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Dubious claim with bad reference

So, I noticed that this claim was made for both 2-fluorination & 4-fluorination, on the respective pages: "Studies demonstrate that 2-flourine amphetamine substitutions limit activity of the compound at the alpha-1 adrenergic receptor with an over 200-fold increased selectivity for A2 receptors over A1 receptors."

I decided to check the citation to see which one it supported, and realized that it was neither. The little bit about fluorinated norepinephrine is also pretty irrelevant in terms of SAR, so I think it was someone with a vested interest in selling these amphetamines attempting to justify the anecdotal effects / dose ceiling where applicable. I've removed the claim from the pages I noticed it in. Storm (talk) 04:58, 7 March 2017 (CET)

Some observations on dosing (single source, single user, multiple batches, multiple RoAs)

This first section is a report on intranasal dosing from a few months ago. New information below.

Prior observations about European batch, April '17 (old information)

European batch, April 2017, quoted as >98% purity, off-white colour. General consistency and appearance not dissimilar to 4-FA. Substance has not been tested independently but source is known and trusted; the substance is distinguishable in consistency from many other closely related compounds and has little smell. Insufflation is subjectively viable as RoA, but not entirely painless. (For context, the reporter will rail 2-FA, but starts to baulk at 3-FPM and ethylphenidate. He's been daft enough to try it with 4-FA - never again.)

In terms of discomfort, absorption and onset, 3-FA has a lot in common with 2-FA. It stings sharply, but this is short lived; it absorbs quickly, onset < 1m and nasal discomfort largely gone over the same timeframe. Use on 2-3 consecutive days is viable from that point of view, if perhaps not clever. So far it has been sampled at doses ranging from 5mg to 60mg intranasally. While I've not yet tried it orally to compare, the oral doses given here show a loosely comparable class of effect when dosed intranasally, weight for weight, i.e. 5mg is around threshold, 30mg is definitely a dose (if short-lived and repeatable), and 60mg would satisfy a cautious definition of 'heavy', perhaps suffixed with 'enough for now'. For contrast, with the 2-subbed equivalent my desired intranasal doses were 2-3x a respectable oral dose; that seems unlikely to be the case here. At that level, 60mg, there is a clearly stimulant effect and a brightening of mood, far short of elation or entactogenesis but nothing to complain at.

I suspect it can go further, having no cardiovascular or respiratory worries at a 60mg dose, not overheating or uncomfortable and it's not 'pushy'. Trouble is at this dose I could sit here and do nothing on it. (dose-dependent, see below) Less surprisingly, the duration is shorter; I haven't quantified it back to baseline, but at 1.5 - 2h I could redose or go to bed. One oddity, it seems anything but anorectic - 250mg over 2 days and around 4,500 calories/day both days. Tentatively I'd suggest adding intranasal dosing and that a 5mg to 60mg range seems i) reasonable and ii) fairly conservative. I'll update if, as with some of its brethren, I try something less conservative.

Discussion around first reports

@Magick Hi there! First, I just wanted to thank you for taking the time to post this very informative and useful post :) Your notes are definitely a good basis for us to add insufflated doses and durations. FWIW I have conducted a significant amount of online research on the effects of 2-FA (although only with oral doses). I also have a lot of background knowledge on the effects of insufflated 2-FMA and 3-FPM as well and, of course, 4-FA for its putative recreational effects. As time went on I grew increasingly wary of the fluorine substitution on these compounds as that seemed to increase the causticity and overall damage on the nasal passages quite significantly based on reports (though this was largely extrapolated from reports of insufflated 4-FA, 2-FMA I have read is not bad to insufflate and I have also read reports of 3-FPM being painful, but not unbearably so. EPH is another story...). So what you're telling me here is that 3-FA does not follow the same pattern for noticeable causticity as 4-FA does? If so that is interesting to note. What you described to me seemed like a very short-lasting version of insufflated 2-FA more or less. Would you say that is fair or does 3-FA and 2-FA display the same durational patterns in your view? Either way, I think I am starting to get an idea of how this compound should be represented. Does 2-5mg Threshold, 5-15mg light, 15-35mg common, 35-60mg strong and 60mg+ heavy sound reasonable to you? With a 1.5-2hr duration (this does seem a little short to me, is this accounting for your personal stimulant tolerance?) The lack of anorectic effect is interesting -- this is relative to other similar fluorinated amphetamines like 2-FA or 2-FMA, right? Perhaps it has something to do with relatively lower adrenergic affinity/activity.
In any case, thanks again for your suggestion! I will do some research and cross-referencing and probably implement these soon. BTW, just so you know, if you type four ~ in a row in a talk section it will insert a signature, which you can use to sign off. Also, adding a ":" at the beginning of each paragraph will allow you to indent your replies; you can repeat these for further indentation. That is all. Take care :) Clarity (talk) 12:57, 1 May 2017 (CEST)
Regarding the FAs, 2-FA was tolerable to insufflate, but not very bioavailable and a bit self-limiting (that is to say, it lost effect with re-dosing as opposed to becoming 'forced' in the way some stims are, and, exceptionally, it needed about twice the dose insufflated as it did orally.). As to discomfort in the nasal mucosa, 3-FA has a lot in common with 2-FA and 3-FPM; it can momentarily bring tears to the eyes, but it absorbs quickly, onset is fast, pain dissipates fast, and no damage was noted from sailing through ~500mg. Both EPH and 4-FA are caustic in a sense of tissue damage, pain, and dissuasion of all but the masochistic. So, yes, 3-FA is different, similar mould to 2-FA. Unknown whether the same applies to oral/intranasal bioavailability as with 2-FA, but highly plausible. (no, it's not)
As for comparisons with 2-FA, for duration it's pretty similar. My 1.5-2hr 'duration' (dubious, dose-dependent) probably reflects the end of the plateau (or the point I'd contemplate a redose) not an overall duration back to 'baseline' (itself subjective). So, yep, that'll be a stim user's duration, then. I'll rephrase that as: onset: 1-2 min, come-up: 2-5 min, peak: 90-120m, offset: 30-120 min, after-effects: 60 - 180m (guesstimating the last a bit). For effects, it felt somewhat less stimulating than 2-FA (less NE / more DA) but again of a similar breed.
On dosing, I'd go a fraction higher than that. 100mg is a decent intranasal dose for me, also didn't prove excessive from cold for an acquaintance who lacked what tolerance I may have had. So, I'd go with 5mg-15mg threshold, 15mg-30mg light, 30-60mg common, 60-100mg strong and 100mg+ heavy. The lack of anorectic effect (dubious) was relative to 2-FA, 2-FMA, dextroamphetamine et al, yes. I'd echo your speculation that this is related to lower adrenergic activity, which was commensurate with the experience. Magick (talk) 03:21, 21 May 2017 (CEST)

New reports on bioassays with another European batch, August '17

Similar colour and consistency, quoted as >98% purity, light pink / off-white colour. General consistency and appearance not dissimilar to 4-FA. The consistency is distinctive; soft crystals of a consistency reminiscent of washing powder (laundry detergent), more easily chopped with a sharp blade than crushed. This is very much as before.

Intranasal dosing

Broadly to confirm most of earlier findings. 100mg intranasal seems optimal for me, with the note that some degree of almost instantaneous effect is observed upon intranasal dosing (increased focus, wakefulness) commensurate with DA release, and that this part of the response doesn't seem dose-dependent within the ranges assayed (25mg - 100mg), i.e. once you've had it, you've had it. There is then a second phase of the response, building over 10-30m, which is more mood lift than additional stimulation (subjectively very nice, too). This response profile is maintained through at least three ~100mg doses (dose spacing was ~4h though would have been ~3.5h in a perfect world). The third dose showed signs of approaching the point of diminishing returns, but not of passing it; there was value to the third dose but slower onset and a hint that maybe we'd be pushing our luck to hope for more.

A lengthy report is not needed on this one, besides that a ~100mg intranasal dose (from cold) was well appreciated; a dose taken when getting ready to go out provided a degree of functional stimulation and mood lift that's not been seen for a while - and one very happy user. Fairly sure it's wasteful of material, though, as discussed above.

Note 1: my spacing of doses (by free choice) is around double the 1.5h to 2h I mention above. I was no less enthusiastic, so I suspect that the higher 100mg dose has a material impact on the duration. Has been sampled at the same dose by others, there seems to be consensus both that there are notable effects from 25-30mg intranasal (which I would describe as pushing the upper end of ADHD relief, not that you'd want to use this for that - but on par with a respectable functional (not recreational) dose of dexamfetamine) and also that 100mg in short order seems worthwhile. None of those reporting are wholly stim-naive; the point here is it's active at ~25mg and a whole different sort of active at ~100mg.

Note 2: compulsive / risk-taking behaviour. Still very moderate by stim-fiend standards; it did not cause fiending. What it did elicit, very rare indeed for me, was a strong reward response. I just knew that another dose would be desired, so chucked it in my wallet with the necessaries. Another dose certainly was desired, not a rough comedown but just, well, canonical amphetamine response. So another dose was had (about 1am), and then another dose was had (about 5am). Which is fun, sometimes. I did pack it in and sleep for a bit in between, and it was easy enough, for me, to desist. However, it's attractive stuff for a session, not optimised to case-in-point use.

Note 3: anorectic effects. I was unable to confirm the particular lack of anorectic effects over and beyond its peers when consumed at ~100mg intranasal doses or ~20mg intrarectal doses. Like most of the fluorinated amphetamines, it did not render it impossible to take nutrition, but neither was I eating 50% more than usual as was observed with my initial sampling. That may be down to idiopathic variability but I suspect it has more to do with aggressive dosing. The first few 100mg intranasal doses were quite impressive; whilst as a regular user of stimulants I am quite accustomed to taking nutrition in between, that's just as well. Conclusion: not proven.

Note 4: hygroscopicity 3-FA absorbs atmospheric moisture very readily and a line left out overnight will turn to unusable jelly. Suitable precautions should be used to avoid degradation or wastage. Keeps OK in thick HDPE plastic, but it would not seem unreasonable to consider storing with dessicants and/or under vacuum. Protect it from exposure to air, anyway.

Conclusions on intranasal dosing

  • Intranasal dosing is effective for 3-FA but the dose desired for recreational use is a significant multiple of the threshold dose.
  • Doses are enjoyed that would not be considered orally; it's great fun but it's wasteful.
    • It stings a bit, could bring a tear to the eyes sometimes. Nothing too foul or lasting; dissipates quickly.
    • The use of saline spray or nasal irrigation would be reasonable harm reduction practice if insufflating 3-FA (and indeed most things).
    • Activity will be found at about a quarter of the dose one might choose for recreational effects.
  • STRONG potential for compulsive behaviour. Reporter is less given to this than many/most of his peers, but this stuff gets boshed.
    • To be more specific, there was not so much a compulsion in whether or how much to redose as a loss of inhibition about behaviour around carrying or consuming the drug; I didn't do anything downright stupid, but there was a massive "oh, what the hell?" factor to it. This did seem unique to intranasal administration at highish doses.

Intrarectal dosing

Sampled this for the hell of it. I don't often do intrarectal dosing for practical reasons, but was talking with someone who'd just plugged another stimulant, it's occurred to me previously that my use of certain substances is inefficient, I was sampling this again and, well, 3-FA seemed a fine idea to try. Settled on a dose of 20mg in 2ml of water (by intelligent guesswork). Dosing was without incident; the 10mg/ml concentration did not cause discomfort, but I wouldn't want to go much stronger. The pharmacokinetic observations in this case were very different. Report is being written 'live'; I'd been minded to update my previous notes anyway, and this was the clincher (no pun intended). Chance conversation coincided with desire for stim dose and with need and ability to defecate first, so there was just no excuse not to.

0-1m Not a lot. The administration is well tolerated, but there is no 'rush' to speak of.
1-5m Threshold of awareness, we've got an active dose of something. It's on its way.
5-10m Signs of mood lift. There was no 'rush' noted. (Potentially unclean experiment, in that other dopaminergic stims had been used in the preceding hours. The expectation is that I would still have noticed an intranasal dose. However, who said I was in any sort of a rush? Something is coming on that is certainly pleasant.
10-30m This progresses in the same direction, and the feeling is familiar as 3-FA. Slow onset (for one accustomed to intranasal stims), coming in gentle 'waves' about every ten minutes. At some point during this period I check the current PW data for oral dosing, finding "onset: 20-60m, come-up: 20-60m). I've not sampled 3-FA orally yet, but intrarectal dosing has little in common with intranasal, so figured these would make a good comparison standard. As indeed they do. Re-reading my chat logs, I remarked positively to the effect of "well it's coming up" about every 3-5 minutes for the first 20 minutes. At T+27m I reported a brightening of vision, which was subtle. It fell short of comparisons with the psychedelic phenethylamines at the 20mg dose sampled; as with certain other amphetamines I could imagine it having at least hints in that direction at higher doses.
30-60m Continue in similar vein. At +35m I observed a "slight body high, for want of better words"; at +55m I observed "this is actually becoming really nice, felt another couple of slow upward ramps just now and about 10min prior". So we have a come-up over the course of an hour, perhaps a little more, which I seem to appreciate.
Note: For reporting purposes I'd characterise the onset as 1-15m; by +18m I observed "does seem quite pleasant, definitely going somewhere...". I continued to remark on the come-up over the course of the first hour. During the second hour, it was less remarkable but not static; I am ambivalent about the divisions between come-up and plateau. It certainly hadn't finished coming up at +1h but nor did it peak much from there.
Tentatively, with all the usual about subjective reports of idiopathic findings of unscientifically shoving drugs up your arse, I'd be thinking along the lines of
Onset: 1-15m
Come-up: 15-90m
Peak: 90-180m
Offset: 30-120m
After effects: 30-120m
60-120m At 1h 50m I remarked "the IR dose is very functional. Could have gone a fraction higher but not regretting sampling that". By very functional, I mean that having decided to write it up on here, I'd spent most of an hour doing so, checking back on chat periodically, and been reasonably happy with how I found myself working. It hadn't been my initial intention to go full trip-report mode (and perhaps this should be split off into one), but I've remained favourably impressed so I've remained writing about it. At this point, it feels like the dose may be reaching a plateau; there is a brightness of mood and a degree of a 'body high'. Less positively, though far from surprising or worrying, my hands and feet are unusually cold, which persists even with slippers and a dressing-gown. Confirmation, if any were needed, that this is stim-induced vasoconstriction (there has also been a drop in ambient temperature) is present in the form of a textbook case of 'stim dick'.
120-180m Loosely commensurate with PW data on oral dosing, which I've not yet tried, I would describe a peak over the period 1.5 to 3h post dosing. I'm writing this line at almost exactly 3 hours post dosing, at which point there is still some degree of discernible benefit in terms of mood and task adherence. Qualitatively it lacks the "sharpness" or focus that characterises "ADHD medication" type stimulants but I wouldn't go so far as to describe it as "wooly". Vague temptation to address that with an oral dose of dexamfetamine has on a couple of occasions crossed my mind, but for the sake of sampling this on its own merit I abstained. It felt like it might be a reasonable complement to it at +1h, and again at +3h, not actioned and not amounting to a complaint in either case.
180-210m Clearly past the peak now; there is not a harsh comedown, but at 3.5h I could be sorely tempted by a redose of some sort. This is in keeping with my findings of much larger intranasal doses (five times larger, to be exact) so whatever its merits and demerits, intrarectal administration has likely advantages for dose efficiency. It doesn't seem to lose anything for duration compared with the much larger intranasal dose.
210-240m Fairly typical stim offset, gentle end of the scale. Not completely flattened or irritated by it. I'd quite have liked a redose at the 3.5h to 4h mark, but decided against to get a picture of duration. The vasoconstriction is mild but persistent for a while; this seems more discernible from the intrarectal dose than from any of the intranasal doses that I have sampled.
240-360m Worn off back to what I'd call baseline, or not clearly distinguishable from it. My hands have now warmed up. The 'comedown' is gentle and has not impeded working on a variety of tasks, including this report, a number of other communications and some technical work. It's conspicuous by its absence, but that's all (writing at T+6h20m). Report ends 6h30m after administration, with little more to add.

Conclusions on intrarectal dosing

  • Intrarectal dosing is highly effective with 3-FA.
    • Doses should be substantially lower than oral or intranasal doses.
    • The come-up is slow and steady, or it was for me. No 'rush' was observed, but gentle waves of come-up over an hour and more.
    • Total 'useful' duration was found to be in the range of 3h - 3.5h, for this reporter. This was a pleasant surprise.
    • The inclination to redose presented itself at 3.5h but was not compulsory; I write this at just over T+4h.
  • A dilution of 10mg/ml in water was easily attainable and was well tolerated intrarectally, i.e. didn't hurt.
  • Estimating relative potency from a single sample is a fool's game, but I'm happy to suggest that 3:1 versus oral dosing (or moreP would be nearer the mark than 2:1.
    • Not yet having sampled 3-FA orally, my typical dosing requirements are in the 'strong' to 'heavy' range across a couple of dozen stimulants.
      • I am familiar with 20mg and 30mg oral doses of dextroamphetamine. This was not lesser by comparison.
      • If 20mg of 3-FA plugged was satisfactory to this particular reporter, stick that down as 'strong' at least.

To me this might suggest 5mg increments from

5mg Threshold
10mg Light
15mg Common
20mg Strong
25mg+ Heavy

This reporter would try 30mg plugged, but he wouldn't expect to find that on the Wiki.

Oral dosing

Not my bag... but it had to be done, after that, didn't it? Time of dosing was fairly exactly ~11h after the intrarectal dose above.

0m 60mg parachuted in a cigarette paper.
30m Effectively nothing noted whatsoever. I was perhaps marginally more awake.
Note: user is accustomed to ~20mg doses of dexamp, more if he sees fit. This will have some effect on tolerance, but it's not night and day. User typically notes more activity at 30mg intranasally, never mind 100mg.
60m Some degree of mood lift. Wasn't expecting fireworks, but this seems understated as compared with smaller doses by other RoAs. This contravenes what I'd first thought based on various other fluorinated amphets.
90m Little change. There is a discernible benefit at threshold levels, but doesn't hold a candle to earlier doses. Some peripheral vasoconstriction is noted; does not seem as clear cut as anticipated. There is a stomach ache, mild but noticeable.
120m Well, I remain awake. If I expected that to be dose-equivalent to 20mg plugged... nope. To 30mg railed? That could be pushing it but I'll not rule it out.
150m Quite underwhelmed with this dose. Now yawning, not incessantly but more than expected. At a 60mg dose, I'm hitting the point where more is wanted at the 2h - 2.5h mark, as before. I suspect that a 100mg dose would be tolerated, but there is a certain queasiness.
180m Fed up with this dose. Was not adequate to present requirements. Not, for my taste, superior to intranasal or intrarectal dosing, which is saying something. Redosing is very much in order, to get ready, organised, and moving. On a hunch, I don't think I've had it with 3-FA yet (though there is such a thing as asking for it). At this point, changing drug, changing activity, changing direction or just packing it in would all be reasonable options. So would testing that hypothesis about 30mg intranasal...
210m Didn't get around to that redose yet, owing to a substantive increase in intestinal motility. Stomach ache was mild (in keeping with serotonergics, which this might to some extent be, not food poisoning. However, I passed three stools in five minutes, which rather speaks for itself.
Cross-check for tolerance by 2 x 30mg intranasal dose
225m (3h 45m post oral dose). After some saline, an intranasal dose of 30mg is consumed. It hurts a little, but threshold signs of onset are there in 20-30 seconds, followed by echoes of the same familiar come-up after two to three minutes.
It takes five minutes before the level of desired cognitive effects found from ~30mg intranasal (one third of my preferred dose) equals or surpasses the best of the effect seen from oral dosing of twice that amount. Because I'm going out, and/or because I had 260mg left and was going to use the 60mg... with the 30mg still coming up... a further 30mg is insufflated in the other nostril, to similar effects. A further come-up is noted from about 2-3 minutes thereafter, in the same vein. I start getting ready, rather happier. This is slightly inferior to what can be achieved by my preferred ~100mg, but it's still nothing to complain about.
240m The oral dose is nothing but a bad memory. OK, not high as a kite, but fit to crack on and in a good mood with it. Oral dose report ends here for the same reason. Will update with retrospectives later, and can peel off into separate TRs as appropriate.

Conclusions on oral dosing

  • Subjectively, you can keep it. I'd rather stick it up my... nose. But the other end's not bad, either.
  • Admittedly, I am typically in the strong/heavy ranges, but that was unimpressive for 60mg.
  • The purgative effect on my gastrointestinal system was not experienced as a benefit.

Questions and inconsistencies

  • Put them here and I'll do my best. Magick (talk) 21:24, 10 August 2017 (CEST)