Abstract:
:Clinical experience with muscarinic agonists in the symptomatic treatment of Alzheimer's disease includes studies of the effects of pilocarpine, arecoline, bethanechol, oxotremorine and RS 86. Although the results are somewhat conflicting, there is evidence that a subgroup of patients may respond with an improvement of cognitive and/or behavioural function. The existing agents tend to induce adverse effects due to the stimulation of peripheral muscarinic receptors. Furthermore they reduce (at least in vitro) acetylcholine release by an action on presynaptic receptors. Strategies to overcome these problems include the development of potent agonists with high blood-brain barrier penetration, the search for agents selective for muscarinic receptor subtypes (using cloned receptors as tools) and the identification of agents acting as presynaptic receptor antagonists, to increase acetylcholine release.
journal_name
Trends Pharmacol Scijournal_title
Trends in pharmacological sciencesauthors
Gray JA,Enz A,Spiegel Rsubject
Has Abstractpub_date
1989-12-01 00:00:00pages
85-8eissn
0165-6147issn
1873-3735journal_volume
Supplpub_type
杂志文章,评审abstract::It has been over 50years since Sir James Black developed the first beta adrenergic receptor (βAR) blocker to treat heart disease. At that time, the concept of cell surface receptors was relatively new and not widely accepted, and most of the tools currently used to characterize plasma membrane receptors had not been d...
journal_title:Trends in pharmacological sciences
pub_type: 杂志文章,评审
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
pub_type: 新闻
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
pub_type: 杂志文章,评审
doi:10.1016/j.tips.2010.08.005
更新日期:2010-11-01 00:00:00
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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abstract::Protein kinase Calpha (PKCalpha) is a member of the AGC (which includes PKD, PKG and PKC) family of serine/threonine protein kinases that is widely expressed in mammalian tissues. It is closely related in structure, function and regulation to other members of the protein kinase C family, but has specific functions wit...
journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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abstract::Pairing orphan G-protein-coupled receptors (GPCRs) to potential ligands found in tissue extracts or in libraries of synthetic compounds has identified an ever-increasing number of transmitters, some of which are novel, some of which were previously known and, more recently, some of which are unexpected. These discover...
journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
pub_type: 杂志文章,评审
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journal_title:Trends in pharmacological sciences
pub_type: 杂志文章,评审
doi:10.1016/j.tips.2009.07.001
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journal_title:Trends in pharmacological sciences
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doi:10.1016/j.tips.2008.10.005
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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abstract::The fruit fly Drosophila melanogaster has been used for modeling cancer and as an in vivo tool for the validation and/or development of cancer therapeutics. The impetus for the use of Drosophila in cancer research stems from the high conservation of its signaling pathways, lower genetic redundancy, short life cycle, g...
journal_title:Trends in pharmacological sciences
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abstract::Molecular forms of acetylcholinesterase exhibit tissue-specific distribution, and each form is anchored to the cell surface via a particular post-translational modification of the catalytic subunit. Nibaldo Inestrosa and Alejandra Perelman review evidence that heparan sulphate proteoglycans are the extracellular matri...
journal_title:Trends in pharmacological sciences
pub_type: 杂志文章,评审
doi:10.1016/0165-6147(89)90067-9
更新日期:1989-08-01 00:00:00
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
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journal_title:Trends in pharmacological sciences
pub_type: 杂志文章,评审
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更新日期:1990-03-01 00:00:00
abstract::The disruption of large protein-protein (PP) interfaces remains a challenge in targeted therapy. Designing drugs that compete with binding partners is daunting, especially when the structure of the protein complex is unknown. To address the problem we propose a deep protein databank (PDB) learning platform to discover...
journal_title:Trends in pharmacological sciences
pub_type: 杂志文章
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