Photomodulation of the 5-HT2A Receptor by a Light-Controllable N,N-Dimethyltryptamine Derivative

[Snafu in the Void]

Very interesting study:

https://onlinelibrary.wiley.com/doi/full/10.1002/anie.202203034

we designed a set of photoswitchable ligands based on the classical psychedelic N,N-dimethyltryptamine (DMT). By incorporation of the DMT-indole ring into the photoswitchable system, we obtained red-shifted ligands which can be operated by visible light. Among these azo-DMTs, compound 2 h (“Photo-DMT”) stands out as its cis isomer exhibits DMT like activity while the trans isomer acts as weak partial agonist. Such a cis-on “efficacy switch” substantially expands the pharmacological toolbox to investigate the complex mechanisms of 5-HT2AR signaling.

 

[izo]

not available via scihub, anybody got a pdf?

 

[realgar]

not available via scihub, anybody got a pdf?

It's an open access article. No need to use Sci-Hub.

https://onlinelibrary.wiley.com/doi/epdf/10.1002/anie.202203034

 

[Skorpio]

That's very cool. I feel like it might be a simpler behavioral tool than DREADDs due to the lack of a need for genetic modulation.

Still seems like one of those fiber optics in the brain type deals, so this drug is for the rodents.

Also no in vivo characterization was done, so it's not sure that it would get to the brain if administered iv.

Either way both cool and super novel, good catch @Snafu in the Void