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Binding aiffinity (Ki) of Cocaine

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Bluelighter
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Oct 29, 2012
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Studying research chemicals
Im not really sure if its the right place to post this... I dont fell like its Advanced drug discussion but its definitely not Basic drug discussion and the Intermadiate drugs discussion AKA Other drugs is for harm reduction only... so... ....

Im actually studying Phenyltropane drugs and I need a comparation between the binding affinity (Ki) of Cocaine and the other Phenyltropane im studying. The problem is I cant find the Ki of Cocaine anywhere I tried Wikipedia, pubmed, google, forums...

Could someone help me

I need the Ki in nM for the transporter of DA, NE and 5-HT.

For exemple : (–)-2β-Carbomethoxy-3β-(4-bromophenyl)tropane better known as RTI-51 have a Ki of... DA: 1,69nM | 5-HT: 10,6nM | NE: 37,4nM

So could someone tell me the Ki of Cocaine please.

Also I remember seeing someone somewhere post a link to a website the have an incrediably large list of chemical with the Ki of all substance, if anyone know what im talking about I would really like to know this website again.

Big thanks !!!
 
Here you go: http://www.cogsci.ucsd.edu/~pineda/COGS260/cocaine/5-HT and cocaine addiction.pdf

http://www.if-pan.krakow.pl/pjp/pdf/2010/6_1005.pdf

Their source: Grabowski J, Rhoades H, Elk R, Schmitz J, Davis C,
Creson D, Kirby K: Fluoxetine is ineffective for treat
-
ment of cocaine dependence or concurrent opiate and co
-
caine dependence: two placebo-controlled, double-blind
trials. J Clin Psychopharmacol, 1995, 15, 163–174

Also: .
Koe BK: Molecular geometry of inhibitors of the uptake
of catecholamines and serotonin in synaptosomal preparations
of rat brain. J Pharmacol Exp Ther, 1976, 199, 649–661

:)
 
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Not really a question re the OP topic, but is the Ki the same as (Michaelis-Menten kinetics) Km? Or how are they related?
By the looks a substrate (to its receptor), its Km is experimentally determined, whereas Ki is not. ( ? ).

Cheers.
 
tyrael said:
Not really a question re the OP topic, but is the Ki the same as (Michaelis-Menten kinetics) Km? Or how are they related?
By the looks a substrate (to its receptor), its Km is experimentally determined, whereas Ki is not. ( ? ).

Cheers.
Click to expand...

Km is a constant to describe enzyme kinetics where you have a substrate a reaction and a product. Ki is a measure of affinity between a chemical and a protein, and is a ratio of how quickly the two associate (Kon) and dissociate (Koff). Both constants are determined experimentally, they just concern different processes.
 
I have my own question about cocaine. I heard a large part of the molecule makes it both hydrophilic and hydrophobic at the same time (yeah, I probably misunderstood something) and that it reaches the brain faster because of this property...?

Please tell me there is something vaguely similar to what I'm talking about.
 
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