Sally Anne Thompson
Affiliation: Merck Research Laboratories
- Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptorsSally Anne Thompson
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Essex, United Kingdom
Mol Pharmacol 61:861-9. 2002....
- Salicylidene salicylhydrazide, a selective inhibitor of beta 1-containing GABAA receptorsS A Thompson
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex
Br J Pharmacol 142:97-106. 2004..The importance of threonine 255 and isoleucine 308 within the beta1 subunit and the lack of interaction with a range of GABA(A) receptor modulators suggests that SCS is interacting at a previously unidentified site...
- 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptorAndrew Mitchinson
Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow CM20 2QR, UK
Bioorg Med Chem Lett 14:3441-4. 2004..2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands with functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimise this functional selectivity are described...
- Activity of chlormethiazole at human recombinant GABA(A) and NMDA receptorsMarcello Usala
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR
Br J Pharmacol 140:1045-50. 2003..IC50's were approximately 500 microm that likely exceed the therapeutic dose range for chlormethiazole, indicating that the primary mechanism of the compounds in vivo activity is via GABAA receptors...
- Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunitMichael G N Russell
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, U K
J Med Chem 48:1367-83. 2005..This was the first indication that selectivity in efficacy in the required direction could be achieved in this series...
- Evidence for an enhancement of excitatory transmission in adult CNS by Wnt signaling pathway modulationVahri Beaumont
The Neuroscience Research Centre, Merck Sharp and Dohme, Terlings Park, Harlow Essex CM20 2QR, UK
Mol Cell Neurosci 35:513-24. 2007..Our findings are consistent with a pre- and postsynaptic site of action, leading to both increased spontaneous and evoked neurotransmission that occurs in a transcription-independent fashion...