William Billard
Schering-Plough
26 Papers
1.1K Citations
William Billard is an academic researcher from Schering-Plough. The author has contributed to research in topics: Muscarinic acetylcholine receptor & Muscarinic acetylcholine receptor M2. The author has an hindex of 15, co-authored 26 publications.
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Papers
Characterization of the binding of 3H-SCH 23390, a selective D-1 receptor antagonist ligand, in rat striatum.
TL;DR: In the present study, the in vitro binding of 3H-SCH 23390 to specific striatal receptor sites has been characterized and saturable and stereospecific, and the results of both saturation and competition studies are consistent with the binding of this radioligand to a single striatal site.
575
•Journal Article
Identification of the primary muscarinic autoreceptor subtype in rat striatum as m2 through a correlation of in vivo microdialysis and in vitro receptor binding data.
TL;DR: The conclusion is that the muscarinic receptor mediating ACh release in rat striatum exhibits a pharmacological profile clearly consistent with it being of the m2 subtype.
109
•Journal Article
Pharmacology of SCH 34826, an orally active enkephalinase inhibitor analgesic.
TL;DR: Direct, naloxone-reversible analgesic effects of SCH 34826 were demonstrated in the mouse low temperature hot-plate test and the mouse acetic acid-induced writhing test, and no respiratory or gastrointestinal side effects of any consequence were noted at doses up to 100 times those active in the D-Ala2-Met5-enkephalinamide potentiation test.
102
Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.
Yuguang Wang,Samuel Chackalamannil,Zhiyong Hu,John W. Clader,William J. Greenlee,William Billard,Herbert Binch,Gordon Crosby,Vilma Ruperto,Ruth A. Duffy,Robert D. McQuade,Jean E. Lachowicz +11 more
TL;DR: A series of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes showed pronounced enhancement of brain acetylcholine release after oral administration in the rat microdialysis assay.
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Muscarinic agonists and antagonists in the treatment of Alzheimer's disease.
William J. Greenlee,John W. Clader,Theodros Asberom,Stuart W. McCombie,Jennifer Ford,Henry Guzik,Joseph A. Kozlowski,Shengjian Li,C Liu,Derek B. Lowe,Vice Susan F,H Zhao,Gouwei Zhou,William Billard,Herbert Binch,R Crosby,Ruth A. Duffy,Jean E. Lachowicz,Vicki L. Coffin,Robert W. Watkins,Vilma Ruperto,Catherine D. Strader,Lisa A. Taylor,Kathleen Cox +23 more
TL;DR: Exploration of a series of piperidinylpiperidines has yielded the potent and selective M2 antagonist SCH-217443, which has excellent bioavailability in rats and dogs and shows activity in a rat model of cognition.
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