Author Topic: Structurally modified ibogaine analogs ....  (Read 2820 times)

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Offline pkeffect

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Structurally modified ibogaine analogs ....
« on: May 07, 2010, 07:39:04 PM »
"We exist in a multidimensional polymorphic hyperspacial internode of neurotranslinguistic manifestations subjugated by hyperbolic quantum entanglement." - me

Offline GratefulDad

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Re: Structurally modified ibogaine analogs ....
« Reply #1 on: May 07, 2010, 10:10:51 PM »
Eur J Pharmacol. 1996 Aug 8;309(2):159-65.
Structurally modified ibogaine analogs exhibit differing affinities for NMDA receptors.
Layer RT, Skolnick P, Bertha CM, Bandarage UK, Kuehne ME, Popik P.

Laboratory of Neuroscience, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0008, USA. rtlayer@helix.nih.gov
Abstract
Based on both preclinical findings and anecdotal evidence in man, the psychoactive indole alkaloid ibogaine has been suggested to have anti-addictive properties. Previous studies indicate that blockade of NMDA receptors may mediate at least some of the putative anti-addictive actions of ibogaine. The potencies of a series of ibogaine analogs to inhibit (+)-[3-3H]5-methyl-10,11-dihydro-5H-dibenzo-[a,d]cyclohepten-5,10- imine ([3H]MK-801) binding to NMDA receptors were examined. This series of analogs included the putative ibogaine metabolite O-desmethylibogaine, its metabolism resistant analog O-t-butyl-O-desmethylibogaine, the iboga alkaloids (+/-)-ibogamine, (+/-)-coronaridine, tabernanthine, harmaline, and the indolotropanes endo-3-(1-methylindol-2-yl)-8-methyl-8-azabicyclo[3.2.1]loctane (RS 075194-190), exo-3-(1-methylindol-2-yl)-8-methyl-8-azabicyclo[3.2.1]octane (RS 075237-190), and endo-3-(indol-2-yl)-8-methyl-8-azabicyclo[3.2.1]octane (RS 025989-190). Among these compounds, ibogaine was the most potent inhibitor of [3H]MK-801 binding (Ki = approximately 1.2 microM), whilst the compounds with the greatest structural similarity to ibogaine, O-desmethylibogaine and O-t-butyl-O-desmethylibogaine were less potent (Ki = approximately 5.5 and 179.0 microL, respectively). In morphine-dependent mice, ibogaine, but not O-desmethylibogaine or O-t-butyl-O-desmethylibogaine, attenuated naloxone precipitated withdrawal jumping. These findings are consistent with the hypothesis that inhibition of the expression of morphine dependence by ibogaine is related to its NMDA receptor antagonist properties.

PMID: 8874134 [PubMed - indexed for MEDLINE]
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Offline pkeffect

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Re: Structurally modified ibogaine analogs ....
« Reply #2 on: May 08, 2010, 11:18:43 AM »
You know the reason I post links and not the whole article is because sometimes its better left in the original format.
"We exist in a multidimensional polymorphic hyperspacial internode of neurotranslinguistic manifestations subjugated by hyperbolic quantum entanglement." - me

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Re: Structurally modified ibogaine analogs ....
« Reply #3 on: May 08, 2010, 12:24:18 PM »
Heavy duty info man!  :D

Offline GratefulDad

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Re: Structurally modified ibogaine analogs ....
« Reply #4 on: May 08, 2010, 01:54:40 PM »
You know the reason I post links and not the whole article is because sometimes its better left in the original format.

Yeah, I figured, but sometimes the links change or go bad, so I figure throwing up the abstract wasn't a bad idea!  ;)


Edited: Closed that tag for ya ;)
« Last Edit: May 08, 2010, 02:01:01 PM by pkeffect »
GratefulDad

"If trees could scream, would we be so cavalier about cutting them down? We might, if they screamed all the time, for no good reason."