Comment · Sat, December 22, 2012
Please help me understand binding affinities
Original post in this thread
kbrc · 13 points
I re-read the ACMD report on MXE just now and saw that it shows binding affinity for SERT (serotonin transporter), but no serotonin receptors (e.g. 5-HT2A like many psychedelics). Could someone explain simply what this means? My understanding is that SERT is sort of the "cargo vessel" for serotonin that docks with serotonin receptors to onload or offload serotonin "cargo". So if MXE binds to SERT, does this mean it's imitation "cargo" and eventually gets offloaded non-selectively to all serotonin receptors? Or that the real serotonin "cargo" gets left on the receptor "docks" (or the synaptic "sea") for longer because the transporters are busy handling MXE? Or perhaps my analogy just totally silly and I need a new understanding entirely.
I'd like to understand the general mechanism here, and also would like to know specifically if MXE would be cross-tolerant with psychedelics that bind to 5-HTx receptors.
What they were answering
kbrc · 1 points
Your link is to a hypothesis, not to actual data. MXE being a DRI or binding to any of those other receptors was total speculation, whereas the ACMD report actually did assays on a large number of receptors and found no binding affinities.
Borax posted the actual PDF some time ago: http://www.reddit.com/r/DrugNerds/comments/x2l1z/methoxetamine_from_drug_of_abuse_to_rapidacting/
It speculates about all those other receptors based on a single reference to http://dx.doi.org/10.1016/j.annemergmed.2011.11.018
u/MisterYouAreSoDumb
That makes much more sense. That many binding affinities seemed crazy. Your point about the SERT provides an explanation for the serotonin syndrome symptoms that some people have been reporting.