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Radioactive biochemical substance used for diagnosis or for study of receptor systems
A radioligand is a microscopic particle which consists of a therapeutic radioactive isotope and the cell-targeting compound — the ligand. The ligand is
Radioligand
Radioligand used for diagnostic purposes
PET radiotracer is a type of radioligand that is used for the diagnostic purposes via positron emission tomography imaging technique. PET is a functional
PET_radiotracer
System of measuring the instability of a protein under varying conditions
radioligand concentration is high enough to saturate the protein. Denatured protein is unable to bind the radioligand and the protein and radioligand
Thermal_shift_assay
GABA receptor antagonist drug and benzodiazepine antidote
with the radioactive isotope carbon-11, flumazenil may be used as a radioligand in neuroimaging with positron emission tomography to visualize the distribution
Flumazenil
Type of radiation therapy
(such as with Lutathera and Pluvicto), the technique is also known as radioligand therapy. Iodine-131 (131I) is the most common RNT worldwide and uses
Radionuclide_therapy
Biochemical analysis procedure
for a radioligand (per mole) are referred to as the specific activity (SA), which is measured in Ci/mmol. The actual concentration of a radioligand is determined
Ligand_binding_assay
Psychoactive substance found in plants in the family Apocynaceae
"Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies". Brain Research. 571 (2): 242–247. doi:10.1016/0006-8993(92)90661-r
Ibogaine
Medical intervention
Auger therapy Other names AT Specialty Radioligand therapy
Auger_therapy
Chemical compound
Labeled with carbon-11 — a radioactive isotope — it has been used as a radioligand in neuroimaging with positron emission tomography (PET) since around
DASB
Drug
is a synthetic compound derived from pindolol, primarily used as a radioligand in pharmacological research. It functions as a non-selective β-adrenoceptor
Iodocyanopindolol
Pharmaceutical compound
can be radiolabeled with the radioisotope fluorine-18 and used as a radioligand with positron emission tomography (PET). Several research studies have
Setoperone
Antispasmodic agent
DRUGMATRIX: Muscarinic M1 radioligand binding (Ligand: [3H] N-Methylscopolamine) - PubChem". "AID 625154 - DRUGMATRIX: Muscarinic M4 radioligand binding (Ligand:
Dicycloverine
Antidepressant medication
Kennett G, et al. (2004). "Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors". Naunyn-Schmiedeberg's
Trazodone
Tricyclic antidepressant
5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling". Molecular
Amitriptyline
Substance that forms a complex with a biomolecule
receptor to adapt, and thus accept or reject each other as partners. Radioligands are radioisotope labeled compounds used in vivo as tracers in PET studies
Ligand_(biochemistry)
Chelate of Lu-177 with dotatate, a peptide derivative bound to a DOTA molecule
a first-in-class medication. In September 2026, the FDA approved the radioligand equivalent Bexlutry. In the US, 177Lu dotatate is indicated for the treatment
Lutetium (177Lu) oxodotreotide
Lutetium_(177Lu)_oxodotreotide
Equation used in pharmacology
In pharmacology, Schild regression analysis, based upon the Schild equation, both named for Heinz Otto Schild, are tools for studying the effects of agonists
Schild_equation
Nuclear medicine tomographic imaging technique
a marker radioisotope is attached to a specific ligand to create a radioligand, whose properties bind it to certain types of tissues. This marriage
Single-photon emission computed tomography
Single-photon_emission_computed_tomography
Chemical compound
(serotonin) 2A receptor). Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain, i.e., studies
Altanserin
Half maximal inhibitory concentration
competitive.[citation needed] In this type of assay, a single concentration of radioligand (usually an agonist) is used in every assay tube. The ligand is used
IC50
Chemical compound
relationship. Labeled with the radioisotope carbon-11 it is used as a radioligand in positron emission tomography (PET) studies to determine neuroreceptor
WAY-100635
Chemical compound
as a medication, moxestrol has been used in scientific research as a radioligand of the estrogen receptor. Moxestrol is or has been used in the treatment
Moxestrol
Antihistamine used to treat allergies
Nix WB, Timmerman H, Leurs R (July 2002). "A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors". The Journal of
Chlorphenamine
Chemical compound
clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (123I) are now available for this application. GBR-12935
GBR-12935
Chemical compound
classical full length form targeted by conventional opioid drugs. In the Radioligand binding assay it has shown to have affinities of 0.11nM at the MOR, 0
IBNtxA
Chemical compound
(December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology
Rauwolscine
Medication used to treat anxiety disorders
D (June 1988). "Molecular pharmacology of 5-HT1D recognition sites: radioligand binding studies in human, pig and calf brain membranes". Naunyn-Schmiedeberg's
Buspirone
Class of CNS depressant drugs
the utilization of a dual PET CT scanner to track the binding of the radioligand florbetapir to beta-amyloid provides stronger neuroimaging data with
Benzodiazepine
Chemical compound
agonist of the 5-HT1A receptor (Ki = 1.36 nM) that has been used as a radioligand in PET studies. It possesses modest affinity for the 5-HT7 (Ki = 9.1
F-11461
Chemical compound
an opioid drug of the benzomorphan group, which was developed as a radioligand for the purpose of labeling opioid receptors during PET scans (with 18F)
Fluorophen
Type of receptor ligand or drug that blocks a biological response
experimentally using Schild regression or for competitive antagonists in radioligand binding studies using the Cheng–Prusoff equation. Schild regression can
Receptor_antagonist
Chemical compound
PRX-03140 is a highly selective and potent (Ki = 14.3 nM) 5-HT4R agonist in radioligand binding assays with more than 100-fold difference in affinities compared
PRX-03140
Atypical antipsychotic medication
dopamine D2 or D4 receptor varies with the affinity of the competing radioligand". European Journal of Pharmacology. 291 (2): 59–66. doi:10.1016/0922-4106(95)90125-6
Olanzapine
Radiopharmaceutical medication
cancer (mCRPC). Lutetium (177Lu) vipivotide tetraxetan is a targeted radioligand therapy. The most common adverse reactions include fatigue, dry mouth
Lutetium (177Lu) vipivotide tetraxetan
Lutetium_(177Lu)_vipivotide_tetraxetan
Chemical compound
elimination, and activation of specific proto-oncogenes. The 35S labelled radioligand of the compound, 35SGTPγS, is used in autoradiography and G-protein binding
GTPgammaS
Chemical compound
a radioligand in positron emission tomography (PET) studies. The [11C]-(+)-McN5652 enantiomer binds to the serotonin transporter. The radioligand is
McN5652
Kappa opioid receptor radioligand
highly selective κ-opioid receptor (KOR) agonist primarily employed as a radioligand in positron emission tomography (PET) neuroimaging research. When radiolabeled
GR-103545
Chemical compound
serotonin-1A receptor. Labeled with fluorine-18 it has been used as a radioligand with positron emission tomography. It has, e.g., been used to examine
MPPF
Dopamine receptor agonist compound
antagonist at D2 receptors. Radiolabelled 11C-5-OH-DPAT is used as an agonist radioligand for mapping the distribution and function of D2 and D3 receptors in the
5-OH-DPAT
Mood disorder
tentative reports of increased VMAT2 activity, measured via PET scans of radioligand binding, suggests a role of dopamine in mania. Decreased cerebrospinal
Mania
Antidepressant
D (June 1988). "Molecular pharmacology of 5-HT1D recognition sites: radioligand binding studies in human, pig and calf brain membranes". Naunyn-Schmiedeberg's
Mianserin
Medication used for migraines & cluster headaches
logarithm of the molar concentration of these compounds at which 50% of the radioligand is displaced) and pKi (negative logarithm of the molar concentration
Sumatriptan
has been assessed with positron emission tomography and the WAY-100635 radioligand, with a study reporting no apparent influence from the SNP. The SNP has
Rs6295
Pharmaceutical compound
labelling of MADAM in two different positions: a highly selective PET radioligand for the serotonin transporter". Journal of Labelled Compounds and Radiopharmaceuticals
MADAM
Genus of cnidarians
S2CID 29262166. Venturini G (1987). "The hydra GSH receptor. Pharmacological and radioligand binding studies". Comparative Biochemistry and Physiology. C, Comparative
Hydra_(genus)
inhibition and kinetics, isothermal titration calorimetry, NMR, and radioligand and competition assays. BindingDB includes data extracted from the scientific
BindingDB
Chemical compound
5-HT2A receptor was 4.9 nM with DOI as the radioligand and 140–191 nM with ketanserin as the radioligand. Its EC50Tooltip half-maximal effective concentration
Bretisilocin
Drug that produces a dream-like state of consciousness
"Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies". Brain Res. 571 (2): 242–247. doi:10.1016/0006-8993(92)90661-r
Oneirogen
Medication used for the treatment of migraine headaches
logarithm of the molar concentration of these compounds at which 50% of the radioligand is displaced) and pKi (negative logarithm of the molar concentration
Rizatriptan
Pharmaceutical compound
K, et al. (July 2008). "[11C]AZ10419369: a selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in
AZ10419369
Pharmaceutical compound
([18F]-norchloro-fluoro-homoepibatidine) is a fluorine-18 (18F) labeled radiotracer and radioligand for positron emission tomography (PET) imaging, developed as a high-affinity
Flubatine
Chemical compound
carbon-11 and fluorine-18, are used as PET radioligands for examining VMAT2. [11C]DTBZ as a PET radioligand with affinity for VMAT2 was developed in the
Dihydrotetrabenazine
Chemical compound in the ergot family of alkaloids
logarithm of the molar concentration of these compounds at which 50% of the radioligand is displaced) and pKi (negative logarithm of the molar concentration
Ergotamine
Chemical compound
The affinity towards adenosine A3 subtype was measured against the radioligand PSB-11. Ozola V, Thorand M, Diekmann M, Qurishi R, Schumacher B, Jacobson
PSB-10
Radiograph made by recording radiation emitted by samples on photographic plates
radiolabeled drug towards the receptor. For in vitro autoradiography, radioligand was directly applying on frozen tissue sections without administration
Autoradiograph
Chemical compound
WB; Timmerman, H; Leurs, R (July 2002). "A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors". The Journal of
Phenylaminotetralin
Species of flowering plant in the mint family
Perovskia atriplicifolia and their in vitro displacement of the respective radioligands for human opioid and cannabinoid receptors", Journal of Natural Products
Salvia_yangii
Medication used for high blood pressure and ADHD
Porter AC, Neubig RR (December 1994). "The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C
Guanfacine
Set of techniques to measure and visualize aspects of the nervous system
after the introduction of CAT in the early 1980s, the development of radioligands allowed single-photon emission computed tomography (SPECT) and positron
Neuroimaging
Chemical compound
devised with the same radioisotope. As with all radioactive 18F-labeled radioligands, the fluorine-18 must be made initially as the fluoride anion in a cyclotron
Fluorodeoxyglucose_(18F)
Chemical compound
receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays". European Journal of Pharmacology
Cyprodime
Chemical compound
that tritium-labeled nisoxetine (3H-nisoxetine, 3H-NIS) is a useful radioligand for labeling norepinephrine uptake sites in vitro, which nisoxetine and
Nisoxetine
Public domain database of binding affinities for drugs and other chemical compounds
which measure the potency of a compound in inhibiting the binding of a radioligand to a specific target, such as a receptor, neurotransmitter transporter
Ki_Database
Mammalian protein found in humans
using radioligands called DASB and DAPP; the first such studies on the human brain were reported in 2000. DASB and DAPP are not the only radioligands for
Serotonin_transporter
Pharmaceutical compound
[3H]-ketanserin from rat cortical homogenate are shown. [...] TABLE 6. Radioligand binding data for N-methyl-N-isopropyl lysergamides: [3H]-ketanserin displacement
IPLA
Class of opioid receptors found in humans
receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays". European Journal of Pharmacology
Mu-opioid_receptor
Metastable nuclear isomer of technetium-99
coregistration technology to produce SPECT/CT scans. These employ the same radioligands and have the same uses as SPECT scanning, but are able to provide even
Technetium-99m
Electrophysiological method to record electrical activity of the brain
such as metal-containing pacemakers EEG does not involve exposure to radioligands, unlike positron emission tomography. ERP studies can be conducted with
Electroencephalography
Synthetic hallucinogen
(PET) in Copenhagen. Being the first 5-HT2A receptor full agonist PET radioligand, [11C]CIMBI-5 shows promise as a more functional marker of these receptors
25I-NBOMe
Class of pharmaceutical drugs
logarithm of the molar concentration of these compounds at which 50% of the radioligand is displaced) and pKi (negative logarithm of the molar concentration
Triptan
Protein-coding gene in the species Homo sapiens
BQZ-12 VU-0090157 VU-0029767 VU0467319 [3H]PT-1284- M1-selective PAM Radioligand Atropine Diphenhydramine Scopolamine Tramadol Dicycloverine Fluoxetine
Muscarinic acetylcholine receptor M1
Muscarinic_acetylcholine_receptor_M1
Medical imaging technique
and ultrasound. SPECT is an imaging technique similar to PET that uses radioligands to detect molecules in the body. PET scanning with the radiotracer
Positron_emission_tomography
Pharmaceutical compound
affinity for the human serotonin 5-HT2A and 5-HT2C receptors with agonist radioligands (Ki = 13–16 nM and 4–6 nM, respectively). These affinities were 20- to
2C-B-5-hemiFLY-α6
Antidepressant
study were due to methodological differences, in particular the use of radioligand binding in isolated membranes (KD) to study interactions as opposed to
Trimipramine
Radiopharmaceutical precursor
chelates the radioactive isotope lutetium-177, a β-emitter used in targeted radioligand therapy. In Ac-PSMA-617, it binds actinium-225, an α-emitter used in
Vipivotide_tetraxetan
Antihypertensive agent
epithelialization. With tritium (3H) radioactively labeled ketanserin is used as a radioligand for serotonin 5-HT2 receptors, e.g. in receptor binding assays and autoradiography
Ketanserin
Combination of cancer diagnosis and treatment
tissues. For example, PRRT based on Lutetium-177 combinations (known as radioligands) has emerged as a treatment option for inoperable metastatic neuroendocrine
Theranostics
et al. (August 2004). "Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors". Naunyn-Schmiedeberg's
List of miscellaneous 5-HT2A receptor agonists
List_of_miscellaneous_5-HT2A_receptor_agonists
Class of cell surface receptors
and dopamine synthesis in rodent brain. Subsequent pharmacological and radioligand-binding studies demonstrated that these so-called sigma-3 sites correspond
Sigma_receptor
Chemical compound
endonmorphin-1 was synthesized, the range of their bioactivities were measured by radioligand binding assay in order to conclude its potency as an opioid. Endomorphin-1
Endomorphin-1
Drug that binds to but does not activate muscarinic cholinergic receptors
14 August 2017. Kalkman HO, Subramanian N, Hoyer D (2001). "Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine
Muscarinic_antagonist
Pharmaceutical compound
potency beyond n-propyl.[163] Yet later work using [3 H]ketanserin as a radioligand for 5-HT2 receptors in rat brain homogenate revealed significantly increased
2,5-Dimethoxy-4-benzylamphetamine
2,5-Dimethoxy-4-benzylamphetamine
Protein-coding gene in the species Homo sapiens
other receptors. SB-207,145 radiolabeled with carbon-11 is used as a radioligand for 5-HT4 in positron emission tomography studies in pigs and humans
5-HT4_receptor
Tumors of the endocrine and nervous systems
(RIT) in which a peptide or hormone conjugated to a radionuclide or radioligand is given intravenously. The peptide or hormone needs to have previously
Neuroendocrine_tumor
Pharmaceutical compound
(June 2001). "Pharmacological evaluation of (+)-2- [123I]A-69024: a radioligand for in vivo studies of dopamine D1 receptors". Life Sciences. 69 (6):
A-69024
Chemical compound
at CB2 as the active (R) enantiomer. It was developed as a selective radioligand for the cannabinoid receptors and has been used as its 131I derivative
AM-2233
Glutamate receptor and ion channel protein found in nerve cells
PMID 10785653. Gibson DA, Harris BR, Rogers DT, Littleton JM (October 2002). "Radioligand binding studies reveal agmatine is a more selective antagonist for a
NMDA_receptor
Chemical compound
side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands". Bioorganic & Medicinal Chemistry Letters. 11 (8): 1045–1047. doi:10
RU-58841
Pharmaceutical compound
human KOR, with an affinity (Ki) of 0.9 nM or 87.3 nM depending on the radioligand and an EC50Tooltip half-maximal effective concentration of 0.8 nM. In
GM-3009
Medication used for alcohol intoxication
that Metadoxine affects the Serotonin receptor family; in an agonist radioligand assay, it was shown that Metadoxine binds to the 5HT-2B receptor, pertaining
Metadoxine
(October 1997). "Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin". Neuropharmacology. 36 (10): 1439–46. doi:10
Urocortin
Chemical compound
medication, promegestone has been widely used in scientific research as a radioligand of the progesterone receptor. Promegestone is used in menopausal hormone
Promegestone
Mammalian protein found in humans
(October 1997). "Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin". Neuropharmacology. 36 (10): 1439–1446. doi:10
Corticotropin-releasing hormone
Corticotropin-releasing_hormone
Chemical compound
emission tomography (PET) in Copenhagen. As a 5-HT2A receptor agonist PET radioligand, [11C]Cimbi-36 was hypothesized to provide a more functional marker of
25B-NBOMe
Class of chemical compounds
PMC 6893898. PMID 31849671. Harms A, Ulmer E, Kovar K. Synthesis and 5-HT2A radioligand receptor binding assays of DOMCl and DOMOM, two novel 5-HT2A receptor
DOx
Chemical compound
"Synthesis and biologic evaluation of a novel serotonin 5-HT1A receptor radioligand, 18F-labeled mefway, in rodents and imaging by PET in a nonhuman primate"
Mefway_(18F)
Chemical compound
logarithm of the molar concentration of these compounds at which 50% of the radioligand is displaced) and pKi (negative logarithm of the molar concentration
Naratriptan
Subtype of serotonin receptor
receptors by Gaddum and Picarelli. In the era before molecular cloning, when radioligand binding and displacement was the only major tool, spiperone and LSD were
5-HT2A_receptor
Serotonin receptor protein distributed in the cerebrum and raphe nucleus
brain may be imaged with the positron emission tomography using the radioligand [11C] WAY-100,635. For example, one study has found increased 5-HT1A
5-HT1A_receptor
Class of transmembrane proteins
receptor 5-HT1P has been distinguished on the basis of functional and radioligand binding studies, its existence has never been definitely affirmed or
5-HT_receptor
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