ibopyrine-chemistry

Winfried Gerbracht Winfried.Gerbracht at t-online.de
Tue Apr 30 03:51:21 EDT 2002



Hi Nick. Hi 'ibogainers' [and ibogaine-sceptics],

I want to inform you briefly about the state of my research-project.
A year ago I got the opportunity to pursue my syntheses of ibopyrines at
the ETH in Switzerland. Due to the moving of the institute I was forced
to interrupt the project halfway down.
Nevertheless, I had been able to synthesize an azepano-acyloin, which is
the direct precursor of the corresponding ibopyrine-indoles (as novel
structural analogs of ibogaine). The synthesis turned out to be even
shorter, easier and more ingenious than expected.

Yesterday I rang up Mr. Borschberg from the ETH and he promised me to
finish the synthesis this summer. Unfortunately there will be no further
chance to perform it myself.

Howard recently posted the abstract of the latest Stan Glick-paper that
focuses the attention on a special (nicotinic) receptor, which was
discovered within the last years, that may play a major role in the
anti-craving mechanism:

	>...The data are consistent with the hypothesis that 
	antagonism at alpha3beta4 receptors is a potential mechanism 
	to modulate drug seeking behavior. 18-Methoxycoronaridine 
	apparently has 	greater selectivity for this site than other 
	agents and may 	be the first of a new class of synthetic agents 
	acting via this novel mechanism to produce a broad spectrum of 
	anti-addictive activity.<

By the way, it's a receptor at which an alkaloid, called epibatidine,
reveals (agonistically) its very potent painkilling activity
(200times more potent than morphium).
This principle affords a revolutionary new mechanism of analgesia, since
it excludes most, if not all of the side-effects of opiate-analgesia:

http://www.phc.vcu.edu/feature/epi/index2.html

I'm quite sure that the ibopyrines  will fit quite well into this
receptor. So I believe to be straight on the right track. As you know
me, I could endlessly talk about receptor interactions, ... it'll be
boring for the most.

I'll keep you informed.

Salute,
Winnie
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