Danette Pascarella
Merck & Co.
7 Papers
Danette Pascarella is an academic researcher from Merck & Co.. The author has contributed to research in topics: Muscarinic acetylcholine receptor M1 & Muscarinic acetylcholine receptor M3. The author has an hindex of 7, co-authored 7 publications.
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Papers
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation
Lei Ma,Matthew A. Seager,Marion Wittmann,Marlene A. Jacobson,Denise J. Bickel,Maryann Burno,K. H. Jones,Valerie Kuzmick Graufelds,Guangping Xu,Michelle Pearson,Alexander McCampbell,Renee C. Gaspar,Paul J. Shughrue,Andrew Danziger,Christopher P. Regan,Rose Flick,Danette Pascarella,Susan L. Garson,Scott M. Doran,Constantine Kreatsoulas,Lone Veng,Craig W. Lindsley,William D. Shipe,Scott D. Kuduk,Cyrille Sur,Gene G. Kinney,Guy R. Seabrook,William J. Ray +27 more
TL;DR: Benzyl quinolone carboxylic acid exploits an allosteric potentiation mechanism to provide selectivity for the M1 receptor and represents a promising therapeutic strategy for cognitive disorders.
281
The Effects of Deleting the Mouse Neurotensin Receptor NTR1 on Central and Peripheral Responses to Neurotensin
Douglas J. Pettibone,J. Fred Hess,Patricia J. Hey,Marlene A. Jacobson,Michael Leviten,E V Lis,Pierre Mallorga,Danette Pascarella,Melissa A. Snyder,Jacinta B. Williams,Zhizhen Zeng +10 more
TL;DR: Data indicate that NTR1 mediates several of the central and peripheral effects of NT, and NT-2 administration impaired rotarod performance in wild-type mice, but had no effect on motor coordination in knockout mice.
134
The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.
Tim Sparey,Pravien Abeywickrema,Sarah Almond,Nicholas J. Brandon,Noel Byrne,Alister Campbell,Pete H. Hutson,Marlene A. Jacobson,Brian A. Jones,Sanjeev Munshi,Danette Pascarella,Andrew Pike,G. Sridhar Prasad,Nancy A. Sachs,Melanie Zea Sakatis,V V Sardana,Shankar Venkatraman,Mary Beth Young +17 more
TL;DR: Novel DAO inhibitors are identified, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma d-serine levels after dosing ip to rats.
95
The Behavioral and Neurochemical Effects of a Novel d-Amino Acid Oxidase Inhibitor Compound 8 [4H-Thieno [3,2-b]pyrrole-5-carboxylic Acid] and d-Serine
Sean M. Smith,Jason M. Uslaner,Lihang Yao,Chadwick M. Mullins,Nathan O. Surles,Sarah L. Huszar,Caitlyn H. McNaughton,Danette Pascarella,Monika Kandebo,Richard M. Hinchliffe,Tim Sparey,Nicholas J. Brandon,Brian A. Jones,Shankar Venkatraman,Mary Beth Young,Nancy A. Sachs,Marlene A. Jacobson,Peter H. Hutson +17 more
TL;DR: It is demonstrated that pharmacological inhibition of DAAO significantly increases d-serine concentration in the periphery and central nervous system and that high doses of d-Serine attenuated both amphetamine-induced psychomotor activity and dopamine release and also improved performance in novel object recognition.
88
The M1 muscarinic receptor allosteric agonists AC-42 and 1-[1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one bind to a unique site distinct from the acetylcholine orthosteric site.
TL;DR: The results suggest that structurally diverse allosteric agonists AC-42, TBPB, and N-desmethylclozapine may interact with different subsets of residues, supporting the hypothesis that M1 receptor activation can occur through at least three different binding domains.
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