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
Direct reply to the original post — see the thread post above.
u/MisterYouAreSoDumb
Where do you see that methoxetamine binds to the SERT? I am unaware of any significant SERT activity with MXE.
The SERT are serotonin transporters that re-uptake used serotonin from the synapse. Basically they pull the serotonin back up into the neurons after it has already done it's job binding to the various receptors. Substances that block the SERT cause increased extracellular serotonin levels, since they are blocked from up-taking it from the synapse. This leads to the serotonin binding to receptors again, which causes the drug's effect.