SKL
Bluelight Crew
- Joined
- Sep 15, 2007
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- 14,647
Okay, folks, from my personal vault, here is an experience with a rather unusual compound which I had a one-off opportunity to sample a while back: β-CFT, a/k/a WIN 35,428, a semi-synthetic tropane dopamine reuptake inhibitor structurally similar to cocaine. There is little known about it's use in man, but in rats it is reinforcing in a way similar to cocaine, albeit less so (something that makes sense in light of my subjective experience with it), and it is quite significantly longer lasting. There have been some rumors that it has shown up in "legal high" products, but I find this very doubtful as the stuff is frightfully expensive and not an easy or quiet synthesis to do. Anyway, I had the opportunity to try it in pure form, and am not one to pass up a unique experience, so my impressions of it are as follows:
β-CFT (WIN 35,428), (–)-2-β-Carbomethoxy-3-β-(4-fluorophenyl)tropane, 7 mg, i.v. At a friend's home, in the early evening, after a good night's sleep and a light meal. First few hours spent inside, then later, walking around the city streets. Writer is on Suboxone maintenance and towards the end of the experience smoked a few bowls of cannabis, otherwise, no other substances were involved.
Initially, there is a barely-perceptible ringing in my ears, much less dramatic than with cocaine, along with a slight lift in mental energy; but there is no particular "rush." The stimulation grows gradually over the next hour or so, I become increasingly talkative, with mildly pressured speech at times to the point of logorrhea. There is not the forceful euphoric push of cocaine or of the more euphoric amphetamines and cathinones, but the feeling of increased energy persists and builds. Well into the second hour, the effects are still increasing and have yet to peak. My attention becomes increasingly narrow and focused, I am tweaking some settings on my computer, and all of my efforts are thus directed. I am in and out of conversation with my friend, but my gaze and attention are fixed at the task at hand, even as our conversation wanders over a great many topics. I am still able to engage verbally, indeed, my speech still has the increased loquaciousness of the first hour, but the task I am engaged in has hold of me to the point that I withdraw inwardly and become less social.
Effects peak around the third hour. There is a remarkable lack of body load, no peripheral jitters, diaphoresis, or obvious vasoconstriction. My mood is positive, but still not what I would call euphoric, certainly not as elevated as by cocaine. Increased concentration persists along with the positive mood. Time flies by--by the time that I drag myself away from the work that I had been doing on the computer, I am halfway through the forth hour of the experience. I ask my friend the time: 11 p.m. I would have guessed around 8 or 8:30. This compound is indeed very long acting--I am still in the thick of it. The plateau is long, for another hour or so I feel stimulated and have no appetite, though I have not eaten much throughout the day. My friend and I have dinner, I am still in a positive mood, still very talkative. Words and concepts feel as though they come very easily, the conversation is an interesting and verbose one covering everything from pharmacology to politics to a current love interest of mine.
My friend and I part ways a bit after midnight, it is now about six and a half hours since administration of the drug. I walk out into the cold night, and still feel invigorated. I decide to walk the better part of the way home, listening to music on earphones. My sense of time continues to be constricted, and I walk about a mile and a half before I am even really aware of how tired my body is -- but then this awareness comes quickly. I hail a cab and when I sit down inside, the exhaustion comes over my body in waves and I cannot get home quickly enough. I lie down and quickly fall asleep at approximately T+7:30. The next morning, there is a very slight hangover and I am dehydrated, but I do not notice any serious aftereffects or dysphoria.
Overall, a worthwhile exercise. The compound is a decent utilitarian stimulant, something I would class with methylphenidate, but superior for it's transparency. It reminds me more of methylphenidate than it does of it's close cousin cocaine or with something along the lines of MDPV--it is far less physical. and also less euphoric, but it's effects are definitely pleasant and positive. I feel as though I could use it for practical purposes, to aid in concentration or as a chemical boost to confidence. The unpleasant comedown and obsessive urge to redose that are so salient with cocaine I find totally absent.
So, going on my subjective experience, there are some notable differences from the parent compound:
I would also note there was no anesthetic properties noted.
Now, let's look at this subjective experience in light of some of the literature:
First, the chemical is longer acting, and while it's "behavioral toxicity" is not dissimilar from cocaine, this does make it a bit less liable to cause people (or rats or pigeons) to get into compulsive patterns with it.
β-CFT (WIN-35,428). (–)-2-β-Carbomethoxy-3-β-(4-fluorophenyl)tropane.
Troparil (β-CPT, WIN-35,065-2). (-)-2-β-Carbomethoxy-3-β-phenyltropane.
Cocaine. (–)-2-β-Carbomethoxy-3-β-benzoxytropane.
β-CFT is derived by adding a fluorine to troparil (Wikipedia, another analogue of interest). It is more of a pure DARI with fewer of the pharmacological eccentricities of cocaine. Chemically speaking, β-CFT if fluorinated troparil, and troparil is cocaine with a phenyl group instead of a benzoyl; the removal of the ester decreases the local anesthetic activity and the sodium-channel blocking which is responsible for a lot of cocaine's cardiotoxicity and peripheral effects. Also, it is more of a pure dopamine reuptake inhibitor with less effect on the serotonin system (relative to dopamine) -- according to Lakoskii et al. (1991), β-CFT has, relative to cocaine, 1/4th the potency as a sodium channel blocker, 3x the potency on 5-HT reuptake, and 11x the potency on dopamine reuptake.
So, it is not shocking that this is a cleaner stimulant with less "gee-whiz" factor/pushy euphoria than the parent compound. It is, by and large, what it's pharmacology suggests ... a cocaine replacement it is most definitely not, but a useful stimulant it may very well be. I am not fond of methylphenidate or MDPV or indeed of most DARIs, and actually, I found β-CFT to be superior to any of the others that I have sampled.
Lakoski, JM, et al. (1991). Cocaine: pharmacology, physiology, and clinical strategies. Boca Raton, FL: CRC Press. excerpt at Google Books
Norman, AB et al. (2004) The self-administration of WIN 35,428 and cocaine: comparisons of satiety threshold and elimination half-life in rats. European Journal of Pharmacology, 483(2-3), 281-287,
abstract available.
Wee, S et al. (2009) A Reduced Rate of In Vivo Dopamine Transporter Binding is Associated with Lower Relative Reinforcing Efficacy of Stimulants. Neuropsychopharmacology 31, 351–362, full text available.
U.S. Patent 3,813,404. Tropane-2-carboxylates and derivatives. Sterling Drug, Inc., U.S.A., PDF available online
QUALITATIVE EXPERIENCE
β-CFT (WIN 35,428), (–)-2-β-Carbomethoxy-3-β-(4-fluorophenyl)tropane, 7 mg, i.v. At a friend's home, in the early evening, after a good night's sleep and a light meal. First few hours spent inside, then later, walking around the city streets. Writer is on Suboxone maintenance and towards the end of the experience smoked a few bowls of cannabis, otherwise, no other substances were involved.
Initially, there is a barely-perceptible ringing in my ears, much less dramatic than with cocaine, along with a slight lift in mental energy; but there is no particular "rush." The stimulation grows gradually over the next hour or so, I become increasingly talkative, with mildly pressured speech at times to the point of logorrhea. There is not the forceful euphoric push of cocaine or of the more euphoric amphetamines and cathinones, but the feeling of increased energy persists and builds. Well into the second hour, the effects are still increasing and have yet to peak. My attention becomes increasingly narrow and focused, I am tweaking some settings on my computer, and all of my efforts are thus directed. I am in and out of conversation with my friend, but my gaze and attention are fixed at the task at hand, even as our conversation wanders over a great many topics. I am still able to engage verbally, indeed, my speech still has the increased loquaciousness of the first hour, but the task I am engaged in has hold of me to the point that I withdraw inwardly and become less social.
Effects peak around the third hour. There is a remarkable lack of body load, no peripheral jitters, diaphoresis, or obvious vasoconstriction. My mood is positive, but still not what I would call euphoric, certainly not as elevated as by cocaine. Increased concentration persists along with the positive mood. Time flies by--by the time that I drag myself away from the work that I had been doing on the computer, I am halfway through the forth hour of the experience. I ask my friend the time: 11 p.m. I would have guessed around 8 or 8:30. This compound is indeed very long acting--I am still in the thick of it. The plateau is long, for another hour or so I feel stimulated and have no appetite, though I have not eaten much throughout the day. My friend and I have dinner, I am still in a positive mood, still very talkative. Words and concepts feel as though they come very easily, the conversation is an interesting and verbose one covering everything from pharmacology to politics to a current love interest of mine.
My friend and I part ways a bit after midnight, it is now about six and a half hours since administration of the drug. I walk out into the cold night, and still feel invigorated. I decide to walk the better part of the way home, listening to music on earphones. My sense of time continues to be constricted, and I walk about a mile and a half before I am even really aware of how tired my body is -- but then this awareness comes quickly. I hail a cab and when I sit down inside, the exhaustion comes over my body in waves and I cannot get home quickly enough. I lie down and quickly fall asleep at approximately T+7:30. The next morning, there is a very slight hangover and I am dehydrated, but I do not notice any serious aftereffects or dysphoria.
Overall, a worthwhile exercise. The compound is a decent utilitarian stimulant, something I would class with methylphenidate, but superior for it's transparency. It reminds me more of methylphenidate than it does of it's close cousin cocaine or with something along the lines of MDPV--it is far less physical. and also less euphoric, but it's effects are definitely pleasant and positive. I feel as though I could use it for practical purposes, to aid in concentration or as a chemical boost to confidence. The unpleasant comedown and obsessive urge to redose that are so salient with cocaine I find totally absent.
DISCUSSION
So, going on my subjective experience, there are some notable differences from the parent compound:
I would also note there was no anesthetic properties noted.
Now, let's look at this subjective experience in light of some of the literature:
- "A slow onset of action has been hypothesized to weaken the reinforcing effects of drugs. The present study evaluated this hypothesis with slow-onset cocaine analogs, WIN 35428, RTI 31, and RTI 51. When cocaine or a cocaine analog was made available to rhesus monkeys (n=4 or 5) for self-administration ... the data support the hypothesis that a slow onset at the DAT is associated with reduced reinforcing efficacy of DAT ligands. The data under both the PR and FR schedules, however, suggest that a slow onset at the DAT influence reinforcing effect only to a limited extent." (Wee et al., 2009)
- "Rats that self-administered cocaine at unit doses between 0.75 and 12 μmol/kg with mean inter-injection intervals between approximately 2 and 18 min also reliably self-administered the cocaine analogue WIN 35,428 (β-CFT; (−)-3β-(4-fluorophenyl)tropane-2β-carboxylic acid methyl ester) at unit doses between 0.1 and 1.6 μmol/kg with mean intervals between 10 and 116 min ... The approximately 43-fold lower rate of consumption of WIN 35,428 relative to cocaine was a product of the seven-fold greater pharmacodynamic potency and the six-fold greater pharmacokinetic potency." (Norman et al., 2004)
- "The cocaine analogues that were potent in inhibiting [3H]cocaine binding to monoamine uptake sites had been shown to be behaviorally active in earlier studies. For instance, WIN 35,065-2 and WIN 35,428 were three to ten times more potent than cocaine in affecting scheduled-controlled behavior of squirrel monkeys ... WIN 35,428 and WIN 35,065-2 generalized to cocaine more potently than cocaine itself in a drug discrimination paradigm in pigeons" (Lakoski et al., 1991)
First, the chemical is longer acting, and while it's "behavioral toxicity" is not dissimilar from cocaine, this does make it a bit less liable to cause people (or rats or pigeons) to get into compulsive patterns with it.
β-CFT (WIN-35,428). (–)-2-β-Carbomethoxy-3-β-(4-fluorophenyl)tropane.
Troparil (β-CPT, WIN-35,065-2). (-)-2-β-Carbomethoxy-3-β-phenyltropane.
Cocaine. (–)-2-β-Carbomethoxy-3-β-benzoxytropane.
β-CFT is derived by adding a fluorine to troparil (Wikipedia, another analogue of interest). It is more of a pure DARI with fewer of the pharmacological eccentricities of cocaine. Chemically speaking, β-CFT if fluorinated troparil, and troparil is cocaine with a phenyl group instead of a benzoyl; the removal of the ester decreases the local anesthetic activity and the sodium-channel blocking which is responsible for a lot of cocaine's cardiotoxicity and peripheral effects. Also, it is more of a pure dopamine reuptake inhibitor with less effect on the serotonin system (relative to dopamine) -- according to Lakoskii et al. (1991), β-CFT has, relative to cocaine, 1/4th the potency as a sodium channel blocker, 3x the potency on 5-HT reuptake, and 11x the potency on dopamine reuptake.
So, it is not shocking that this is a cleaner stimulant with less "gee-whiz" factor/pushy euphoria than the parent compound. It is, by and large, what it's pharmacology suggests ... a cocaine replacement it is most definitely not, but a useful stimulant it may very well be. I am not fond of methylphenidate or MDPV or indeed of most DARIs, and actually, I found β-CFT to be superior to any of the others that I have sampled.
REFERENCES
Lakoski, JM, et al. (1991). Cocaine: pharmacology, physiology, and clinical strategies. Boca Raton, FL: CRC Press. excerpt at Google Books
Norman, AB et al. (2004) The self-administration of WIN 35,428 and cocaine: comparisons of satiety threshold and elimination half-life in rats. European Journal of Pharmacology, 483(2-3), 281-287,
abstract available.
Wee, S et al. (2009) A Reduced Rate of In Vivo Dopamine Transporter Binding is Associated with Lower Relative Reinforcing Efficacy of Stimulants. Neuropsychopharmacology 31, 351–362, full text available.
U.S. Patent 3,813,404. Tropane-2-carboxylates and derivatives. Sterling Drug, Inc., U.S.A., PDF available online
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