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Emetic Activity of Reduced Lysergamides

Started by java, September 09, 2004, 07:14:00 AM

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java

Note The article referenced but not posted after searching TFSE no hits for 16 532 1973 with the study , hence with that in mind I post it as it may be of some use to the Hive , thanks to Hyperlab Chemister reference at

http://rzv073.rz.tu-bs.de/bib/dir1/Books/booknews.htm



Emetic Activity of Reduced Lysergamides
David g. Teiger; Ronald J. Kassel; Fatima N. Johnson, Istvan E. Ary
 Journal of Medicinal ChemistryVol. 16 No. 3 532 1973

Abstract

A new efficient method for the direct amidation of d-lysergic acid was used to prepare a variety of lysergamides. A pharmacological evaluation of these compounds, their di- and tetrahydro derivatives, and derivatives bearing substituents in the indole portion of the molecule showed that, in general, only 9,lOdihydrolysergamides of primary amines possess activity comparable to the potent emetic activity of the components of dihydroergotoxine.
https://www.thevespiary.org/rhodium/Rhodium/hive/hiveboard/picproxie_docs/000530446-lysergamide-emetics.pdf" target="_blank" title="Download this file">




Fastandbulbous

I imagine that their emetic properties is closely linked to their dopamine agonist activity, as dopamine in the CTZ (chemoreceptor trigger zone) is a pretty good way of ensuring a bout of doing the big spit (I really like Hunter S Thompson's name for vomiting!). It's the dopamine agonist activity of apomorphine and emetine that makes them so good at instigating vomiting (calling an alkaloid emetine really makes you want to try it, doesn't it!)