Results 51 to 60 of about 2,283,209 (217)

Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay

Heliyon, 2021
Estradiol is a steroid hormone that works as an agonist estrogen receptor (ER). This compound is widely used as a ligand and bind specifically to the ERα.
Isti Daruwati, Abednego Kristande Gwiharto, Ahmad Kurniawan, Isa Mahendra, Tri Hanggono Achmad, Mukh Syaifudin, Muchtaridi Muchtaridi   +6 more
doaj   +1 more source

The integrated Lei‐CNS PBPK‐PD model effectively predicts clozapine brain disposition and D2 receptor occupancy in humans

British Journal of Clinical Pharmacology, EarlyView.
Aim Clozapine, used for treatment‐resistant schizophrenia, has a narrow therapeutic window and highly variable plasma pharmacokinetics (PK), necessitating careful monitoring. Direct measurement of unbound brain PK in humans is unethical. To develop a physiologically based pharmacokinetic–pharmacodynamic (PBPK‐PD) model to predict clozapine brain ...
Mengxu Zhang, Thomas I. F. H. Cremers, Vivi Rottschäfer, Elizabeth C. M. de Lange   +3 more
wiley   +1 more source

ω-Conotoxin GVIA Mimetics that Bind and Inhibit Neuronal Cav2.2 Ion Channels

Marine Drugs, 2012
The neuronal voltage-gated N-type calcium channel (Cav2.2) is a validated target for the treatment of neuropathic pain. A small library of anthranilamide-derived ω-Conotoxin GVIA mimetics bearing the diphenylmethylpiperazine moiety were prepared and ...
Peter J. Duggan, Aijun Yang, Irina Vetter, Jeffrey R. McArthur, Richard J. Lewis, Kellie L. Tuck, Jonathan B. Baell, Charlotte Elisabet Tranberg   +7 more
doaj   +1 more source

A Cell-Based Radioligand Binding Assay for Farnesyl: Protein Transferase Inhibitors [PDF]

SLAS Discovery, 2003
Farnesyl:protein transferase (FPTase) catalyzes the covalent addition of the isoprenyl moiety of farnesylpyrophosphate to the C-terminus of the Ras oncoprotein and other cellular proteins. Inhibitors of FPTase (FTIs) have been developed as potential anticancer agents, and several compounds have been evaluated in clinical trials.
Robert B, Lobell, Joseph P, Davide, Nancy E, Kohl, H Donald, Burns, Wai-Si, Eng, Raymond E, Gibson   +5 more
openaire   +2 more sources

Competition radioligand binding affinity values.

, 2019
Competition radioligand binding affinity values.
Daniel Womer (6807767), John M. Streicher (503153), Keith M. Olson (1484329), David I. Duron (6807764), Ryan Fell (6807770)   +4 more
core   +1 more source

Histamine and the mechanisms of nausea and vomiting: Translating the uncertain pharmacology of cyclizine

British Journal of Clinical Pharmacology, EarlyView.
Abstract Cyclizine is a long‐established, short‐acting drug, registered for preventing motion sickness, post‐operative nausea and vomiting (PONV) and ‘vomiting of known cause’. The latter is not defined but may include pregnancy and patients receiving palliative care, historically accepted without large, controlled trials.
Gareth J. Sanger, Paul L. R. Andrews
wiley   +1 more source

Towards the Development of a Targeted Albumin-Binding Radioligand for Theranostic Applications: Synthesis, Radiolabelling and Preliminary In Vivo Studies [PDF]

, 2020
GluCAB is a newly synthesised macrocyclic radioligand designed to bind in vivo to albumin (HSA) for the purpose of development as a dual-targeting oncological theranostic agent.
Iqbal, Parker, Zoltan, Szucs, Thomas, Ebenhan, Jan Rijn, Zeevaart, Roger, Hunter, Cathryn H.S., Driver   +5 more
core   +2 more sources

Analysis of variation in L‐365,260 competition curves in radioligand binding assays [PDF]

British Journal of Pharmacology, 1996
. For several years, we have used the cholecystokinin (CCK)B/gastrin receptor selective antagonist, L‐365,260, as a reference compound in a variety of studies in CCKB/gastrin receptor radioligand binding assays. Here, we have analysed the competition curve data sets obtained between L‐365,260 and [125I]‐BH‐CCK8S in guinea‐pig gastric gland and mouse ...
E A, Harper, S P, Roberts, N P, Shankley, J W, Black   +3 more
openaire   +2 more sources

Translational development of crisugabalin for neuropathic pain

British Journal of Clinical Pharmacology, EarlyView.
Abstract Crisugabalin (HSK16149) is a next‐generation α2δ ligand developed to preserve the mechanistic rationale of gabapentinoids while refining target engagement and exposure‐related tolerability constraints. We performed a translational review of molecular/structural studies, in vivo pharmacology and behavioural safety assessments, phase I clinical ...
Rafael Batista João, Jilly Octoria Tagore Chan, Luísa Mendes Araújo, André Batista João, Raquel Mattos Filgueiras, Paulo César Ragazzo   +5 more
wiley   +1 more source

Miniaturized Bioaffinity Assessment Coupled to Mass Spectrometry for Guided Purification of Bioactives from Toad and Cone Snail

Biology, 2014
A nano-flow high-resolution screening platform, featuring a parallel chip-based microfluidic bioassay and mass spectrometry coupled to nano-liquid chromatography, was applied to screen animal venoms for nicotinic acetylcholine receptor like (nAChR ...
Ferry Heus, Reka A. Otvos, Ruud L. E. G. Aspers, Rene van Elk, Jenny I. Halff, Andreas W. Ehlers, Sébastien Dutertre, Richard J. Lewis, Sybren Wijmenga, August B. Smit, Wilfried M. A. Niessen, Jeroen Kool   +11 more
doaj   +1 more source