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Pharmacology Where the fuck can I find the ic50 for DAT and NAT for dextro (S)-meth?

This thread contains discussion about a Pharmacology-related topic
MephedroneCandy

MephedroneCandy

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Mar 18, 2022
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I found IC50 for taar1, for MAO, for everything except reuptake transporters!!! Even in bindingdb.

Edit: Solution to the exercise
Racemic Methamphetamine: DAT Ki=0.46 μM, NAT Ki=0.11 μM
S isomer 17 times more potent at DAT and twice at NAT than R isomer.

2/0.46=(1/17x)+1/x

S isomer DAT ki = 0,24 μM

2/0.11=(1/2x)+1/x

S isomer NAT ki = 0,08 μM

So it is true. R methamphetamine really has negligible affinity for DAT like we knew.

And the S isomer still is disbalanced for NAT.

Destromethamphetamine has a DAT/NAT affinity ratio identical to amphetamine contrary to popular belief (1:3)!!!!! Even though it probably release more dopamine thanks to sigma1 affinity, which in methamphetamine case, helps the reversal of DAT,
 
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They don't bind to DAT or NET, they bind to the transports. Or, I GUESS you might want DAT and NET affinity, but that isn't was produces the stimulant activity. And you specifically want the LESS potent isomer?

Unusual request, I don't think anyone has studied any of them, to the best of my knowledge.
 
AlsoTapered said:
They don't bind to DAT or NET, they bind to the transports. Or, I GUESS you might want DAT and NET affinity, but that isn't was produces the stimulant activity. And you specifically want the LESS potent isomer?

Unusual request, I don't think anyone has studied any of them, to the best of my knowledge.
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It is known the affinity to DAT and nat of amphetamine and a lot of RCs. Why not methamphetamine? Dextromethamphetamine releases more dopamine than levo why are you saying it is the less potent? Levomethamphetamine is used in nasal decongestants. DAT and NAT are the transporters.

DAT = Dopamime transporter
NAT = Noradrenaline transporter
 
I found DAT and NAT affinities for racemic meth (Ki=0.46 μM and Ki=0.11 μM). But I want to know how much dextromethamphetamine is more balanced on DAT.
 
(S) is the potent isomer. In old currency you might term it 'dextro' but we haven't for 30+ years. I PRESUME you meant to say dextro.
 
AlsoTapered said:
(S) is the potent isomer. In old currency you might term it 'dextro' but we haven't for 30+ years. I PRESUME you meant to say dextro.
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Who gives a fuck

It's still used

Everyone gets it

Yes of course "destro" is a typo
 
AlsoTapered said:
(S) is the potent isomer. In old currency you might term it 'dextro' but we haven't for 30+ years. I PRESUME you meant to say dextro.
Click to expand...
Yes sorry. I was confused by r=right. And by destro I mean dextro because In my mother tongue it is written like this.
 
Mjäll said:
What? You just said no-one has studied them. Now you say it IS known
Click to expand...

In the mean time I found a paper - I was surprised that someone WOULD study it, but there you go. It WAS trialed as an anoretic which I hadn't realized, so I was looking at those papers. I still am because it's always worth a read.
 
AlsoTapered said:
In the mean time I found a paper - I was surprised that someone WOULD study it, but there you go. It WAS trialed as an anoretic which I hadn't realized, so I was looking at those papers. I still am because it's always worth a read.
Click to expand...
Send it. Im interested anyway
 
AlsoTapered said:
In the mean time I found a paper - I was surprised that someone WOULD study it, but there you go. It WAS trialed as an anoretic which I hadn't realized, so I was looking at those papers. I still am because it's always worth a read.
Click to expand...

Now you're still talking about the isomer he didn't ask about right
 
MephedroneCandy said:
I found DAT and NAT affinities for racemic meth (Ki=0.46 μM and Ki=0.11 μM). But I want to know how much dextromethamphetamine is more balanced on DAT.
Click to expand...
Assuming it is racemic, doesn't it mean I can do 0.46/2 uM to have its DAT Ki? Since the R isomer should not have affinity for DAT? But the NAT affinity remains an incognita. If you send the paper that says the affinity for NAT of the r isomer we could calculate the difference.
 
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Not quite. (R) methamphetamine is still classed as a stimulant so unless it's action is mediated by another process, I presume it has some affinity. It's just not as easy to find. Levomethamphetamine IS in the Merck Index but not with much detail and only a few references which I am looking into.
 
AlsoTapered said:
Not quite. (R) methamphetamine is still classed as a stimulant so unless it's action is mediated by another process, I presume it has some affinity. It's just not as easy to find. Levomethamphetamine IS in the Merck Index but not with much detail and only a few references which I am looking into.
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Its action is mediated mainly by noradrenaline release, like ephedrine.
 
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