefore, most peptides have to be modified syn- thetically to minimize rapid enzymatic degradation [1, 41]. Great ...
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New approaches for the reliable in vitro assessment of binding affinity based on high-resolution real-time data acquisition of radioligand-receptor binding kinetics
... kinetic binding ap- proaches comprise tracer administration and subsequent binding to living cells, expressing the dedicated target ...time-resolved radioligand-receptor binding kinetics has ...
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Radioimmunoassay of growth hormone dependent insulinlike growth factor binding protein in human plasma
... A specific radioimmunoassay has been established for a growth hormone-dependent insulinlike growth factor (IGF) binding protein (BP) from human plasma. Although the assay was directed against a 53-kD, acid-stable ...
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Chemical and analytical aspects of radioligand development for quantitative neuroimaging
... There are a number o f disadvantages associated with the positron emitting iodines for use in human s t u d i e s . T h e low level o f positron em ission (23%) means that the count rate from a given dose will be low. In ...
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Detection by Radioligand Assay of Antibodies against Borna Disease Virus in Patients with Various Psychiatric Disorders
... Eleven and 17 sera for BDV-N and -P, respectively, were positive in Western blotting but not in radioligand assay. One of the factors for this disagreement may be low specificity of Western blotting due to ...
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