Tracazolate reveals a novel type of allosteric interaction with recombinant γ-aminobutyric acidA receptors

SA Thompson, PB Wingrove, L Connelly… - Molecular …, 2002 - ASPET
Tracazolate, a pyrazolopyridine, is an anxiolytic known to interact with γ-aminobutyric acid (GABA)
A receptors, adenosine receptors, and phosphodiesterases. Its anxiolytic effect is …

Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABAA Receptor Agonists at the α3 Subunit

…, AJ Macaulay, D Thomas, SA Thompson… - Journal of medicinal …, 2005 - ACS Publications
We have previously identified the 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazine
(1) as a potent partial agonist for the α 3 receptor subtype with 5-fold selectivity in …

Mutation at the putative GABAA ion‐channel gate reveals changes in allosteric modulation

SA Thompson, MZ Smith, PB Wingrove… - British journal of …, 1999 - Wiley Online Library
We have mutated a conserved leucine in the putative membrane‐spanning domain to
serine in human GABA A β2 and investigated the actions of a number of GABA A agonists, …

Mechanism of action of general anaesthetics—new information from molecular pharmacology

SA Thompson, K Wafford - Current opinion in pharmacology, 2001 - Elsevier
Major progress in our understanding of the mechanisms of anaesthesia has been made
during the past year. Several key advances in defining very specific sites of action on ligand-…

Evidence for an enhancement of excitatory transmission in adult CNS by Wnt signaling pathway modulation

V Beaumont, SA Thompson, F Choudhry… - Molecular and Cellular …, 2007 - Elsevier
The role for Wnt signaling modulation during synaptogenesis, neurogenesis and cell fate
specification have been well characterized. In contrast, the roles for Wnt signaling pathways in …

2, 5-Dihydropyrazolo [4, 3-c] pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor

…, R Narquizian, A Smith, LJ Street, SA Thompson… - Bioorganic & medicinal …, 2004 - Elsevier
2, 5-Dihydropyrazolo [4, 3-c] pyridin-3-ones are GABAA receptor benzodiazepine binding
site ligands with functional selectivity for the α3 subtype over the α1 subtype. SAR studies to …

Functional characteristics of recombinant human GABAA receptors containing the ϵ-subunit

SA Thompson, TP Bonnert, PJ Whiting, KA Wafford - Toxicology letters, 1998 - Elsevier
(1) This paper further examines the functional characteristics of recombinant human GABA A
receptors containing the ϵ-subunit expressed in Xenopus oocytes. (2) α1β1ϵ receptors are …

Antagonism of human CC‐chemokine receptor 4 can be achieved through three distinct binding sites on the receptor

…, C Weston, G Nalesso, SA Thompson… - Pharmacology …, 2013 - Wiley Online Library
Chemokine receptor antagonists appear to access two distinct binding sites on different
members of this receptor family. One class of CCR 4 antagonists has been suggested to bind to …

Activity of chlormethiazole at human recombinant GABAA and NMDA receptors

M Usala, SA Thompson, PJ Whiting… - British journal of …, 2003 - Wiley Online Library
Investigation into the modulatory effects of chlormethiazole at human recombinant γ‐aminobutyric
acid A receptor (GABA A ) and N‐methyl‐D‐aspartate (NMDA) receptors was …

Effect of the TRPV1 antagonist SB‐705498 on the nasal parasympathetic reflex response in the ovalbumin sensitized guinea pig

…, P Saklatvala, SA Thompson… - British Journal of …, 2013 - Wiley Online Library
Background and Purpose Nasal sensory nerves play an important role in symptoms associated
with rhinitis triggered by environmental stimuli. Here, we propose that TRPV1 is pivotal in …