V
Vilma Ruperto
Researcher at Schering-Plough
Publications - 25
Citations - 1051
Vilma Ruperto is an academic researcher from Schering-Plough. The author has contributed to research in topics: Muscarinic acetylcholine receptor M2 & Muscarinic acetylcholine receptor. The author has an hindex of 13, co-authored 25 publications receiving 1032 citations.
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Journal ArticleDOI
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.
Journal ArticleDOI
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.
Journal ArticleDOI
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.
TL;DR: Structural-activity relationship studies support the existence of a hydrophobic pocket in the receptor where the piperidine ring of dihydrohimbacine binds.
Journal ArticleDOI
Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.
Yuguang Wang,Samuel Chackalamannil,Wei Chang,William J. Greenlee,Vilma Ruperto,Ruth A. Duffy,Robert D. McQuade,Jean E. Lachowicz +7 more
TL;DR: Novel, selective M2 muscarinic antagonists, which replace the metabolically labile styrenyl moiety of the prototypical M2 antagonist 1 with an ether linkage, were synthesized and showed high selectivity against M1, M3, and M5 receptors.