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Strattera - affinities?

C

C10H12N20

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Jul 1, 2004
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It is SNRI, but does anybody have data on DA and 5HT reuptake transporter affinities for this drug?
 
I might be wrong, but I think this study refers to the primary metabolite of Atomotexine

Here it is

To summarize from the article, "Therefore, (R)-[3H]tomoxetine binds to the NE uptake site with high affinity and the 5-HT uptake site with somewhat lower affinity."

Not very conclusive, if it even is what I think it is :\

This study gives the NE affinity as 0.29 nM and the 'other' site as 16 nM. Again, pretty inconclusive.

Several Iodine derivatives of atomotexine have very high affinities for the 5HT transporters according to This study but that is a different compound completely. Interestingly enough, removing the methyl group completely switches the compound to a potent NE reuptake inhibitor.

I am very interested in this, as both me and my girlfriend are on Strattera and we both think it is the greatest single thing that has ever happened to us. I have taken it for over a year as well.
 
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i might start taking it soon, just give it to me straight, is it safe to roll while taking strattera daily
 
Safe? Probably, but it will effect your roll to a degree.. to what degree, we should ask liquidchakra. Oh, and tomoxetine is the old term for atomoxetine.
 
BilZ0r said:
Safe? Probably, but it will effect your roll to a degree.. to what degree, we should ask liquidchakra. Oh, and tomoxetine is the old term for atomoxetine.
Click to expand...


I cant say for ecstacy specifically, but for two other phenethylamines (2C-I and 2C-C) the experience was far more clean and directed than I expected. The ego effects were also greatly reduced, but not the visual effects. I can see alot of people disliking this feeling of control, especially if they took the drug in order to loose control temporarily.
 
Liquidchakra,

Yes Strattera is quite magic. Just from the effects, I suspected that it does have some influence on 5HT, and I am glad to see it is the case. Thank you for that link. I am not sure why it is being prescribed as ADD med, cause it works on anxiety/depression better than any other drug, at least for me. And yes, how about the feeling of "a mild ecstasy-like roll" when the thing kicks in? ;) My friend calls it worksman's ecstasy for that.
 
it made me feel funny when i got prescribed it....then it was concerta.....im about to just get adderall :)
 
Atomoxetine is probably going to become the first line of defense against ADHD in the future I imagine... increases dopamine in the prefrontal cortex, but not so much in the rest of the brain.
 
Tomoxetine didn't do a bloody thing for me. Bupropion (Wellbutrin) was far more helpful (not quite enough for ADD, but certainly helped (and still does) for depression). Methylphenidate was extremely helpful, but required thrice a day dosing and was very 'up and down' in pharmacokinetics. The (d)-amphetamine XR spansule has been perfect--long acting, no peripheral effects, no up and down kinetics and once daily dosing.
 
bilzor,

I thought the primary anti-adhd action of atomoxetine is achieved via selective inhibition of NE reuptake.Are u saying that the drug's effects on dopamine also play an important role?

I have not seen any info on dopamine effects of strattera, but i'll take your word for it.

Does that mean that it has less potential for addiction?
 
There aren't many dopamine transporters in the frontal cortex, the noradrenaline transporter is the way out for dopamine there, so the blocking the NET increases dopamine in the frontal cortex, discussed here.
 
thats all good information. thank you everybody. i've had undianosed ADHD for several decades. now that i'm trying to stay clean, i think i might try strattera, as opposed to the amphetamines or methyphenidate.

is anyone familiar with pemoline and it's effects? just a thought.
 
Pemoline (4-keto-aminorex, 'Cylert') is an interesting one. It is a fabulous looking molecule--a derivative of the much ballyhooed stimulant hit of 1986, 4-methylaminorex (4-MAX)--and is the most researched phenyloxazolidine. This compound was introduced as a treatment for ADHD in children that lasted 12-14 hours (much longer than methylphenidate), but is no longer widely used due to fear of liver toxicity, a risk with all of the phenyloxazolidine compounds that appears to be most severe with pemoline. The risk is still relatively low, but has given pemoline a bad reputation. Virtually no doctors will prescribe this compound, as it has a black box (fatal warning) in the PDR and requires a patient consent form to prescribe. If you get a script, be sure to request a dosage level that will actually do something for an adult. The average child dose was 37.5 mg qD, but a study of Royal AF pilots in the UK revealed 112.5-150 mg of pemoline magnesium to be the optimum dose for cognitive enhancement in the wake of severe fatigue.

As for mechanism of action, some researchers think that the phenyloxazolidines act mainly as reuptake inhibitors at the DAT and substrates at the SERT--they inhibit the reuptake of dopamine, but cause the release of serotonin. One prominent study, however, demonstrated that aminorex and related compounds act as substrates for both the DAT and SERT proteins, rendering them similar to d-methamphetamine in terms of neurotoxicity and cardiac side effects (Zheng et al, 1997, J. Pharm. Pharmacol. 49: 89-96). Another study revealed long-term decreases in tryptophan hydroxylase levels after administration of 4-methylaminorex (a possible sign of serotonergic neruotoxicity, but kind of weak, argument wise), but no signs of dopaminergic toxicity were seen (Hanson et al, 1992, Eur. J. Pharmacol. 218:287-293).
 
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thank you for that. very fascinating. i like to research componds on my spare time. you saved me a lot of trouble. i'm trying to stay as clean as possible, so i'm going to try the strattera.
 
I used to take straterra for my adhd (doctor thought aderall made me lose too much weight) When I first started taking straterra, I thought it was actually helping me pay attention in class. Little did I know that straterra's chemical composition was quite different from aderall (as it wasn't a stimulant) After a few weeks straterra stopped working for me, and I began sleeping in classes as I did before when I was without aderall. After awhile I came to the conclusion that straterra was nothing more than a placebo, and whats funny is that my psychiatrist agreed with me about it being a worthless placebo. Soon enough I was back on aderall, which my body seems dependent on after so many years of daily use and upped dosages. Its not that I abuse it or anything, its just that I've been using it for so long to combat my adhd that now my body needs it in order to stay awake throughout various periods of the day. I've noticed that I'm quite sluggish and somber on the 2 days of the week that I don't take my aderall (saturday and sunday) on those 2 days I'm either falling asleep, sleeping, or waking from an inopprotune nap which annoys me quite alot. I seem to lose such large chunks of time now thanks to aderall, or the lack of it. Its really annoying when I've got a term paper due and I end up just dozing off in the middle of writing it.

Sorry if it sounds like I'm ranting. Its good to know that all those full bottles of straterra on my countertop aren't worthless after all. Peace and one love
 
I think strattera (atomoxetine) can be useful for many people. From what research I did after I had my horrible encounter with it, it seems that it may have a higher risk of peripheral side effects than amphetamine of methylphenidate, especially at times when dosage is increased. I was prescribed strattera for ADD, and it was awful. I had stomach cramps, difficulty sleeping, nightmares, constipation and then diarhea. I felt extremely spaced out all day. The thing it reminded me most of was a VERY bad MDMA hangover. Like I had eaten 6 rolls the night before and then gotten the flu. It didn't get any better so after about a week I stopped taking it, threw it in the trash, and have been taking Adderall XR ever since, with no bad side effects.
 
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I've taken a large variety of antidepressants and stimulants to try to help deal with depression and severe lack of motivation. A few years ago, I got reboxetine (don't know the trade name) from a pharmacy in Europe, as it's not available in the US. This is pretty much strattera's predecessor. It seemed like basically a sugar pill, though I was using very large amounts of meth daily, so I dunno... too expensive though. Anyway recently I tried strattera, primarily as an antidepressant, with hope it would have motivating effects. It didn't seem to do much, but I only took it a few weeks before I decided it made me feel way too SHITTY. I just felt physically nasty while taking it, and had issues eating, nausea, etc... Kind of like dogtoy. So I went back to my semi best friend Zoloft. Since then I've added in time-release methylphenidate (not concerta, the other generic stuff), which isn't too spectacular on its own, but then I added provigil on top of THAT, and now hey, things seems better. Provigil is awesome. The doctors won't prescribe me amphetamine because of my history with stimulant addiction (and I honestly wouldn't let them give it to me if they wanted to).

Anyway, heard good things about strattera too though..
 
Possibly off topic......but atomoxetine is efficacious in the treatment of ADHD but it doesn't raise dopamine levels in the striatum or nucleus accumbens. But it does raise it 3 fold in the pre-frontal cortex! Ahh, now in the PFC though the main mechanism of DA uptake is through the Norepinephrine transporter....and atomoxetine is a SNRI.
 
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