Results 71 to 80 of about 3,259,253 (212)

Radioligand Binding to Nanodisc-Reconstituted Membrane Transporters Assessed by the Scintillation Proximity Assay

, 2016
The scintillation proximity assay is a powerful technique for measuring radioligand binding to membrane transporters and has become an integral part of high-throughput drug discovery screening efforts. Here we adapt the method for use with purified LeuT,
Mahmoud L. Nasr (1842112), Satinder K. Singh (1332018)   +1 more
core   +1 more source

Positive modulation of glucagon‐like peptide 1 (GLP‐1) receptor by endogenous haemorphins with implications in glucose metabolism and diabetes

British Journal of Pharmacology, EarlyView.
Haemorphins act on GLP‐1 receptor (GLP‐1R) activity and signalling in a positive allosteric manner. This leads to potentiated GLP‐1‐mediated activity and signalling, as well as insulin synthesis, which may have implications for glucose metabolism and, thereby, diabetes and obesity. (The graph was created in BioRender.com).
Farheen Badrealam Khan, Rwdah Mohamed Alameri, Yasir S. Raouf, Damien Maurel, Naiem Ahmad Wani, Anatoliy Shmygol, Irfa Anwar, Heng B. See, Elizabeth K. M. Johnstone, Elodie Dupuis, Eric Trinquet, Kevin D. G. Pfleger, Emilia Oueis, Mohammed Akli Ayoub   +13 more
wiley   +1 more source

A Robust Assay for Dexamethasone in Plasma Using a Heterologous 125I Radioligand and a Magnetizable Solid-Phase Antiserum

, 1990
An assay using an antiserum raised against a dexamethasone 21-hemisuccinate conjugate and the heterologous radioligand dexamethasone 21-(carboxymethyl) ether was developed, validated, and used to study the pharmacokinetics of this steroid for 12 h ...
Cook, Nigel N.J., Read, Graham G.F., Lejeune-Lenain, C., Riad-Fahmy, Diana   +3 more
core   +1 more source

Distribution and target engagement of peripherally administered fremanezumab in the cerebrospinal fluid of healthy volunteers

Headache: The Journal of Head and Face Pain, EarlyView.
Abstract Objectives/Background Our objective was to describe the distribution of fremanezumab to the cerebrospinal fluid (CSF) in healthy volunteers, and investigate its engagement and stabilization of its target, calcitonin gene‐related peptide (CGRP). Fremanezumab is a CGRP‐targeting monoclonal antibody approved for migraine prevention.
Jacki Rorabaugh, Edward Hellriegel, Juline Bryson, Ryan Tiver, Hang Zeng, Xiaofeng Lu, Steve Barash, Giulia Ghibellini, Olga Szilagyi, Ignacio Echenique, Andrew H. Ahn, Peter J. Goadsby, Laura Rabinovich‐Guilatt   +12 more
wiley   +1 more source

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

Epigenetic Dysregulation of Somatostatin Receptors (SSTR) 1–5 and Therapeutic Implications in Neuroendocrine and Non‐Neuroendocrine Malignancies

International Journal of Cancer, Volume 159, Issue 11, Page 2633-2652, 1 December 2026.
ABSTRACT Somatostatin receptors (SSTR) mediate the antiproliferative, antisecretory, and proapoptotic effects of somatostatin and its synthetic analogs. Their surface expression on neuroendocrine tumor (NET) cells is required for somatostatin analog therapy and radiopharmaceutical therapy (RPT).
Neeraj Kumari, Pablo Hoffmann, Laura Reichl, Maximilian Schmutz, Nina Fischer, Thi Tuong Vi Dang, Fulvia Ferrazzi, Pascal Johann, Michaela Kuhlen, Constantin Lapa, Rainer Claus   +10 more
wiley   +1 more source

Correction to Radioligand Binding to Nanodisc-Reconstituted Membrane Transporters Assessed by the Scintillation Proximity Assay

, 2016
Correction to Radioligand Binding to Nanodisc-Reconstituted Membrane Transporters Assessed by the Scintillation Proximity ...
Mahmoud L. Nasr (1842112), Satinder K. Singh (1332018)   +1 more
core   +1 more source

Characterization of the Lysophosphatidic Acid Receptor 5 Antagonist RLPA‐76 as a Novel Analgesic in Male Rats and Mice

Pharmacology Research &Perspectives, Volume 14, Issue 6, December 2026.
ABSTRACT Clinically used analgesics such as gabapentinoids and opioids have limited efficacy and adverse effects like abuse liability, and there is a dire need for novel analgesics with improved safety profiles. Since lysophosphatidic acid can induce neuropathic pain in rodents, LPA receptor antagonists have been investigated as potential analgesics ...
Kristen L. Woodhouse, Maowei Wang, Sai Ganesh Balaji Venkata Anupindi, Olatunbosun Adeoke, Dehui Zhang, Yanan Zhang, Jun‐Xu Li   +6 more
wiley   +1 more source

NMDA receptor subunit‐dependent analysis of radiprodil inhibition in neonatal male rat substantia nigra dopaminergic neurons

British Journal of Pharmacology, Volume 183, Issue 23, Page 6767-6786, December 2026.
Abstract Background and Purpose Radiprodil is a GluN2B subunit selective NMDA receptor negative allosteric modulator which is currently under clinical investigation as a possible anti‐epileptic drug for paediatric use. Our goal was to investigate the inhibition of dopaminergic neuron NMDA responses by radiprodil.
Bangyuan Liu, Alasdair J. Gibb
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