N&PD Moderators: Skorpio | thegreenhand
O-4310 (1-isopropyl-6-fluoro-psilocin) is a tryptamine derivative developed by Organix which acts as a serotonin receptor agonist. It is claimed to have an EC50 of 5nM at 5-HT2A with 89% efficacy vs 5-HT, and 100x selectivity over 5-HT2C, while being apparently inactive at the 5-HT2B antitarget.[1]
Indeed O-4244 may be the best candidate psychedelic, though O-4310 is the most 5HT2A selective. The 1-ethyl derivative O-4284 and corresponding 7-fluoro isomer O-3943 also look promising.The most potent likely psychedelic compound from that patent (thanks Organix! patent US7655691) is O-4244 or 3-(2-Dimethylaminoethyl)-6-fluoro-1-methyl-1H-indol-4-ol. It displays strong h5HT2A (0.55 nM for 61% IP3 turnover activity) and h5HT2C (0.66 nM for 75% IP3 turnover activity) partial agonist activity while having no activity at 5HT2B.
Keep in mind also that binding numbers are not always perfect and that the NBOMe's had low 5-ht2b affinity as well, until they didn't.The most potent likely psychedelic compound from that patent (thanks Organix! patent US7655691) is O-4244 or 3-(2-Dimethylaminoethyl)-6-fluoro-1-methyl-1H-indol-4-ol. It displays strong h5HT2A (0.55 nM for 61% IP3 turnover activity) and h5HT2C (0.66 nM for 75% IP3 turnover activity) partial agonist activity while having no activity at 5HT2B. This is on par with the other ultrapotents such as the NBOMe's and LSD, although at such high intrinsic activities I would have some worry about toxicity if one isn't particularly exacting about their doses.