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 · 2 points
From the ACMD report:
http://imgur.com/9DRQR
Also of interest, they found binding affinity for neither DA nor DAT.
u/MisterYouAreSoDumb
That's interesting. I cannot for the life of me find any evidence of it in studies, though. It seems that it is an NMDAR antagonist and dopamine re-uptake inhibitor. It also an agonist at dopamine D2, serotonin 5HT2, muscarinic cholinergic, sigma-1, opioid mu and k receptors. I show no SERT binding affinity. It's actually a really interesting substance!