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The Official "Stablon is a smart drug" thread

Okay, I could use some help from some of the experts on here...I found the following study which seems like it's saying tianeptine sodium (37.5 mg/day) is no better than zoloft/sertraline (50 mg/day) for depression and that there really isn't much difference in side effects - Invalid Link Removed. Am I interpreting that correctly? If so, I'm curious as to why more people just don't take sertraline (besides the usual ssri stigma).

Ssri's negatively effect libido and orgasm (cause anorgasmia). Stablon/Tianeptine does the opposite.

SSRI's negatively effect concentration in many, Tianeptine does the opposite.

I don't think it's about stigma. Tianeptine just has a host of more effective, overall results. It's just superior.
 
Well, I'm not saying ssris arent effective, but erasing depression through the complete removal of all emotion isn't my preferred choice of treatment.

Erase all hope of having a normal orgasm after a few weeks also, especially at higher doses. And learn to appreciate constant stomach discomfort and loose stools too, because that's usually next. Not sure about long-term Tia, but it might promote the opposite (constipation.)

Like you say, zeroing emotions is useful when emotions are predominately negative (depression.) But what about after the challenge has passed and the potential for a positive outlook returns? It's hard to even recognize when that inflection occurs zeroed-out on SSRIs.
 
The Official "Stablon is a smart drug" thread

And then there's SNRI's, known to cause panic attacks / mania. (I.e.: Effexor), and horrible withdrawals.
 
I wish T worked for me in regards to depression and mood, as the reports I've read are fantastic! I have tried every form, at every dose, and all I get is spaced out and lethargic.

Oh, and constipated.
 
Erase all hope of having a normal orgasm after a few weeks also, especially at higher doses. And learn to appreciate constant stomach discomfort and loose stools too, because that's usually next. Not sure about long-term Tia, but it might promote the opposite (constipation.)

Like you say, zeroing emotions is useful when emotions are predominately negative (depression.) But what about after the challenge has passed and the potential for a positive outlook returns? It's hard to even recognize when that inflection occurs zeroed-out on SSRIs.
Yeah, I ended up constipated lol.
 
I got Stablon, and I got a powder from reputable sources of both varieties. Had such high hopes!
 
Looking for some ideas on things that might stack safely with tianeptine. Magnesium just doesn't seem to be cutting it anymore with reducing the anxiety (or too much energy) provided by 25 mg of tianeptine sulfate. Strangely enough, I also don't seem to be able to take magnesium before bed anymore because now it seems to provide energy instead of sedation...which I read is typical when you are no longer deficient. If I take 50 mg of tianeptine sulfate, then it's much more calming and mood lifting...but the cost to use it doubles. I'm thinking about trying l-theanine with it but am unsure how the two might combine since tianeptine modulates currents between the ampa and nmda receptors; and l-theanine is an agonist of the ampa receptor and antagonist of the nmda receptor...however, since theanine is believed to also increase dopamine maybe together they'd provide a really good mood boost. Thoughts?

edit: apparently zinc augments antidepressants - Invalid Link Removed. They used it with ssris but maybe it will augment tianeptine too. Will try adding a multivitamin and see if that helps.
 
Yup! NMDA is actually very important for mood. Sure less of it leads to dissociation and less emotions but at the same time, more of it allows for positive emotional experience. NMDA is also what D-Aspartic Acid activates to boost testosterone/libido.

So, for mood benefits it would be better to take a nmda agonist (like l-theanine) than a nmda antagonist (like magnesium)? Albeit, both being relatively weak in that department.
 
Generally yes, though it depends on your emotional state. It also depends on other factors like how much GABA you have etc. Magnesium is still a necessary mineral, but too much tends to inhibit cognitive functions a little bit, and NMDA-receptors have a critical role in memory, so that makes sense. Even people with borderline personality disorder often show LOW NMDA activity, and as well schizophrenia is characterized by NMDAR-deficits. So its clear its linked mainly with cognitive functions, which is why even though some get a mood benefit from antagonists, that effect is short lived or has too many side-effects. If you have uncontrolled panic disorder on the other hand, NMDA activation may not be the way to go.

Theanine probably exerts its anti-depressant effects through NMDA, and anti-anxiety through GABA activation mostly though.
Lysine is a perfect sidekick to Theanine, and helps anxiety tremendously. It also increases mood to an extent.

Great info. Thanks!
 
The Official "Stablon is a smart drug" thread

Cymbalta did me well for a year or so, but the withdrawals were awful.

Likewise. Effexor got my a$$ in gear and out of a depression I was in over 10 yrs ago, but coming off it was horrible. And even though I was pulling lots of booty back then, I could rarely finish. These days things are much different I went 4 times yesterday with my girl lol
 
Generally yes, though it depends on your emotional state. It also depends on other factors like how much GABA you have etc. Magnesium is still a necessary mineral, but too much tends to inhibit cognitive functions a little bit, and NMDA-receptors have a critical role in memory, so that makes sense. Even people with borderline personality disorder often show LOW NMDA activity, and as well schizophrenia is characterized by NMDAR-deficits. So its clear its linked mainly with cognitive functions, which is why even though some get a mood benefit from antagonists, that effect is short lived or has too many side-effects. If you have uncontrolled panic disorder on the other hand, NMDA activation may not be the way to go.

Theanine probably exerts its anti-depressant effects through NMDA, and anti-anxiety through GABA activation mostly though.
Lysine is a perfect sidekick to Theanine, and helps anxiety tremendously. It also increases mood to an extent.

What type of lysine dose are you thinking? Around a gram?
 
Generally 1.5 grams at the very least, preferably on an empty stomach. Look up this study "Lysine fortification reduces anxiety and lessens stress in family members in economically weak communities in Northwest Syria".
I myself find most benefit with 2.5 grams - 3 grams at night though.
Also, here's a good study which is short enough to quote.

Not only that, Lysine also shows central activity as a depressant, enhancing substrate binding at GABA receptors. A mechanism resembling the way barbiturates work. This probably relates to it's adrenal influence but could be a completely separate anxiolytic mechanism.

I've taken large doses of Lysine before in an effort to abort colds, and never noticed overt sedation. However, I've never stacked it with a GABAnergic before either.
 
Not only that, Lysine also shows central activity as a depressant, enhancing substrate binding at GABA receptors. A mechanism resembling the way barbiturates work. This probably relates to it's adrenal influence but could be a completely separate anxiolytic mechanism.

I've taken large doses of Lysine before in an effort to abort colds, and never noticed overt sedation. However, I've never stacked it with a GABAnergic before either.

Did you notice it to help anxiety?
 
Did you notice it to help anxiety?

No, not that I noticed. I did have to run to the bathroom the next morning though, lol. So I've learned my lesson! Higher doses of L-Lysine (the base and HCl) seem well tolerated, just like higher doses of ascorbic acid, but ONLY when I'm truly sick. If not, even moderate doses aren't well absorbed, so prophylactic value is low IMO. A few grams a day is plenty.

But you know what amino does help? A few grams of L-Methionine (which I was not expecting) but 2.5+g produces a distinct relaxation for several hours.
 
Actually L-Lysine's anti-anxiety effects are greatly related to its anti-serotonin effect at the 5-HT4 receptors.

That's right! I had forgotten about that one. This might even be the primary contribution to it's relaxing effect. Good catch, Area.

So yeah, Lysine has multiple anti-anxiety mechanisms. I take 2g a day with 2g Proline, mostly for connective repair.
 
For anyone that has tried tianeptine sulfate, have you found it better for depression to take one larger dose in the morning or splitting that dose and taking half in the morning and half in the afternoon?

Edit: the reason I ask is that I've been taking 25 mg in the morning and afternoon but have developed some insomnia issues. Therefore, I'm now wondering if maybe just taking both (50 mg) in the morning would provide lasting effects through the day but maybe not result in the same issues with insomnia.

I haven't been getting insomnia with it but my sleep hasn't been as restorative - in fact, my deep sleep % on the Sleep as Android app has decreased a bit since starting tianeptine sulfate (25 mg once per morning). After research I learned that mu opioid agonists (which tianeptine, and its effects are likely downstream from this) can affect sleep architecture. Studies for reference:

Morphine Inhibits Sleep-Promoting Neurons in the Ventrolateral Preoptic Area Via Mu Receptors and Induces Wakefulness in Rats

Mu opioid receptor regulation and opiate responsiveness.

The effect of opioids on sleep architecture.

Acute intravenous administration of morphine perturbs sleep architecture in healthy pain-free young adults: a preliminary study.

Granted, tianeptine doesn't come close to morphine in terms of a mu opioid agonist, but it is certainly a possibility.
 
Also- another study I came across. Sorry you'll have to google it, can't post links yet. The study was done on HEALTHY individuals, not depressed individuals, so take that for what it is worth.

Tianeptine in an experimental medicine model of antidepressant action. (Cooper et al, 2015)

The tianeptine group recalled a significantly lower proportion of positive self-referential words compared to the placebo group

Tianeptine-treated subjects displayed reduced attentional vigilance to positive stimuli

A single dose of tianeptine did not produce expected positive effects on emotional processing seen previously with acute administration of clinically effective antidepressant therapies
 
Also- another study I came across. Sorry you'll have to google it, can't post links yet. The study was done on HEALTHY individuals, not depressed individuals, so take that for what it is worth.

Tianeptine in an experimental medicine model of antidepressant action. (Cooper et al, 2015)

The tianeptine group recalled a significantly lower proportion of positive self-referential words compared to the placebo group

Tianeptine-treated subjects displayed reduced attentional vigilance to positive stimuli

A single dose of tianeptine did not produce expected positive effects on emotional processing seen previously with acute administration of clinically effective antidepressant therapies

What does this mean?
 
Opiates tend to increase histamine release as well, massively, in the brain and body.
{ncbi.nlm.nih.gov/pubmed/7694026}
{onlinelibrary.wiley.com/doi/10.1111/j.1742-7843.2010.00655.x/pdf}
{ncbi.nlm.nih.gov/pubmed/14742371}

Huh...didn't know that. I wonder if that's why I have such a strong reaction to such low doses and have trouble sleeping. Had the same problem when I once tried a low dose of bupropion. I couldn't sleep for two days and broke into bad rashes. Doctor said it was due to bupropion increasing histamine. Maybe I just need to take an antihistamine at night to help me sleep while taking tianeptine.
 
Opiates tend to increase histamine release as well, massively, in the brain and body.
{ncbi.nlm.nih.gov/pubmed/7694026}
{onlinelibrary.wiley.com/doi/10.1111/j.1742-7843.2010.00655.x/pdf}
{ncbi.nlm.nih.gov/pubmed/14742371}

From this study you posted:

Opioid-induced mast cell activation and vascular responses is not mediated by mu-opioid receptors: an in vivo microdialysis study in human skin.

It actually says in title/abstract: "Because naloxone did not attenuate these effects, it is unlikely that mu-opioid receptors are involved in the activation of mast cells."

Tianeptine's main effects are from MOR agonism (with a much lower potency for DOR agonism) so I would think that tianeptine would not have any substantial effect on histamine levels.
 
Yes it's possible kappa-opioid plays a larger role, but that can not rule out mu-action itself even despite the above study. That's because there are secondary targets of opioids like beta-arrestin and potassium channels which become downstream targets. In other words, in the cell culture studied *if looking at prejunctional / synaptic targets* may not show a direct influence of mu-agonism but instead, mu-agonism activates histamine from a secondary or postsynaptic target.

I believe you meant delta opioid, as opposed to kappa opioid.

Hmm, now that is very interesting about a possible downstream histamine effect. I will have to take a look at this discussion portion of the studies.
 
What does this mean?

From the study:

"the effects in the present single dose study are more in keeping with the negative bias seen in depressed patients than with the positive bias induced by a range of antidepressants in healthy volunteers"

It is unknown why this is - the study mentions that the decrease in serotonin could be a reason, although it does state "role of serotonin reuptake enhancement has produced contradictory results".
 
Still really loving tianeptine sulfate. I seem to have settled around a 25 mg in the morning and a second dose around noon. I take 200 mg of magnesium glycinate and 200 mg of l-theanine with it. That seems to take the edge off the stimulation. My mood is much better and as a result of the extra stimulation it provides, I've been lifting weights much more consistently (almost every day now). Also, I've noticed a definite increase in libido (which has been pretty much non-existent for the last 6+ months). The only negative right now is that I have to take some benedryl at night to help me sleep.
 
Do any of you see an issue with taking a dose of Lithium Orotate at night, while taking tianeptine during the day?

Crazy you should ask that, I was just looking online this morning about combining the two and seeing if there might be any negative interactions. I have read that lithium works great as an augmenter with SSRIs but haven't seen anything yet about combining it with Tianeptine. Please post any results if you do try combining the two.
 
From this study you posted:

Opioid-induced mast cell activation and vascular responses is not mediated by mu-opioid receptors: an in vivo microdialysis study in human skin.

It actually says in title/abstract: "Because naloxone did not attenuate these effects, it is unlikely that mu-opioid receptors are involved in the activation of mast cells."

Tianeptine's main effects are from MOR agonism (with a much lower potency for DOR agonism) so I would think that tianeptine would not have any substantial effect on histamine levels.

Tianeptine at regular doses might not effect it greatly, but acute doses effect it 100%.

Everytime I do an acute dose of 75-100mg, I get itchy around my head, scalp, nose, body. A clear sign of massive histamine release.

Once in a while I take an acute dose for an immediate reaction during times of great stress, etc
 
Tianeptine at regular doses might not effect it greatly, but acute doses effect it 100%.

Everytime I do an acute dose of 75-100mg, I get itchy around my head, scalp, nose, body. A clear sign of massive histamine release.

Once in a while I take an acute dose for an immediate reaction during times of great stress, etc

That's what I experience (along with excess energy, I have massive itching all over) when taking tianeptine. I wonder if taking benedryl at night to help me sleep is the real reason why I've been doing better with it lately (and not due to the magnesium and theanine). I've always had high histamine levels and just a couple months ago stopped taking an antihistamine every day (had been taking it for almost two years). I think tomorrow I'll try adding some zyrtec during the day (with tianeptine and no magnesium or theanine) and see if that helps. Lots of great info and things to try in this thread.
 
That's what I experience (along with excess energy, I have massive itching all over) when taking tianeptine. I wonder if taking benedryl at night to help me sleep is the real reason why I've been doing better with it lately (and not due to the magnesium and theanine). I've always had high histamine levels and just a couple months ago stopped taking an antihistamine every day (had been taking it for almost two years). I think tomorrow I'll try adding some zyrtec during the day (with tianeptine and no magnesium or theanine) and see if that helps. Lots of great info and things to try in this thread.

That's fairly normal though for a big dose. How much are you taking?
 
That's fairly normal though for a big dose. How much are you taking?

25-50 mg doses (higher dose causing more intense itching). May be unrelated but figured I would check anyway. Sorry, don't mean to derail the thread...at least, not any more than I already have. :)
 
25-50 mg doses (higher dose causing more intense itching). May be unrelated but figured I would check anyway. Sorry, don't mean to derail the thread...at least, not any more than I already have. :)

No it's fine, this is a general Stablon discussion

Sounds like you're a hyper-responder! That's not too bad, means you can get away with lower doses.

It takes me twice what you take for the same effect.
 
Are any of you guys concerned with addiction? Im thinking of trying it...but want to hear about you guys' accounts on potential addiction first.
 
Are any of you guys concerned with addiction? Im thinking of trying it...but want to hear about you guys' accounts on potential addiction first.

I guess it can be addictive, but if you abuse higher doses, it'll down regulate you fast and stop working, so it's kind of self-regulating.
 
I guess it can be addictive, but if you abuse higher doses, it'll down regulate you fast and stop working, so it's kind of self-regulating.

Gotcha. Thanks. My first google search kicked out some addiction forum where a dude said he was blowing 20k a month taking like 300 12.5mg capsules multiple times a day...i was just like .

It seems there is some conflicting/individual dosages in this thread. What is a good starting dosing regimen? 12.5mg bid - early morning then 6-8 hrs later? Coupled with 2g lysine and some L-theanine on the first dose?
 
Also- another study I came across. Sorry you'll have to google it, can't post links yet. The study was done on HEALTHY individuals, not depressed individuals, so take that for what it is worth.

Tianeptine in an experimental medicine model of antidepressant action. (Cooper et al, 2015)

The tianeptine group recalled a significantly lower proportion of positive self-referential words compared to the placebo group

Tianeptine-treated subjects displayed reduced attentional vigilance to positive stimuli

A single dose of tianeptine did not produce expected positive effects on emotional processing seen previously with acute administration of clinically effective antidepressant therapies

I know Tia isn't a classic TCA, but most tricyclics are notoriously non-selective regarding receptor interactions. I'm talking 30-40 different sub-receptors in a dozen different systems, and Tia likely has some degree of anti-cholinergic activity too (which would antagonize any minor histaminergic properties.) Besides, the pruritis is more likely serotonergic. Other TCAs like amitriptyline are known to inhibit histamine release from activated mast cells, but still allow the release of serotonin. Stacking Tia with an SSRI might precipitate this, and the itchy hives can also have a psychosomatic component involving serotonin receptors.

Something like cyproheptadine or an NSAID is likely to be more helpful than a histamine antagonist like diphenhydramine.

Also, 'Did not produce expected positive effects on emotional processing seen previously with acute administration' is a clue that A1 agonism probably predominates at conventional doses. 'Reduced attentional vigilance' is the anxiolytic benefit that most users highlight, but that adenosine hook means any abuse potential should be greatly attenuated. Still, I have seen some reports on-line that 100-200mg produces a euphoric effect distinct from its low dose character, and that's probably the threshold where low affinity MOR interactions overtake adenosine's depressive influence.
 
I know Tia isn't a classic TCA, but most tricyclics are notoriously non-selective regarding receptor interactions. I'm talking 30-40 different sub-receptors in a dozen different systems, and Tia likely has some degree of anti-cholinergic activity too (which would antagonize any minor histaminergic properties.) Besides, the pruritis is more likely serotonergic. Other TCAs like amitriptyline are known to inhibit histamine release from activated mast cells, but still allow the release of serotonin. Stacking Tia with an SSRI might precipitate this, and the itchy hives can also have a psychosomatic component involving serotonin receptors.

Something like cyproheptadine or an NSAID is likely to be more helpful than a histamine antagonist like diphenhydramine.

Also, 'Did not produce expected positive effects on emotional processing seen previously with acute administration' is a clue that A1 agonism probably predominates at conventional doses. 'Reduced attentional vigilance' is the anxiolytic benefit that most users highlight, but that adenosine hook means any abuse potential should be greatly attenuated. Still, I have seen some reports on-line that 100-200mg produces a euphoric effect distinct from its low dose character, and that's probably the threshold where low affinity MOR interactions overtake adenosine's depressive influence.
I can confirm the euphoria at those doses, even a bit less is quite powerful. Amazing, in fact. It was also easy for me to chase it up until I hit a gram or 2 a day, then went through withdrawal which was terrible.
 
Gotcha. Thanks. My first google search kicked out some addiction forum where a dude said he was blowing 20k a month taking like 300 12.5mg capsules multiple times a day...i was just like .

It seems there is some conflicting/individual dosages in this thread. What is a good starting dosing regimen? 12.5mg bid - early morning then 6-8 hrs later? Coupled with 2g lysine and some L-theanine on the first dose?

20K for 300 12.5mg caps? Damn. He must be exaggerating enormously. I pay around $60 for 10g of tianeptine bulk powder, including rushed shipping, and that's for more than I need for a month, even if it's being abused.
 
No bud. He was taking "300 12.5mg caps as a single dose with MULTIPLE DOSES daily". As in 1 dose would be 3.75g and he was doing this multiple times a day. Seemed crazy to me, but who the ef knows lol.
 
No it's fine, this is a general Stablon discussion

Sounds like you're a hyper-responder! That's not too bad, means you can get away with lower doses.

It takes me twice what you take for the same effect.

Took 10 mg zyrtec last night before bed (since it lasts much longer than benedryl) and slept like a log. This morning I took tianeptine with just magnesium (no l-theanine) and didn't have the usual energy boost (no added anxiety). In fact, I've had to drink coffee twice so far today just to stay awake (always got very tired when taking zyrtec in the past even though they claim it's non-drowsy). I'll try taking just 5 mg of zyrtec tonight but it appears histamine could be the reason for the negative reactions I had (whether due to tianeptine increasing histamine or some kind of rebound effect when I had stopped taking zyrtec every day for so many years). The two doses I took today felt much more calming afterwards...the typical response that people have to it.
 
No bud. He was taking "300 12.5mg caps as a single dose with MULTIPLE DOSES daily". As in 1 dose would be 3.75g and he was doing this multiple times a day. Seemed crazy to me, but who the ef knows lol.

Wow yeah that's insane lol.... I've taken up to 400mg a couple times before, but I could not imagine taking more. But still, even if he took 10g daily, that should not equal 20K per week lol, more like under 1K. He must've been trolling. At those doses, his receptors would be shot too.
 
The Official "Stablon is a smart drug" thread

Serotonin definitely plays a role in pruritis (Itching), good call on that one. Makes sense too, stress can increase serotonin, serotonin can increase itching and also some compulsive behavior. Histamine is more involved with specific allergen induced inflammation and itching, rather than psychological itching which is more serotonin based.

I have an interesting story for you though.

Last fall I was taking a fairly high dose of Dienolone ace and was using Tianeptine on the regular to offset any mental sides. I was kind of abusing Tianeptine though, taking big doses often for the energy and appetite suppression, and of course it's other effects.

Well I triggered an allergic reaction with my dien ace, by not rotating site injects enough in one place. It cause a rash that spread down my glute. But in only a matter of a week, it stopped going down my glute and instead, my whole stomach, sides and chest were on fire, for days. I had to go to a doc and get prednisone. But the allergic rash lasted for months!!! And it kept coming back!! It was insane. I finally figured out how to stop it, and that was to completely stop my Tianeptine usage, plus cortisone cream and prescription anti-histamines.

I did so for the past 4-5 months and the rash disappeared and never returned. I blame this all on a huge surge in histamines as I had an almost full-body histamine reaction. My doctor also said it looked just like a drug rash, but I know I'm not allergic to Tia, as I'm fine now.
 
Okay, hopefully someone on here can help me understand something. Please forgive me if my understanding is completely wrong or if I have things backwards. I was reading up more on differences between tianeptine sodium and sulfate and it was noted that Sulfate (H2SO4) is 98g/mol, whereas sodium (Na+) is 22g/mol. This difference is why many say you need to take around three to four times the amount of tianeptine sulfate versus the sodium form to get the same amount of the tianeptine molecule. So, if you neglect any contribution to a slower release of the sulfate form (which there probably is some delayed absorption due to differences in molecular size but nothing clinically proven since the only test on it used a slow release matrix for the tianeptine sulfate tablet), then wouldn't it make sense that you should dose tianeptine sulfate similar to tianeptine sodium...except maybe twice a day (to account for some slight difference that may exist in absorption)? In other words, if the standard dose of tianeptine sodium is 12.5 mg three times a day, then tianeptine sulfate should be dosed around 37.5-50 mg two times each day to get the same amount of the tianeptine molecule as the standard dosing for tianeptine sodium?
 
I wish I could help. This thread has confused me so much about the sulfate version, that I've gone back to sodium and am sticking with that since it works as expected.
 
I wish I could help. This thread has confused me so much about the sulfate version, that I've gone back to sodium and am sticking with that since it works as expected.

Yeah, I'm considering switching to the sodium version since it's so well studied and significantly cheaper.
 
I wish I could help. This thread has confused me so much about the sulfate version, that I've gone back to sodium and am sticking with that since it works as expected.

Well, I'm an idiot. My thinking was way off. This link gives a good description comparing the sodium and sulfate forms - Invalid Link Removed. I don't know if it's completely correct but has good numbers and reasoning to back it up.
 
Has anyone noticed an ill effect on their training from tianeptine? I've been using 50mg of tianeptine sulfate once daily in the morning with an empty stomach. It's been 17 days now, and although it has noticeable mood brightening, antidepressant and anxiolitic effects, it seems to tank my recovery and ability to handle volume. Maybe it's just the training stress though.

Apart from the positive effects noted above, the negative effects so far are constant lethargy, reduced libido and appetite, and constipation.

The analgesic effects were very notable during the first week, I felt great in the gym but I suspect that is an easy way to hurt yourself. It went away after the first week.

At this point, I don't think I want to take it chronically but I would like to acquire its long-term benefits of normalizing your HPA axis, promoting BDNF, repairing neuronal damage due to stress and increasing synaptic plasticity. Does anyone know how long I need to keep taking it for? The original Server literature states that the sodium salt needs 6-8 weeks to work well, so I'd bet it's even longer for the sulfate salt but I'm not sure I want to be lethargic for that long.
 
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