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tropane dri

Nexus298

Bluelighter
Joined
Feb 9, 2008
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118
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usa
Ive just heard about the variation of the dri and was wondering if anyone could point me in the direction of more info on this. i am looking for binding affinities of dopamine cocaine mdpv petadrone apvp methylphenidate and any other dri compounds if they are even known. i also would like to know of the location of the tropane dri's. im pretty sure the bonding affinithes for mdpv apvp pentedrone and the other 5 carbon phens are not available yet so i would like to postulate that they have a higher tropane dri affinity based on subJective effects.
 
Also what is the possibility of an endegonous neurotransmitter with higher affinity than dopamine?
 
i would like to postulate that they have a higher tropane dri affinity based on subJective effects.

I'm sorry, I don't really understand your question. Tropane is just a particular functional group found in several cocaine like stimulants, not an active drug. Eg, most of the RTI-series are phenyltropanes (while cocaine itself is just a tropane, with an ester linking the phenyl group). What is "tropane dri affinity"? Affinity for monoamine transporters determines a large proportion of the effects of numerous stimulants.

Also what is the possibility of an endegonous neurotransmitter with higher affinity than dopamine?

It is scarce. The dopamine receptor evolved in concert with its endogenous ligand, while other potential endogenous ligands did not. One exception might be binding affinities of DMT at some 5ht receptor subtypes, but DMT is only a partial agonist there and might not even act as a neurotransmitter.

ebola
 
I meant the affinity for this dri that is preferential to tropanes. i would like any sources with any info on this subject
 
I'm a bit confused by what you're asking. DRI means dopamine reuptake inhibitor, it describes drugs like cocaine and methylphenidate (ritalin). Maybe you mean DAT (dopamine transporter)?
 
If you're looking for affinity data, try searching Pubmed and Google.

Here's some to get you started.
From a paper on 'bath salts', the affinities for MDPV:
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And a Big Ol' Wikipedia Data Dump.

Most of these compounds had their affinities known before people started making them.... that was why they were selected as "research chemicals". Some enterprising young chemist looked in the med chemistry journals and picked the stimulants with the tightest DAT binding.....
 
Am I confused, or do these data suggest that MDPV functions as a releaser?

ebola

I think you're correct. This is the first time I've seen any data on MDPV monoamine uptake (never mind release), and all I can say is that is quite a lot of dopamine...
 
Am I confused, or do these data suggest that MDPV functions as a releaser?

Given the Emax is something like 24%, I don't think it's a very effective releaser... nobody considers cocaine a releaser either.

Lower numbers = higher affinity, yes.
 
Given the Emax is something like 24%, I don't think it's a very effective releaser... nobody considers cocaine a releaser either.

Ah. What does this suggest about interpretation of EC50 values in the absence of %Emax data?

ebola
 
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