Super-potent N-benzyl Phens?

[fastandbulbous]

A rumour says that Alcon Switzerland have studied these and similar compounds as anti glaucoma agents.

Well alpha-methyl BOB (beta-methoxy DOB) has been investigated as an anti-glaucoma agent as well, so that would be any pharmaceutical company impetus for divorcing 5HT2a agonism from hallucinogenic effects (well the money involved from marketing them to be strictly honest!).

I always thought that all of the phenethylamine (& amphetamine) 5HT2a agonists were also equally active at 5HT2c receptors as well, which rather muddies up the picture regarding the PEAs. There wasn't a PEA/alpha methylPEA that acts exclusively at 5HT2a, well at least not last time I looked (although they're not as promiscuous as the tryptamines when it comes to receptors, or a complete tart like LSD, which will have it away with just about any receptor!)

 

[vecktor]

Well alpha-methyl BOB (beta-methoxy DOB) has been investigated as an anti-glaucoma agent as well, so that would be any pharmaceutical company impetus for divorcing 5HT2a agonism from hallucinogenic effects (well the money involved from marketing them to be strictly honest!).

I always thought that all of the phenethylamine (& amphetamine) 5HT2a agonists were also equally active at 5HT2c receptors as well, which rather muddies up the picture regarding the PEAs. There wasn't a PEA/alpha methylPEA that acts exclusively at 5HT2a, well at least not last time I looked (although they're not as promiscuous as the tryptamines when it comes to receptors, or a complete tart like LSD, which will have it away with just about any receptor!)

true, there are not as far as I am aware any highly selective 2a agonists of any type. The trouble being that the 2c and 2a receptors are highly similar. I am waiting to see data for the asymetric benzo furan/chromans, which might offer some selectivity in the right 2a over 2c way. these compounds have been made by a glennons group I think and have a chromane ring on one side and a furan on the other.

there are selective 2c antagonists though. strong 5HT2c agonism does not seem to be desirable.
the fully aromatic dragonflies are mildly selective for 2c over 2a which isn't the right way round.
2c is pretty much irrelevent for activity as the administration of selctive 2c antagonists doesn't abolish the descriminative stimulus. perhaps when some of the selective 2c antagonists or inverse agonists hit the market in the near future some interesting experimentation can be carried out.

 

[Helios.]

I don't think BOB-DOB would be a great thing to use for eyedrops.

just my 99 cents.