3 ms·
That's misleading, MDMA itself has very little affinity for 5HT2b, but its action on the SERT dumps loads of serotonin which displays, by definition, pretty hig
by Uberphallus 11y ago
That's misleading, MDMA itself has very little affinity for 5HT2b, but its action on the SERT dumps loads of serotonin which displays, by definition, pretty high affinity for it (Ki < 10, according to this https://www.acnp.org/g4/GN401000039/Ch039.html https://www.acnp.org/g4/GN401000039/Ch039.html). So even if the chemical doesn't show significant activity on 5HT2b in vitro, in vivo it actually does.
- Nursie 11y agoFair enough! You're likely more informed than I am in these matters. So here's a question - I had assumed that the SERT-dumping action of MDMA took place in the brain and did not spread masses of serotonin to the rest of the body, is this correct? Or does MDMA trigger serotonin floods that do get out to the system in general? The drug (be it MDMA or xAPB) is swimming around the whole system and is therefore free to act on the 5HT2b receptors present in the heart itself, which could promote valve mutation. Is this true for the serotonin as well?
- Uberphallus 11y agoThe substance reaches wherever blood gets to, with exceptions when crossing the brain barrier. Most of the 5-HT receptors are in the brain though. It's not true for serotonin. Serotonin is to be released, taken back and metabolized locally, in and around the synapse. It doesn't travel around the body, at least in significant amounts, as hormones do.