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- Newsgroups: alt.psychoactives
- From: bwhite@oucsace.cs.ohiou.edu (William E. White )
- Subject: There is a specific beta-carboline binding site!
- Message-ID: <Cz9MIp.5B3@oucsace.cs.ohiou.edu>
- Date: Mon, 14 Nov 1994 16:16:00 GMT
-
- While going through journals this weekend I came across an interesting
- study which (although not, to my knowledge replicated yet, seems to
- have OK methodology) has found a specific binding site for norharman
- (beta-carboline). This is fairly old so maybe it's been refuted
- (or maybe everyone but me knows this already). In particular this was
- before the explosion of identified 5HT receptor types (which now
- includes 5HT1A, 5HT1B, 5HT1C, 5HT1Dalpha, 5HT1Dbeta, 5HT1E, 5HT1F,
- 5HT2, 5HT3, 5HT4, 5HT5A, 5HT5B, 5HT6, and 5HT7!)
-
- The abstract:
-
- Journal of Chemical Neuroanatomy 1990 Jan-Feb;3(1):19-24
- "Quantitative autoradiography of [3H]norharman ([3H]beta-carboline)
- binding sites in the rat brain."
-
- The anatomical distribution of [3H]norharman binding sites was determined
- by quantitative autoradiography in rat brain slices. They are enriched
- in hypothalamic, thalamic, accumbens and amygdaloid nuceli as well as in
- hippocampal, neocortical, and olfactory-related structures. The distri-
- bution pattern differs from that of other previously described receptors
- or binding sites (e.g., monoamine oxidase, benzodiazepine, tryptamine,
- 5-hydroxytryptamine receptors (5-HT1a, 5-HT1B, 5-HT1C, 5-HT2), which
- suggests that a unique class of [3H]norharman binding sites exists in the
- rat brain. The findings are consistent with previous experiments which
- showed high-affinity binding sites for [3H]norharman in rat brain
- membranes (KD 1.552 nM; autoradiography KD 5.5nM). A correspondance in
- the displacing activity of drugs was found for both methods (crude
- membrane fraction: harman much greater than tryptamine much greater than
- 5-hydroxytryptamine greater than N-methyl-beta-carboline-3-carboxamide
- (FG 7142) = diazepam; autoradiography: harman much greater than tryptamine
- much greater than FG7142 greater than 5-hydroxytryptamine greater than
- diazepam). Provided that the binding sites represent functional receptors,
- the present anatomical findings may explain the biological effects of
- norharman, e.g. pro-conflict behaviour (limbic-hypothalamic structures),
- tonic-clonic convulsions (limbic-cortical structures) and alterations of
- locomotor activity (accumbens nucleus).
-
-
- --
- | Bill White +1-614-594-3434 | bwhite@oucsace.cs.ohiou.edu |
- | 44 Canterbury, Athens OH 45701 | finger for PGP2.2 block |
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