AMPA receptor ligands: synthetic and pharmacological studies of polyamines and polyamine toxins

Medicinal Research Reviews
K Strømgaard, I R Mellor

Abstract

Alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors (AMPAR), subtype of the ionotropic glutamate receptors (IGRs), mediate fast synaptic transmission in the central nervous system (CNS), and are involved in many neurological disorders, as well as being a key player in the formation of memory. Hence, ligands affecting AMPARs are highly important for the study of the structure and function of this receptor, and in this regard polyamine-based ligands, particularly polyamine toxins, are unique as they selectively block Ca2+ -permeable AMPARs. Indeed, endogenous intracellular polyamines are known to modulate the function of these receptors in vivo. In this study, recent developments in the medicinal chemistry of polyamine-based ligands are given, particularly focusing on the use of solid-phase synthesis (SPS) as a tool for the facile generation of libraries of polyamine toxin analogues. Moreover, the recent development of highly potent and very selective AMPAR ligands is described. Additionally, we provide a detailed account on the mechanism and site of action of AMPAR blockade by polyamine-based ligands, including examples of how these ligands are used as tools to study AMPAR, and a comparison with their acti...Continue Reading

References

Apr 12, 1979·Nature·J B PatlakP N Usherwood
Mar 1, 1992·Toxicon : Official Journal of the International Society on Toxinology·I S BlagbroughP N Usherwood
Apr 15, 1992·The Journal of Comparative Neurology·R S Petralia, R J Wenthold
Jul 2, 1992·Nature·T KutsuwadaM Arakawa
Jan 1, 1991·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·H Karst, T Piek
Nov 11, 1991·Neuroscience Letters·A DraguhnV Witzemann
Nov 7, 1991·Nature·K MoriyoshiS Nakanishi
Jan 11, 1990·Toxicon : Official Journal of the International Society on Toxinology·M BruceP N Usherwood
Jul 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·A T EldefrawiP N Usherwood
Jun 1, 1988·Trends in Pharmacological Sciences·C Melchiorre
Mar 1, 1986·The Biochemical Journal·A E Pegg
Mar 6, 1980·Nature·P Krogsgaard-LarsenD Lodge
Jan 1, 1984·Annual Review of Biochemistry·C W Tabor, H Tabor
Jul 15, 1995·The Journal of Physiology·S K KambojS G Cull-Candy
Apr 1, 1995·Trends in Neurosciences·Z G Wo, R E Oswald
Sep 26, 1995·Proceedings of the National Academy of Sciences of the United States of America·S D Donevan, M A Rogawski
May 23, 1995·Proceedings of the National Academy of Sciences of the United States of America·M W WoodA M VanDongen
Feb 3, 1995·The Journal of Biological Chemistry·Z G Wo, R E Oswald

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Citations

Feb 24, 2007·Psychopharmacology·Keli CameraMaribel Antonello Rubin
Dec 17, 2009·Amino Acids·Anna MinariniCarlo Melchiorre
Apr 7, 2004·Toxicon : Official Journal of the International Society on Toxinology·Ian R Mellor, Peter N R Usherwood
Mar 5, 2010·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Gary Gang ChenGustavo Turecki
Mar 18, 2011·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Alexander C Jackson, Roger A Nicoll
May 20, 2011·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Alexander C JacksonRoger A Nicoll
Jul 26, 2005·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Kristian Strømgaard
Aug 31, 2006·Magnetic Resonance in Chemistry : MRC·Kristian StrømgaardJerzy W Jaroszewski
Oct 29, 2011·Angewandte Chemie·Christian A OlsenKristian Strømgaard
Jul 2, 2005·Bioorganic & Medicinal Chemistry·Trine F AndersenKristian Strømgaard
Mar 19, 2016·The Journal of Pharmacology and Experimental Therapeutics·Michael P MaherTimothy W Lovenberg
May 9, 2012·European Journal of Pharmacology·David W McClymontIan R Mellor
Feb 3, 2015·Journal of Neurochemistry·Rosamund E Combs-BachmannJames J Chambers
Apr 3, 2007·Pharmacology & Therapeutics·Márcia Renata MortariWagner Ferreira dos Santos
Dec 1, 2009·Analytical and Bioanalytical Chemistry·Satoshi MigitaTetsuya Haruyama
Mar 5, 2015·Chemistry : a European Journal·Si Yu TanYanli Zhao
Jul 9, 2004·Biophysical Journal·Denis B TikhonovPeter N R Usherwood
Jun 23, 2005·Toxicon : Official Journal of the International Society on Toxinology·Samy ZalatIan R Mellor
Sep 1, 2006·Journal of Medicinal Chemistry·Trine F AndersenKristian Strømgaard
Jan 17, 2013·Journal of Medicinal Chemistry·Mette H PoulsenKristian Strømgaard
Dec 30, 2010·Journal of Natural Products·Anne F BarslundKristian Strømgaard
Sep 15, 2006·The Journal of Physical Chemistry. a·P ThanasekaranKuang-Lieh Lu
Mar 30, 2007·Journal of the American Chemical Society·Aaron Nilsen, Pamela M England
May 17, 2011·Pharmacology, Biochemistry, and Behavior·Carlos Riaza Bermudo-SorianoEnrique Baca-Garcia

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