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Synthese selektiver Muskarin M3-Rezeptor Antagonisten

Synthese selektiver Muskarin M3-Rezeptor Antagonisten


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About the Book

Bachelorarbeit aus dem Jahr 2014 im Fachbereich Chemie - Sonstiges, Note: 1.0, Friedrich-Alexander-Universität Erlangen-Nürnberg, Sprache: Deutsch, Abstract: G-Protein gekoppelte Rezeptoren (GPCR) sind die größte Klasse von Membranprote-inen im menschlichen Genom und eine wichtige Targetklasse für derzeitige Medika-mente. Sie folgen alle demselben strukturellen Aufbauprinzip aus sieben transmembranären α-Helices (TM), die über drei intrazelluläre und drei extrazelluläre Schleifen (ICL und ECL) miteinander verbunden sind. Bei Aktivierung durch einen endogenen oder exogenen Liganden wird eine Signalkaskade induziert, an deren erster Stelle das tri-mere G-Protein steht. Dieses koppelt an den ICL 3, wird gespalten und migriert ent-lang der Innenseite der Membran zum Effektorsystem. Eine interessante Gruppe sind die muskarinergen Acetylcholin Rezeptoren (mAChR), die namentlich von deren endogenen Liganden Acetylcholin und vom exogenen A-gonisten Muscarin abgeleitet sind. Neben der Expression im ZNS ist deren Präsenz im pullmonalen System von großem Interesse. Sie werden mit Atemwegserkrankun-gen, wie der chronisch obstruktive Lungenerkrankungen (COPD) und Asthma in Verbindung gebracht. Diese Rezeptoren können in die Subklassen M1-M5 unterteilt werden. M1, M3 und M5 sind Gq/11 und M2, M4 sind Gi/o gekoppelt. Von den in menschlichen Atemwegen ex-primierten Rezeptoren M1-M4, ist der M3-Rezeptor hauptsächlich auf den glatten Muskelzellen zu finden und stellt das Haupttarget für Medikamente dar. Ziel ist es, in der Therapie von COPD selektiv den Subtyp M3 zu blockieren, um eine Bronchial-verengung zu vermeiden. Simultanes Blockieren des präsynaptischen M2-Rezeptors führt zu einer abgeschwächten Wirkung[6], da dieser ein Autorezeptor ist.


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Product Details
  • ISBN-13: 9783668255586
  • Publisher: Grin Publishing
  • Binding: Paperback
  • Language: German
  • Returnable: N
  • Spine Width: 3 mm
  • Width: 148 mm
  • ISBN-10: 366825558X
  • Publisher Date: 08 Jul 2016
  • Height: 210 mm
  • No of Pages: 48
  • Series Title: German
  • Weight: 127 gr


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