6 replies to this topic

[VICREP]

I have been very intrigued by the potential of selective Kappa antagonists for a while, mainly for their potential in restoring hedonic tone.

 

LY2456302 seems like it could be a viable option, however there are no online sources for it, and I'm wondering if someone could point me in the right direction to where I may be able to have it synthesized?

 

Thank you

[Area-1255]

You need a lab or contact someone who can do custom synthesis, you'll need a university address or another "registered" location to ship to...usually sigma-aldreich type places can prove to be viable sources.

[VICREP]

You need a lab or contact someone who can do custom synthesis, you'll need a university address or another "registered" location to ship to...usually sigma-aldreich type places can prove to be viable sources.

 

Thanks Area-1255

 

I'm not sure how I would go being able to organize a chem synthesis then. I guess I'll have to keep my eyes open on these forums, hopefully someone else with the connections becomes interested in a group buy for a Kappa Antagonist

[Area-1255]

 

You need a lab or contact someone who can do custom synthesis, you'll need a university address or another "registered" location to ship to...usually sigma-aldreich type places can prove to be viable sources.

 

Thanks Area-1255

 

I'm not sure how I would go being able to organize a chem synthesis then. I guess I'll have to keep my eyes open on these forums, hopefully someone else with the connections becomes interested in a group buy for a Kappa Antagonist

 

Why not just get amentoflavone? It's a potent natural kappa antagonist.

Flavonoids as Opioid Receptor Ligands: Identification and Preliminary Structure–Activity Relationships

Edited by Area-1255, 22 March 2015 - 05:47 PM.

[VICREP]

You need a lab or contact someone who can do custom synthesis, you'll need a university address or another "registered" location to ship to...usually sigma-aldreich type places can prove to be viable sources.

Thanks Area-1255

I'm not sure how I would go being able to organize a chem synthesis then. I guess I'll have to keep my eyes open on these forums, hopefully someone else with the connections becomes interested in a group buy for a Kappa Antagonist

Why not just get amentoflavone? It's a potent natural kappa antagonist.
Flavonoids as Opioid Receptor Ligands: Identification and Preliminary Structure–Activity Relationships

Interesting......

"In contrast, amentoflavone had good activity at the κ opioid receptor with a Ke of 490 ± 150 nM"

How does this affinity compare to that of other kappa antagonists?

[Area-1255]

 

 

 

You need a lab or contact someone who can do custom synthesis, you'll need a university address or another "registered" location to ship to...usually sigma-aldreich type places can prove to be viable sources.

Thanks Area-1255

I'm not sure how I would go being able to organize a chem synthesis then. I guess I'll have to keep my eyes open on these forums, hopefully someone else with the connections becomes interested in a group buy for a Kappa Antagonist

Why not just get amentoflavone? It's a potent natural kappa antagonist.
Flavonoids as Opioid Receptor Ligands: Identification and Preliminary Structure–Activity Relationships

Interesting......

"In contrast, amentoflavone had good activity at the κ opioid receptor with a Ke of 490 ± 150 nM"

How does this affinity compare to that of other kappa antagonists?

 

It's impressive considering it's a natural compound, but not the most potent affinity in the book...it would technically be classed as "moderate" affinity but because the opioid receptors are a "superfamily" and have molecular jurisdiction over 100s of physiological processes, that's pretty eye-opening for something natural.

[VICREP]

It's definitely a notable find. Probably not going to have anywhere near the magnitude of effect I would like from a Kappa antagonist though.