Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase
摘要:
Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed. The role played by the amino groups of homo- and heterobivalent ligands in the interaction with the peripheral and catalytic sites of AChE and BuChE were investigated. The syntheses of these materials together with the results of AChE/BuChE inhibition assays are detailed. (C) 2001 Elsevier Science Ltd. All rights reserved.
Specific Targeting of Acetylcholinesterase and Butyrylcholinesterase Recognition Sites. Rational Design of Novel, Selective, and Highly Potent Cholinesterase Inhibitors
摘要:
Tacrine-based AChE and BuChE inhibitors were designed by investigating the topology of the active site gorge of the two enzymes. The homobivalent ligands characterized by a nitrogen-bridged atom at the tether level could be considered among the most potent and selective cholinesterase inhibitors described to date. The nitrogen-containing homobivalent ligands 3e,g and the sulfur-containing 3h validated the hypothesis of extra sites of interaction in the AChE and BuChE active site gorges.
SAMPLE COLLECTION DEVICES WITH BLOOD STABILIZING AGENTS
申请人:Hoke Randal A.
公开号:US20130209985A1
公开(公告)日:2013-08-15
Disclosed are devices for collecting and stabilizing blood or plasma and which contain an anti-coagulant, an antiplatelet agent, and a solubilization agent, and which may optionally include at least one other blood stabilization agent. Methods of making and using the devices in clinical medicine are also provided.
Disclosed are collection devices for collecting and stabilizing whole blood or a component thereof, which include a first end and a second end and at least one interior wall defining a reservoir, wherein the reservoir contains a stabilization agent that includes a lysophospholipase (LysoPLA) inhibitor. Also disclosed are methods for making and using the devices.
US9459187B2
申请人:——
公开号:US9459187B2
公开(公告)日:2016-10-04
Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase
作者:Luisa Savini、Giuseppe Campiani、Alessandra Gaeta、Cesare Pellerano、Caterina Fattorusso、Luisa Chiasserini、James M Fedorko、Ashima Saxena
DOI:10.1016/s0960-894x(01)00294-3
日期:2001.7
Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed. The role played by the amino groups of homo- and heterobivalent ligands in the interaction with the peripheral and catalytic sites of AChE and BuChE were investigated. The syntheses of these materials together with the results of AChE/BuChE inhibition assays are detailed. (C) 2001 Elsevier Science Ltd. All rights reserved.