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Where to get Suboxone binding affinity data?

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capRx

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May 19, 2007
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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:
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.
 
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