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Melevodopa & similar dopamine agonist to releasing agent SAR

Nagelfar

Nagelfar

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Seeing how MDMA is a SERT releaser with serotonin agonism traits. Might a dopamine agonist, such as melevodopa, be modified to be also a DAT releaser while retaining its DA receptor agonism profile?

Perhaps (in the instance of melevodopa) by some means such as adding a second nitrogen?
 
Does melevodopa cross the BBB? It doesn't look like it should, but maybe it fools the amino acid transporter or something?

Also: methamphetamine et al do not generally have significant DA receptor affinity, though they are all TAAR agonists of varying affinity. Something like PF-219061 could be modified to hit both the transporter and some of the D2-like receptors (D2, D3, and D4), maybe, but D2 and D3 are generally linked to the less pleasant effects of dopaminergic stimulants.

D4 agonists include derivatives of 4-phenyl-indol-2-ylmethylpiperazine, which does not look like any DAT ligand I've ever heard of.
 
Last edited:
atara said:
Does melevodopa cross the BBB? It doesn't look like it should, but maybe it fools the amino acid transporter or something?

Also: methamphetamine et al do not generally have significant DA receptor affinity, though they are all TAAR agonists of varying affinity. Something like PF-219061 could be modified to hit both the transporter and some of the D2-like receptors (D2, D3, and D4), maybe, but D2 and D3 are generally linked to the less pleasant effects of dopaminergic stimulants.

D4 agonists include derivatives of 4-phenyl-indol-2-ylmethylpiperazine, which does not look like any DAT ligand I've ever heard of.
Click to expand...

Melevodopa is an "effervescent prodrug" closer to levo-dopa than dopamine, and since L-dopa crosses the BBB I assume melevodopa does too.

My question is more about how DRAs could be similar enough to dopamine, drugs with structures like oxidopamine or melevodopa but also to methamphetamine, to have agonist properties themselves and if so which drugs do; not whether or not ones I mentioned as examples indeed had such properties (but if, and if, to what degree which do, would be welcome information as well)
 
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