• N&PD Moderators: Skorpio

Dopaminergics.

narutokun said:
Great chart if it is indeed accurate, but why do they put so many zeros after the 10s, initially I was reading 10.000 instead of 10. Getting a closure on this then, what is the best compound with the most dopamine release and reuptake with the least NE release and reuptake?

because 10.000 = 10,000 = 10000 = ten thousand.
 
narutokun said:
How bad is it of just pointing it out for me? :|

When the answers are right in front of you and you're asking us to highlight them for you (and they're even highlighted within the chart), it just strikes of laziness. If you can talk someone else into it, more power to you.
 
There are lots of direct dopamine agonists, for example:

N-Alkylated 2-aminotetralins: central dopamine-receptor stimulating activity
Uli Hacksell, Uno Svensson, J. Lars G. Nilsson, Stephan Hjorth, Arvid Carlsson, Haakan Wikstroem, Per Lindberg, Domingo Sanchez
J. Med. Chem.; 1979; 22(12); 1469-1475.

But for some reason are direct dopamine agonists usually not recreational, and only very few are self-administered in rats. Maybe a dopamine autoreceptor antagonist could be the answer to recreational dopamine without body load and come down.
 
If you like vomiting lots, then you'll probab;y love DA agonists.
otherwise, not so much ;)
 
There was a human report/warning of 2-aminotetralin here at BL some time ago, and it was anything but pleasant and the guinea pig ended up in the hospital. In other words I would proceed with very much caution if experimenting with aminotetralins.
 
I am guessing but I think alot of the body load comes from increased serotonin release and reuptake inhibition too. I think the serotonin response for sure has most to do with the increase in temps associated with MDMA. Does MDMA cause a increase in heart rate and BP like other a-methyl PEA's?
 
that chart is nice...though absent are some common DARIs such as Methylphenidate (also curious to Ethyl variant), MPDV, Amineptine, as well as CFT, CPT, amfonelic acid...anyway would have liked to see those as well on such a chart amongst others

of all said compounds that have been bioassayed what is the most selective DARI?
 
^I also wanted to see methylphenidate's data on that chart.
johanneschimpo said:
because 10.000 = 10,000 = 10000 = ten thousand.
I don't know, the chart is flawed then, because using different notations without standardizing it on the same paper will only cause confusion. Whoever translated the figures onto the chart forgot to standardize. For me at least, 10,000 means 10. While 10.000 means ten thousand which would be the same as 10000. If one takes a look he will see that on the chart he uses commas, dots and neither to represent the same thing, which can be obviously confusing; if 10,000 really means 10000 like you are saying, that is. Look that once he puts in 1000 instead of 1,000, among other examples that can be taken from the chart. Can anyone confirm this? Not using standard notations on the same fucking page is obviously leading to different interpretations on the figures.
 
10,000 no matter how written is always 10,000 on that chart , not 10 or otherwise as it was the upper limit on most of the testing and notable noted as always GREATER THAN 10,000
 
It is pretty obvious that as they are EC50s that 10,000 or 10000 or whatever is 10^4 or ten thousand, a big number rather than a small number with rediculous precision. :\
I will practically guarantee that no-one in the target audience of the paper was confused by the notation.
and what the big number actually means is that they got bored trying to get an EC50 and gave up at somewhere around the 10 micromolar concentration.
The only thing I found of interest in that chart is that diethylpropion has virtually no activity in vitro so it must be the metabolite that is active, something which I hadn't figured.
Does anyone with access to the original paper know whether the chart is a meta collection of different reported figures from different papers or whether all the substances were assayed using the same experimental?
Bear in mind that different experimental conditions give widely differing results even for the same substance.

dopamine agonists= not fun as a general rule.
dopamine reuptake inhibitors = sometimes fun
I think have posted on this subject before on this board.
 
LuxEtVeritas said:
10,000 no matter how written is always 10,000 on that chart , not 10 or otherwise as it was the upper limit on most of the testing and notable noted as always GREATER THAN 10,000
Note that phendimetrazine lists 19000 in the first collumn, a value that is higher than 10000. Standardized numerical notation is imperative imo. Regardless of the target audience or whatever. :|
 
Anyway, is there any other option for reducing all this cardiac stimulation/discomfort besides obviously not taking the drug or taking it along with a benzodiazepine for example? What about all this general idea of taking a CNS stimulant along with a depressant, is it really actually safe? I've heard many different opinions on that matter so I'm sort of confused. :\
 
^

firstly i bet it is a meta collection and makes comparison not all that meaningful
second indeed it does not account for active metabolites which as stated in regard to diethylpropion which indeed is a pro-drug (same with phendimetrazine) renders this chart less real world useful once more....think others such as sibutramine et al
 
I was wondering why they leave some off as >10K and then others give exact-ish figures above 10k.
 
^Yes that's what I thought, I think who compiled the chart didn't standardize the numeric notations either, hence the confusion I was making before as well. lol. 8(
 
LuxEtVeritas said:
because again it is likely a meta-collection using a compiling of a different studies and some may have had higher upper limits than 10k

Oh, yeah, that would make sense. It would be quite a project otherwise.
 
DadeMurphy said:
Other way around.
It goes tyrosine -> DOPA -> dopamine -> NA -> adrenaline.

So dopamine doesn't exactly "break down" to NA, but it can be converted to NA by cells containing dopamine b-hydroxylase ie. DAergic neurons.
Principle product of DA metabolism is homovanillic acid.

Ah, okay. I think I got confused; adrenaline itself is not psychoactive yes, but induces the relase of nor-adrenaline which is...? Is that compltely wrong? (the question is not realted to your response as such, but more to where I think I may have been coming from in my response...)
 
Yeah epinephrine isn't psychoactive but norepinephrine is. Stressful events will trigger the release of both. Injecting epinephrine should not release much NE as a consequence I should think, it would be dangerous to have a autoinduction cycle where epinephrine release triggers NE release which triggers epinephrine release which.. etc.
 
narutokun said:
^I also wanted to see methylphenidate's data on that chart.

I don't know, the chart is flawed then, because using different notations without standardizing it on the same paper will only cause confusion. Whoever translated the figures onto the chart forgot to standardize. For me at least, 10,000 means 10. While 10.000 means ten thousand which would be the same as 10000. If one takes a look he will see that on the chart he uses commas, dots and neither to represent the same thing, which can be obviously confusing; if 10,000 really means 10000 like you are saying, that is. Look that once he puts in 1000 instead of 1,000, among other examples that can be taken from the chart. Can anyone confirm this? Not using standard notations on the same fucking page is obviously leading to different interpretations on the figures.

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 (, = .)
 
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