resorcinol
05-04-2009, 12:49 AM
radioactive.
We'll never, ever know what 2C-At would feel like, or DOAt. If the SAR trend were to continue 2C-At would be very potent. It would also be very potent at tearing your 5-ht(2a) receptors to shreds with radiation (and plenty of other cells also). In fact ingesting a mg of 2C-At would kill you dead. It's so sad that At is radioactive.
We can approximate though. The radius of the trifluoromethane group is similar to the atomic radius of astatine, and TFM is a pseudohalogen. So 2C-TFM (which is very potent) is probably a good representation of how 2C-At would feel if At wasn't radioactive.
There are interesting heteroatoms that do have stable isotopes that can be used to create exotic drugs, though. Selenium is the one with perhaps the largest untapped potential. It's a chalcogen just like oxygen and sulfur, and we know that chalcogens (especially oxygen, and occasionally sulfur) are incorporated into many psychoactive drugs. Selenium could almost certainly substitute for oxygen or sulfur in MANY psychoactives and result in active drugs. 2C-Se (which actually has a methylseleno group at position 4 since selenium forms two covalent bonds, not one like a halogen). 2C-Se is a fullblown hallucinogen of the classical type at 100 mg (not very potent, but definitely active and worthwhile, unlike the flop that was 2C-N). 2C-Se-x (the selenium analogs of the sulfur containing 2C-T-x drugs) drugs would likely be interesting and potent, as would DOSe (which would likely be quite potent).
I've lately had a fascination with morphine-like opioids where some of the oxygens are replaced with either sulfur or selenium ... a place where few opioids have gone to actual human use (sulfur has in a few rare cases like sufentanil and dimethylthiambutene, but selenium hasn't). I'm pretty sure that 14-mercapto-hydrocodone (imagine oxycodone but replace the oxygen in the -OH at position 14 with a -SH), 14-methylthio-hydrocodone (imagine oxycodone but replace that same -OH as before with a -S-CH3), and 14-methylseleno-hydrocodone (replace the same -OH as in the other two with a -Se-CH3) would all be awesome.
The 14-mercapto-hydrocodone would likely be similar in potency and effects to oxycodone. The latter two would likely be similar in effects to oxycodone but more potent (possibly by a significant margin).
So while we can never know what drugs with astatine, polonium, francium, etc heteroatoms would feel like because the elements are unstable, there are stable elements that have not been exploited very much in pharmacology (selenium is particularly attention grabbing because chalcogen atoms are ubiquitous in drugs, psychoactive and non ... oxygen is everywhere, sulfur is occasionally found, but selenium has been ignored [even though it's likely to create relatively non-toxic organic chalcogen containing compounds ... non toxic in that the selenium's presence is unlikely to impart toxic characteristics to most cases where it replaces oxygen or sulfur ... of course highly toxic compounds that contain selenium could be created, like an irreversible inhbitor of cholinesterase that contains selenium heteroatom(s) would be deadly, but not because of the selenium, but because of it's pharmacological action ... sarin is a cholinesterase inhibitor that's irreversible and that's how it kills]). Tellurium is an even heavier chalcogen than selenium (next down in the chalcogen column), but tellurium heteroatoms would be bad news -- there'd definitely be toxicity issues directly from tellurium. Polonium is the next chalcogen down, with an even heavier atomic mass, but whoops.... it's radioactive. I'm sure 14-methylpolono-hydrocodone is potentially a mu agonist, but the alpha particles from the radioactive decay of polonium would shred your mu receptors and plenty of other cells throughout the systemic circulation.... polonium is HIGHLY radiologically toxic when ingested (relatively safe outside the body though even in large quantities since alpha particles from alpha decay cannot penetrate into the body from an alpha emitter outside the body). So selenium, deserves some attention. Tellurium is rightfully ignored for chemical toxicity reasons, polonium because it's a highly toxic radiological poison.
We'll never, ever know what 2C-At would feel like, or DOAt. If the SAR trend were to continue 2C-At would be very potent. It would also be very potent at tearing your 5-ht(2a) receptors to shreds with radiation (and plenty of other cells also). In fact ingesting a mg of 2C-At would kill you dead. It's so sad that At is radioactive.
We can approximate though. The radius of the trifluoromethane group is similar to the atomic radius of astatine, and TFM is a pseudohalogen. So 2C-TFM (which is very potent) is probably a good representation of how 2C-At would feel if At wasn't radioactive.
There are interesting heteroatoms that do have stable isotopes that can be used to create exotic drugs, though. Selenium is the one with perhaps the largest untapped potential. It's a chalcogen just like oxygen and sulfur, and we know that chalcogens (especially oxygen, and occasionally sulfur) are incorporated into many psychoactive drugs. Selenium could almost certainly substitute for oxygen or sulfur in MANY psychoactives and result in active drugs. 2C-Se (which actually has a methylseleno group at position 4 since selenium forms two covalent bonds, not one like a halogen). 2C-Se is a fullblown hallucinogen of the classical type at 100 mg (not very potent, but definitely active and worthwhile, unlike the flop that was 2C-N). 2C-Se-x (the selenium analogs of the sulfur containing 2C-T-x drugs) drugs would likely be interesting and potent, as would DOSe (which would likely be quite potent).
I've lately had a fascination with morphine-like opioids where some of the oxygens are replaced with either sulfur or selenium ... a place where few opioids have gone to actual human use (sulfur has in a few rare cases like sufentanil and dimethylthiambutene, but selenium hasn't). I'm pretty sure that 14-mercapto-hydrocodone (imagine oxycodone but replace the oxygen in the -OH at position 14 with a -SH), 14-methylthio-hydrocodone (imagine oxycodone but replace that same -OH as before with a -S-CH3), and 14-methylseleno-hydrocodone (replace the same -OH as in the other two with a -Se-CH3) would all be awesome.
The 14-mercapto-hydrocodone would likely be similar in potency and effects to oxycodone. The latter two would likely be similar in effects to oxycodone but more potent (possibly by a significant margin).
So while we can never know what drugs with astatine, polonium, francium, etc heteroatoms would feel like because the elements are unstable, there are stable elements that have not been exploited very much in pharmacology (selenium is particularly attention grabbing because chalcogen atoms are ubiquitous in drugs, psychoactive and non ... oxygen is everywhere, sulfur is occasionally found, but selenium has been ignored [even though it's likely to create relatively non-toxic organic chalcogen containing compounds ... non toxic in that the selenium's presence is unlikely to impart toxic characteristics to most cases where it replaces oxygen or sulfur ... of course highly toxic compounds that contain selenium could be created, like an irreversible inhbitor of cholinesterase that contains selenium heteroatom(s) would be deadly, but not because of the selenium, but because of it's pharmacological action ... sarin is a cholinesterase inhibitor that's irreversible and that's how it kills]). Tellurium is an even heavier chalcogen than selenium (next down in the chalcogen column), but tellurium heteroatoms would be bad news -- there'd definitely be toxicity issues directly from tellurium. Polonium is the next chalcogen down, with an even heavier atomic mass, but whoops.... it's radioactive. I'm sure 14-methylpolono-hydrocodone is potentially a mu agonist, but the alpha particles from the radioactive decay of polonium would shred your mu receptors and plenty of other cells throughout the systemic circulation.... polonium is HIGHLY radiologically toxic when ingested (relatively safe outside the body though even in large quantities since alpha particles from alpha decay cannot penetrate into the body from an alpha emitter outside the body). So selenium, deserves some attention. Tellurium is rightfully ignored for chemical toxicity reasons, polonium because it's a highly toxic radiological poison.