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1 ies and was selected for evaluation as a PET radioligand.
2 showed excellent kinetic properties as a PET radioligand.
3 the radioligand and (S,S)-68 displacing the radioligand.
4 ET with [(11)C]MePPEP, a CB1 inverse agonist radioligand.
5 wly developed dopamine transporter (DAT) PET radioligand.
6 uman tissues with (125)I-GLP-1(7-36)NH2 as a radioligand.
7 adioligand injection was virtually unchanged radioligand.
8 [(11)C]carfentanil, a selective MOR agonist radioligand.
9 the healthy volunteer white matter for both radioligands.
10 of either, inhibiting the development of PET radioligands.
11 gands; and sequential injection of different radioligands.
12 sitron emission tomography and TSPO-specific radioligands.
13 rospective clinical trials with several PSMA radioligands.
14 mor targeting are diagnostic and therapeutic radioligands.
15 rostate specific membrane antigen-617 (PSMA) radioligands.
16 y needed as versatile complementary tools to radioligands.
17 nthetic approach simplifies the discovery of radioligands.
18 visualized using translocator protein (TSPO) radioligands.
19 muSv/MBq, which is typical for (18)F-labeled radioligands.
20 crease the therapeutic index of the targeted radioligands.
22 positron emission tomography with the novel radioligand (11)C-dihydroergotamine, which is chemically
25 gand (18)F-MNI-659, the dopamine D1 receptor radioligand (11)C-NNC 112, and the 5-HT2A radioligand (1
26 gand (18)F-MNI-659, the dopamine D1 receptor radioligand (11)C-NNC 112, and the 5-HT2A radioligand (1
27 ls were imaged with the dopamine D2 receptor radioligand (11)C-raclopride, the PDE10A radioligand (18
28 ls were imaged with the dopamine D2 receptor radioligand (11)C-raclopride, the PDE10A radioligand (18
31 n emission tomography (PET) imaging with the radioligand [(11)C]AZ10419369 administered as a bolus fo
32 with positron emission tomography, using the radioligand [(11)C]AZ10419369 for quantification of cere
33 nteers using the mu-opioid receptor-specific radioligand [(11)C]carfentanil three times, as follows:
35 ography (PET) scans with the 5-HT2AR agonist radioligand [(11)C]Cimbi-36: one at baseline and one or
36 mission tomography scans with the novel FAAH radioligand [(11)C]CURB and structural magnetic resonanc
38 n of activated microglia, as measured by the radioligand [(11)C]PK11195, and the regional distributio
39 orted CB2 positron emission tomography (PET) radioligand [(11)C]RSR-056, 38 fluorinated derivatives w
41 tron emission tomography (PET) with the SV2A radioligand [(11)C]UCB-J to examine synaptic density in
42 and sex-matched healthy controls, using the radioligands [(11)C]DASB (3-amino-4-(2-dimethylaminometh
43 utility of the novel 5-HT2A receptor agonist radioligand, [(11)C]CIMBI-36, and a d-amphetamine challe
46 ns of the positron emission tomography (PET) radioligand [11C]raclopride directly to subsecond dopami
47 the highly specific dopamine transporter PET radioligand, 11C-PE2I, to assess the association between
48 vivo kinetics of the novel tau-specific PET radioligand (18)F-AV-1451 in cognitively healthy control
49 ) was examined with the dopamine transporter radioligand (18)F-FE-PE2I (94 MBq) to evaluate the in vi
52 tor radioligand (11)C-raclopride, the PDE10A radioligand (18)F-MNI-659, the dopamine D1 receptor radi
53 tor radioligand (11)C-raclopride, the PDE10A radioligand (18)F-MNI-659, the dopamine D1 receptor radi
54 efore, we recommend clinical transfer of the radioligand (18)F-PSMA-1007 for use as a diagnostic PET
57 dy uses the novel second-generation TSPO PET radioligand [(18)F]FEPPA to evaluate whether microglial
60 e report the pharmacokinetics of a novel PET radioligand, (18)F-LSN3316612, which binds with high aff
61 for in vitro and in vivo characterization of radioligands(2), yet there exist few radiolabelling prot
62 n AD sections comparable to the tau-specific radioligand (3)H-T808; second, by very low nonspecific b
63 no group in 17 resulted in high affinity Y4R radioligands ([(3)H]-(2R,7R)-10, [(3)H]18) with subnanom
64 n determined in competition with the agonist radioligand [(3)H]7-hydroxy-N,N-dipropyl-2-aminotetralin
65 erties of tool compounds for CB2R (e.g., the radioligand [(3)H]CP55,940) are not optimal, despite the
67 of the highly stable carbamoylguanidine-type radioligand [(3)H]UR-KAT479 ([(3)H]23), a subtype select
68 O and specific binding of two TSPO targeting radioligands (3H-PK11195 and 3H-PBR28) in tissue section
69 ntroduction of small-molecule PSMA inhibitor radioligands, 40 y after the clinical introduction of (1
73 e describe the characterization of an M1 PAM radioligand, 8-((1S,2S)-2-hydroxycyclohexyl)-5-((6-(meth
74 nge with unlabeled ligand failed to diminish radioligand accumulation in brain tissue, due to the blo
79 inding assay, with (R,R)-68 potentiating the radioligand and (S,S)-68 displacing the radioligand.
80 to those previously reported using the same radioligand and a high-resolution research tomograph.
82 tive binding assays (IC(50)) and dual-tracer radioligand and fluorescence internalization studies.
84 egions of interest were the striatum for all radioligands and additionally the striatum, rostral cort
86 utility and the development of tools such as radioligands and positron emission tomography tracers th
87 ecular targets; coinjection of a cocktail of radioligands; and sequential injection of different radi
88 of neuroinflammation, most second-generation radioligands are sensitive to the single nucleotide poly
91 concern for therapeutic applications of PSMA radioligands, because therapeutic radiation will damage
92 0)Y-pentixather-a CXCR4-directed therapeutic radioligand-before conventional conditioning therapy fol
93 tistically significant reduction (-36.2%) in radioligand binding (HCs, 5.6; T1DMs, 3.6; P = 0.03).
94 adenosine receptor (AR) agonists) to enhance radioligand binding allosterically at the human dopamine
97 binding configurations with a combination of radioligand binding and flux assays on wild-type and mut
98 e A1AR second extracellular loop (ECL2) with radioligand binding and functional interaction assays to
100 uch that endoplasmic reticulum export of and radioligand binding and substrate uptake by these DAT mu
101 localization and quantitative correlation of radioligand binding and tau antibody staining on the sam
102 mutagenesis and the scintillation proximity radioligand binding assay improved our understanding of
103 The synthesized compounds were tested in radioligand binding assay on rat cortex against [(3)H]-c
104 e challenges (SPMChs) and PBMC B2AR numbers (radioligand binding assay) and signaling (cyclic AMP ELI
108 esized by organic chemistry and evaluated in radioligand binding assays using FAP-expressing HT-1080
109 ds: Synthesis, radiochemistry, stability and radioligand binding assays were performed for the novel
116 nositol 1,4,5-trisphosphate accumulation and radioligand binding experiments to determine the impact
120 overed substantial ubiquitous GSK-3-specific radioligand binding in Tg2576 Alzheimer's disease (AD),
123 TR2 expression in tumor cells, and increased radioligand binding of (68)Ga-DOTATOC to these tumor cel
125 d a strong correlation was found between the radioligand binding signal for both tracers and the numb
128 ist dissociation kinetics, and together with radioligand binding studies suggested a role for slow of
133 void of tau pathology, excluding significant radioligand binding to any other central nervous system
135 scribe a novel method of kinetic analysis of radioligand binding to neuroreceptors in brain in vivo,
136 tion in brain tissue, due to the blocking of radioligand binding to plasma proteins that elevated the
141 HxR (x: 1-4) subtypes on Sf9 cell membranes (radioligand binding, [(35)S]GTPgammaS, or GTPase assays)
142 amples and mode of action studies, including radioligand binding, inositol phosphate, and toxicity as
144 5/7.18, comparable to binding constants from radioligand binding/flow cytometry; fast association/dis
146 nds have traditionally been characterized by radioligand-binding assays, which have low temporal and
147 based on systematic mutagenesis coupled to a radioligand-binding thermostability assay that can be ap
150 lution, in vitro binding of the PD-sauvagine radioligand currently provides the most sensitive and ac
151 The resulting binding potentials of the radioligand declined by 50-60% in the presence of unlabe
153 n acceptable compromise between optimal PSMA radioligand design and a broad range of clinical demands
154 ctrophysiology in Xenopus laevis oocytes and radioligand displacement assays with human embryonic kid
156 e availability of cooperativity factors from radioligand displacement experiments are expected to imp
159 ly half of the 38 lead compounds altered the radioligand dissociation rate, a hallmark of allosteric
163 nectin was labeled with (18)F to yield a PET radioligand for assessing PD-L1 expression in vivo.
164 18)F-PF-06684511 is the first successful PET radioligand for BACE1 brain imaging that demonstrates fa
167 luorodibenzo[b,d]thiophene 5,5-dioxide) is a radioligand for estimating the availability of alpha7-nA
168 s show that (18)F-LSN3316612 is an excellent radioligand for imaging and quantifying OGA in rhesus mo
170 e-NB1 is a highly selective and specific PET radioligand for imaging the GluN2B subunit of the NMDA r
171 F-tetrafluoroborate ((18)F-TFB), a novel PET radioligand for imaging the human sodium/iodide symporte
172 Conclusion: (18)F-MK-6240 is a promising PET radioligand for in vivo imaging of neurofibrillary tau a
174 meno[3,4-f]-quinoline ((+/-)-(11)C-YJH08), a radioligand for PET that engages the ligand binding doma
177 mission tomography (PET) and [(11)C]UCB-J, a radioligand for the synaptic vesicle glycoprotein 2A (SV
178 that the future development of any improved radioligand for TSPO should consider the possibility tha
180 ical potential of (68)Ga-NOTA-AE105 as a new radioligand for uPAR PET imaging in cancer patients.
181 ical potential of (68)Ga-NOTA-AE105 as a new radioligand for uPAR PET imaging in cancer patients.
182 at (18)F-fluorodeprenyl-D2 is a suitable PET radioligand for visualization of MAO-B activity in the h
186 idity of novel (18)F-GE-179 and (18)F-GE-194 radioligands for the detection of changes in active NMDA
187 using positron emission tomography (PET) and radioligands for the translocator protein (TSPO), a mark
188 the aim of this study was the development of radioligands for Y(1)R imaging by positron emission tomo
191 incidence and mortality of PC, the new PSMA radioligands have already had a remarkable impact on the
193 (11)C-JNJ-42491293, a novel high-affinity radioligand (human 50% inhibitory concentration = 9.6 nM
198 g (67/68)Ga-, (111)In-, and (177)Lu-NeoBOMB1 radioligands in GRPR-expressing cells and mouse models.
199 indicate that the high accumulation of PSMA radioligands in salivary glands does not correspond to h
200 of prostate-specific membrane antigen (PSMA) radioligands in salivary glands is still not well unders
201 e, that the significant accumulation of PSMA radioligands in SMG is not primarily a result of PSMA-me
202 e whether the accumulation of PSMA-targeting radioligands in submandibular glands (SMGs) can be expla
203 -11-labelled complex pharmaceuticals and PET radioligands, including a one-step radiosynthesis of the
204 rience over the last 3 years using different radioligands indicates that PRLT is highly effective for
206 t radioactivity in rat brain at 30 min after radioligand injection was virtually unchanged radioligan
207 ron emission tomography with a D2R-selective radioligand insensitive to endogenous dopamine, (N-[(11)
209 nsporters, and PET studies suggest that this radioligand is suitable for quantitative neuroimaging of
210 MAGL inhibitor 7 (PF-06809247) as a suitable radioligand lead, which upon radiolabeling was found to
211 nonspecific binding of the first-generation radioligand, low-resolution scanners, small sample sizes
212 hypothesized that imaging with EGFR-specific radioligands may facilitate noninvasive measurement of E
213 uced changes to agonist binding validated by radioligand measurements, and iii) testable hypotheses o
215 breast cancer, targeting this receptor with radioligands might have a significant impact on staging
216 of general and efficient approaches to label radioligands necessary for drug discovery programs remai
217 tly employed histamine H(2) receptor (H(2)R) radioligands possess several drawbacks, for example, hig
220 [(3)H]6 constitutes the first GPR84 agonist radioligand representing a powerful tool for this poorly
221 Noninvasive PET/CT imaging using a CXCR4 radioligand revealed enlarged med-LNs with increased cel
224 c binding to Y(1)R in vitro and in vivo, the radioligands still need to be optimised to achieve highe
225 ort the suitability of (11)C-GSK1482160 as a radioligand targeting P2X7R, a biomarker of neuroinflamm
226 ort the suitability of (11)C-GSK1482160 as a radioligand targeting P2X7R, a biomarker of neuroinflamm
227 atic castration-resistant prostate cancer by radioligands targeting prostate-specific membrane antige
230 ssion tomography (PET) and [(11) C]ABP688, a radioligand that binds specifically to the mGluR5 allost
232 relationship study of a library of 25 novel radioligands that aims to identify radiotracers with opt
233 neuroimaging has been limited by the lack of radioligands that are selective for noradrenergic neurot
234 dvance in positron emission tomography (PET) radioligands that bind to the translocator protein (TSPO
237 ely, a few notable successes in the targeted radioligand therapeutic space are changing this dynamic,
238 opportunity for a new and promising wave of radioligand therapies to significantly change the oncolo
239 rom 48 patients subjected to (177)Lu-labeled radioligand therapy ((177)Lu-DOTATOC, 26; (177)Lu-PSMA,
240 se were stratified to receive (90)Y-PSMA-617 radioligand therapy (mean, 3.2 GBq; range, 2.8-3.7 GBq);
241 te-specific membrane antigen (PSMA)-targeted radioligand therapy (PRLT) using (177)Lu-labeled PSMA-61
242 d molecular radiotherapy using PSMA-targeted radioligand therapy (PRLT) with (177)Lu-PSMA ligands.
243 te-specific membrane antigen (PSMA)-targeted radioligand therapy (PRLT), especially (177)Lu-PSMA-617.
244 e antigen (PSMA)-positive tumor volume after radioligand therapy (RLT) based on a pretherapeutic PET/
245 rostate-specific membrane antigen 617 (PSMA) radioligand therapy (RLT) in comparison with the establi
246 -motif chemokine receptor 4 (CXCR4)-directed radioligand therapy (RLT) in multiple myeloma and acute
249 te-specific membrane antigen (PSMA)-targeted radioligand therapy (RLT) is effective against prostate
250 617 is a promising new therapeutic agent for radioligand therapy (RLT) of patients with metastatic ca
251 Lu-prostate-specific membrane antigen (PSMA) radioligand therapy (RLT) using inhibitors of PSMA is a
252 might be used to overcome the limitations of radioligand therapy (RLT) with (177)Lu-prostate-specific
256 based PSMA ligands used for both imaging and radioligand therapy are the mainstays of the current suc
260 ed prostate-specific membrane antigen (PSMA) radioligand therapy using PSMA-617 and PSMA-I&T ligands
263 is an effective and promising candidate for radioligand therapy, with a favorable preliminary safety
264 ven the high level of safety of (177)Lu-PSMA radioligand therapy, with only minimal grade 3 and 4 tox
273 eceptor CB(2), in a Facade detergent enables radioligand thermostability assessments of this receptor
274 ding of a positron emission tomography (PET) radioligand to the vesicular monoamine transporter 2, (V
275 hy with the [(11)C]-(+)-PHNO and [(18)F]FPEB radioligands to quantify regional dopamine D(2/3) and me
277 R agonist positron emission tomography (PET) radioligand, to investigate endogenous opioid tone in AD
279 nd (S,S)-68 have differential effects on the radioligand used for the binding assay, with (R,R)-68 po
280 erocyclic positron emission tomography (PET) radioligands using the copper-mediated (18)F-fluorinatio
281 -bearing antibody and a tetrazine (Tz)-based radioligand via the rapid and bioorthogonal inverse elec
284 igands was enhanced; NET binding of only one radioligand was enhanced; SERT radioligand binding was m
286 modified with TCO, and a novel NOTA-PEG7-Tz radioligand was synthesized with the goal of improving o
287 , the binding of two structurally dissimilar radioligands was enhanced; NET binding of only one radio
289 n of (67)Ga-, (111)In-, and (177)Lu-NeoBOMB1 radioligands was studied in PC-3 cells at 37 degrees C,
291 sualized P2X7R in the monkey brain, and this radioligand will be further evaluated in a clinical sett
292 utetium-177 ((177)Lu)-PSMA-617 (LuPSMA) is a radioligand with high affinity for prostate specific mem
294 son's disease using 11C-BU99008 PET, a novel radioligand with high specificity and selectivity for im
295 orts to develop a suitable (18)F-labeled PET radioligand with improved characteristics for imaging th
296 f neuroinflammation; and (ii) 18F-AV-1451, a radioligand with increased binding to pathologically aff
298 or (H(1)R) antagonists were determined using radioligands with either slow (low k(off)) or fast (high
299 in vivo performance characteristics of both radioligands with the previously reported 3'-aza-2'-(18)