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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.


Author Stevan Pecic

Product Details


GTIN 9783847344919

Release Date 30.09.2019

Language English

Pages 276

Product type Paperback

Dimension 8.66 x 5.91 x 0.63  inches

Product Weight 15.17 ounces

Aporphines - MDMA Antagonists and AChE Inhibitors

Synthesis and Evaluation

Stevan Pecic


Seller: Dodax EU

Delivery date: between Tuesday, July 14 and Thursday, July 16

Condition: New

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