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Derek E. Brundish
Researcher at Novartis
Publications - 36
Citations - 954
Derek E. Brundish is an academic researcher from Novartis. The author has contributed to research in topics: Residue (chemistry) & Receptor. The author has an hindex of 12, co-authored 36 publications receiving 947 citations.
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Journal ArticleDOI
[3H]CGP 39653: a new N-methyl-D-aspartate antagonist radioligand with low nanomolar affinity in rat brain
Matthew A. Sills,Graham E. Fagg,Mario F. Pozza,Christof Angst,Derek E. Brundish,S D Hurt,E. J. Wilusz,Michael Williams +7 more
TL;DR: Results suggest that [3H]CGP 39653 selectively binds to the NMDA receptor as an antagonist with high affinity and is currently the ligand of choice for labeling theNMDA receptor.
Journal ArticleDOI
CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity
G.E. Fagg,H.-R. Olpe,Mario F. Pozza,J. Baud,Martin W. Steinmann,M. Schmutz,C. Portet,P. A. Baumann,K. Thedinga,Helmut Bittiger,H. Allgeier,Roland Heckendorn,Christof Angst,Derek E. Brundish,John Grey Dr Dingwall +14 more
TL;DR: CGP 37849 and CGP 39551 are potent and competitive NMDA receptor antagonists which show significant central effects following oral administration to animals and may find value as tools to elucidate the roles of NMDA receptors in brain function, and potentially as therapeutic agents for the treatment of neurological disorders such as epilepsy and ischaemic brain damage in man.
Journal ArticleDOI
CGS 8216: receptor binding characteristics of a potent benzodiazepine antagonist.
Andrew J. Czernik,Barbara Petrack,Helen J. Kalinsky,Stacy Psychoyos,William D. Cash,C Tsai,Roy K. Rinehart,Frank R. Granat,R. A. Lovell,Derek E. Brundish,R. Wade +10 more
TL;DR: 3H-CGS 8216 may be a useful ligand for probing the antagonist properties of the benzodiazepine receptor and is likely to exhibit interesting therapeutic effects.
Journal ArticleDOI
Specific binding of 3H-substance P to rat brain membranes.
Michael R. Hanley,Bengt E. B. Sandberg,Chi-Ming Lee,Leslie L. Iversen,Derek E. Brundish,R. Wade +5 more
TL;DR: The 3H-substance P binding sites are consistent with those expected for substance P receptors, and the rank order of potency of these substance P-related peptides agrees with that reported for their effects in depolarizing spinal cord neurones.
Journal ArticleDOI
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.
Derek E. Brundish,Bull A,Donovan,Joseph D. Fullerton,Sheila Garman,Judy Hayler,Diana Janus,Peter D. Kane,McDonnell M,Garrick Smith,Wakeford R,Christoph Walker,Graham Arton Howarth,William Hoyle,Mark C. Allen,John Ambler,K D Butler,Talbot +17 more
TL;DR: In animal models of both venous and arterial thrombosis, one inhibitor was shown to produce a dose-dependent inhibition of thrombus formation that in some situations was superior to that of MD-805.