johanneschimpo
Bluelighter
P.S.: he is using standard notation. a comma ( , ) means thousand, and a period ( . ) means decimal
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N&PD Moderators: Skorpio
Dopaminergics.
- Thread starter narutokun
- Start date
Ham-milton
Bluelighter
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- Jul 20, 2007
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Yeah, comma's are far more common than periods for marking the difference between 100's and 1000s.
At least I think it is, in scientific literature anyway.
is that muttering I hear? "just another example of the US trampling on the rest of the world"I hope we have got past the whole comma versus period notation debate. In my opinion using commas to separate thousands is redundant in any case, counting the zeros is fine.
back on topic.
I think that GBR 12909 is the most DA selective of the dopamine reuptake inhibitors 'commonly'found. however it is not just a DAT inhibitor and in reality is not very selective.
Nomifensine which is widely used as a DAT inhibitor experimentally is also an effective NE reuptake inhibitor.
Some of the more exotic tropanes are much more selective DAT vs NET vs SERT. Meltzers group came up with a few very selective ligands based on the 3-3,4-dichlorophenyl tropane structure with DAT/SERT >1000 and DAT/NET >200.
Bridging the tropanes also increases selectivity. these substances are not widely available.
additionally DAT affinity does not always correlate with extracellular DA levels as their are several sites on the DAT protein and some ligands bind to sites that are not involved in DA transport. There is also strong evidence that DAT exists in several populations some which are labelled with high affinity by dopamine and others which are labelled with WIN 35,428 and which might not be efficient at transporting DA. This appears to be related to the number of cycles DAT has been through.
It seems unlikely that it is possible to tell whether something is more DAT or NET selective by tasting it as some have suggested.
V
fastandbulbous
Bluelight Crew
Yes. It's the active metabolite that does all the appetite supressing, that being N-ethylcathinone. You have to lop off one of the ethyl groups for the active compound (I got some a while ago - N-ethylcathinone/ethcathinone - and it brought back memories of the much beloved Tenuate Dospan; Chalkies or tombstones to those aquainted with them!). That's why I can't quite grasp why a pyrrolidine group is so efficient, such as with 2-(1-pyrrolidino)propiophenone & MDPV, when substituted into the amine position. I mean dimethylamphetamine is a non starter & all the tertiary amine amphetamines, even benzphetamine with the easily removed N-benzyl group, are no great shakes in the stimulant stakes. Stick a keto group on there and suddenly all the rules go out the window. Best chain length - 5-6 carbons, Most active N-substituted groups - pyrrolidino. Why is the keto group so important when dopamine doesn't have any substitutions into the beta carbon atom? That should work for noradrenaline, with the beta-hydroxy group on noradrenaline's ethylamine side chain, but why's it so important to dopamine?
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Ham-milton
Bluelighter
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Only PEAs with a beta-ester will (I think)
narutokun
Bluelighter
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Yes that's the case.johanneschimpo said:I don't know if you're aware of this, but there are two different types of notation. For example, comparing the US and a random European country (I know it varies everywhere), the comma and the decimal mean the opposite thing.
ex: four and a half
US: 4.5
Europe: 4,5
ex. fifty thousand
US: 50,000
Europe: 50.000
Right?
I know you know this, I think you just want to be difficult.
It appears the convention that you use in Brazil (Brasil
) is opposite to the one used on that chart. So for convenience, read each period as a comma (. = ,) and each comma as a period (, = .)
swilow
Bluelight Crew
^Lol.
swilow
Bluelight Crew
^You.
