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Where to get Suboxone binding affinity data?

C

capRx

Bluelighter
Joined
May 19, 2007
Messages
107
I always hear the debate about the naloxone in the Suboxone is inactive because of the high binding affinity of buprenorphine, but no one ever lists the binding affinity for either! So I am trying to figure out the binding affinity data for buprenorphine and naloxone, but wherever I look I get different data. I've seen ki value at the MOR for buprenorphine ranging from .08-.3 and .8 for naloxone. Is there a database that I can look at that lists these values for naloxone, buprenorphine, and other drugs? Thanks!

-cap
 
You can try this:

http://pdsp.med.unc.edu/pdsp.php

They do seem to vary quite a lot, it's hard to compare two substances unless they're tested under the same conditions, so you really need a single source with values for both.
 
Slapdragonx said:
Buprenorphine:

Mu: .21-1.5 Ki
Delta: 1.6-4.5 Ki
Kappa: .62-.8 Ki

Naloxone:

Mu: .66-3.7 Ki
Delta: 19-120 Ki
Kappa: 1.1-66 Ki

ChEMBL is a great place to look for affinities:
Click to expand...

Thank you so much! Are Ki values always in a such a varying range? I mean .21-1.5 for the MOR is a huge difference.. And where did you find this information on the website. I've tried searching it, but couldn't find anything.
 
Last edited:
skillet said:
You can try this:

http://pdsp.med.unc.edu/pdsp.php

They do seem to vary quite a lot, it's hard to compare two substances unless they're tested under the same conditions, so you really need a single source with values for both.
Click to expand...

True. that would make sense why there is such a large range for each one.. thanks for the insight, and the website!
 
capRx said:
Thank you so much! Are Ki values always in a such a varying range? I mean .21-1.5 for the MOR is a huge difference.. And where did you find this information on the website. I've tried searching it, but couldn't find anything.
Click to expand...

They are tested as to how much they can displace certain radiolabelled compounds from the receptors.
 
Slapdragonx said:
Buprenorphine:

Mu: .21-1.5 Ki
Delta: 1.6-4.5 Ki
Kappa: .62-.8 Ki

Naloxone:

Mu: .66-3.7 Ki
Delta: 19-120 Ki
Kappa: 1.1-66 Ki
Click to expand...

Also, I just wanted to point out, for those who may be confused by the values (like I was initially)...

"The smaller the Ki, the greater the binding affinity" (source)
 
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