Cyproheptadine binding affinity table

[Makrosky]

Hey guys,

I unexpectedly came across a paper on pubmed that included a table comprehensively describing cyproheptadine receptor affinities. I'm not sure if they created the binding profile ex-professo for the paper or they took an already existent one, they say this but I don't understand what that means exactly:

Cyproheptadine HCl and pizotyline maleate and were
examined in a number of different radioligand binding assays
by the NIMH Psychoactive Drug Screening Program; PMMA
was examined at 5-HT2A and 5-HT2C serotonin receptors. The
agents were initially screened several times at a concentration
of 10,000 nM; if an agent produced > 50% inhibition, a Ki
value was determined in quadruplicate. Where an agent
produced < 50% inhibition of binding, a Ki of > 10,000 nM
is reported. Assay details and standard binding protocols can be
found at:http://pdsp.cwru.edu/pdspw/binding.php.

Since they are radioactive binding assays it's in vitro.
(link to the study : http://www.sciencedirect.com/science/ar ... 5705003126)

And here is the table:


I don't understand either why there's a column called "Cyproheptadine" and another one called "HCL". Does that mean cypro can be in another chemical form that is not HCL ?

Interesting to see the effects on adrenergic and beta-two adrenergic receptors....

Is this good info ? Comments welcome!

Also I found this : http://pdsp.med.unc.edu/pdsp.php where you can search for specific affinities for the receptors you want.

 

[Such_Saturation]

The values from wikipedia are all different, and I remember finding different ones all over

 

[Makrosky]

The values from wikipedia are all different, and I remember finding different ones all over

I was thinking exactly the same. Wikipedia source is the same as for the table I posted...

But I think on wikipedia they only took human receptors while in the paper they took all of them? It's not described.

Don't really know how this works.

 

[Such_Saturation]

I think CR is cloned rat but it's only a few of those.

 

[Makrosky]

Feedback anyone ?

I don't really understand the table. The lower the affinity, the more it antagonizes ? Because H1 and H2 are very low and that should be the main effect of cypro.

 

[Such_Saturation]