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Sauerstoff-Heterocyclen ALS Neue, Selektive Liganden Fur Die Cannabinoid-Rezeptoren

Sauerstoff-Heterocyclen ALS Neue, Selektive Liganden Fur Die Cannabinoid-Rezeptoren

          
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About the Book

Die Entwicklung neuer Medikamente stellt seit jeher eine grosse Herausforderung an die Wissenschaft dar. Ein wichtiger Ansatzpunkt ist hierbei die Identifizierung korpereigener Targets, an denen neue Wirkstoffe ansetzen und dadurch den Krankheitsverlauf beeinflussen konnen. Eine wichtige Klasse an Targets bilden die membranstandigen G-Protein-gekoppelten Rezeptoren (GPCRs), zu denen auch die Cannabinoid-Rezeptoren gehoren. Die GPCRs sind Gegenstand aktueller Forschung zur Wirkstoffentwicklung, da uber diese Rezeptoren ein Eingriff in den Stoffwechsel der Zelle erfolgen kann, ohne dass das Medikament selbst in die Zelle eindringen muss. vspace{2ex Im Rahmen dieser Arbeit wurden neue, hoch affine und selektive Liganden fur die Cannabinoid-Rezeptoren sowohl auf Coumarin- als auch auf THC-Basis entwickelt. Die Darstellung der Coumarine erfolgte hierbei uber eine organokatalytische emph {de novo-Strategie. Ein hoch enantioselektiver Zugang zu Liganden auf THC-Basis konnte durch eine organokatalytische Diels-Alder-Reaktion unter Verwendung verschiedener Imidazolidinon-Katalysatoren nach MacMillan geschaffen werden. Desweiteren wurden diese Liganden in Radioligand-Rezeptor-Bindungsstudien auf ihre Affinitat zu den beiden Cannabinoid-Rezeptoren CB_1und CB_2untersucht. Dabei stellte sich heraus, dass Verbindungen mit Affinitaten im niedrigen nanomolekularen Bereich fur den CB_1- bzw. den CB_2-Rezeptor synthetisiert werden konnten. Je nach Verbindung wurde eine bis zu 100-fach hohere Selektivitat zu Gunsten des CB_1- bzw. des CB_2-Rezeptors beobachtet.


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Product Details
  • ISBN-13: 9783832525590
  • Publisher: Logos Verlag Berlin
  • Binding: Paperback
  • Language: German
  • Returnable: N
  • Spine Width: 0 mm
  • Width: 145 mm
  • ISBN-10: 3832525599
  • Publisher Date: 28 Aug 2010
  • Height: 210 mm
  • No of Pages: 280
  • Series Title: Beitrage Zur Organischen Synthese
  • Weight: 700 gr

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