Aporphines - MDMA Antagonists and AChE Inhibitors: Synthesis and Evaluation

Aporphines - MDMA Antagonists and AChE Inhibitors: Synthesis and Evaluation

von Stevan Pecic
Taschenbuch - 9783847344919
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Beschreibung

MDMA is a psychoactive drug which is thought to act via stimulation of secretion as well as inhibition of re-uptake of large amounts of serotonin, noradrenaline and dopamine in the brain. MDMA also acts directly on a number of receptors, including 5-HT2A receptors. There is considerable evidence that 5-HT2A antagonists can modulate behavioral and physiological effects of MDMA in animals. Nantenine an aporphine alkaloid ex Nandina domestica has been reported to block and reverse a range of behavioral and physiological effects of MDMA in mice. In this book is shown synthesis and design of a library of novel analogs in order to investigate the structural requirements for nantenine's 5-HT2A activity. To elucidate possible binding modes of these compounds and to determine the correlation with our binding data, we built a 5-HT2A homology model based on a bovine rhodopsin template and then performed docking/scoring experiments. In the second part of the book, nantenine as well as a number of flexible analogs were evaluated for acetylcholinesterase (AChE) inhibitory activity in a microplate spectrophotometric assays based on Ellman's method.

Details

Verlag LAP Lambert Academic Publishing
Ersterscheinung Februar 2014
Maße 220 mm x 150 mm x 17 mm
Gewicht 427 Gramm
Format Taschenbuch
ISBN-13 9783847344919
Auflage Nicht bekannt
Seiten 276

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