4-FA |
| 4-FA | |||||||||||||||||||||||||||||
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| The skeletal formula of 4-FA | |||||||||||||||||||||||||||||
| Chemical Nomenclature | |||||||||||||||||||||||||||||
| Common names | 4-FA | ||||||||||||||||||||||||||||
| Substitutive name | 4-Fluoroamphetamine | ||||||||||||||||||||||||||||
| Systematic name | (RS)-1-(4-fluorophenyl)-N-propan-2-amine <-- Class Membership --> | ||||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||||
| Psychoactive class | Stimulant | ||||||||||||||||||||||||||||
| Chemical class | Amphetamine | ||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||
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| Summary sheet: 4-FA |
4-Fluoroamphetamine (4-FA) is a substituted amphetamine with stimulant, entactogenic and nootropic effects. It is described subjectively as being between amphetamine and MDMA. It is rarely found on the streets but commonly sold as a grey area research chemical through online vendors along with related compounds such as 2-fluoroamphetamine and 4-fluoromethamphetamine.[1][2]
Contents
Chemistry
4-Fluoroamphetamine (4-FA) is a synthetic molecule of the amphetamine family. Molecules of the amphetamine class contain a phenethylamine core featuring a phenyl ring bound to an amino (NH2) group through an ethyl chain with an additional methyl substitution at Rα. Amphetamines are alpha-methylated phenethylamines. 4-fluoroamphetamine contains a flourine group at R4 of its phenyl ring and is a fluorinated analogue of amphetamine.
Pharmacology
4-Fluoroamphetamines pharmacology differs based on the amount of substance consumed.
When 100mg or more is introduced, 4-FA acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine, producing euphoric, enactogenic effects similar to MDMA. When lower doses of ~75mg are ingested, it only acts on dopamine and norephinephrine, producing effects more similar to a functional stimulant. The mechanism of action of 4-FA effectively boosts the levels of the norepinephrine, dopamine, and serotonin neurotransmitters in higher doses in the brain by binding to and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. This allows dopamine, norepinephrine and serotonin to accumulate within the brain, resulting in stimulating, euphoric and entactogenic effects.[3] [4] [5]
Studies demonstrate that 4-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.[6] It has also been demonstrated that 4-substitution of a hydrogen with fluorine on the aromatic ring of norepinephrine produces a beta-adrenergic agonist with little alpha activity.[7] This has led the online community to speculate that the milder uncomfortable cognitive and/or physical side effects and greater efficacy as a nootropic associated with this substance are at least partially due to decreased activity at the alpha-1 adrenergic receptors resulting in significantly less norepinephrine reuptake inhibition.
Subjective effects
In comparison to other substituted amphetamines, 4-FA is particularly free of side effects such as nausea, high blood pressure, anxiety and an uncomfortable offset. In low doses, it is considered to be an extremely functional and effective nootropic for performing tasks or general productivity of any sort. At higher dosages, however, it becomes dysfunctional and recreational due to the intensity of its euphoria and stimulation.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical effects
- Stimulation
- Tactile enhancement
- Physical euphoria
- Dehydration
- Appetite suppression
- Increased heart rate
- Increased perspiration
Cognitive effects
- Euphoria - This effect can be described in its manifestation as a series of euphoric waves that recede and reappear randomly throughout the experience.
- Empathy, love and sociability enhancement - In comparison to other substances, this effect can be described as identical to the effects produced by MDMA, but with less intensity.
- Thought acceleration
- Thought connectivity
- Focus enhancement
- Ego inflation
- Wakefulness
- Analysis enhancement
- Motivation enhancement
- Sexual arousal
- Novelty enhancement
- Compulsive redosing
- Wakefulness
After effects
The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. Its effects commonly include:
Toxicity and harm potential
The toxicity and long-term health effects of recreational 4-FA use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because 4-FA has very little history of human usage. Anecdotal evidence from people who have tried 4-FA within the community suggest that there do not seem to be any negative health effects attributed to simply trying this drug at low to moderate doses by itself and using it sparingly (but nothing can be completely guaranteed).
The LD50 (mouse; i.p.) of 4-FA is 46 mg/kg.[8] 4-FA does not cause long-lasting depletion of brain serotonin unlike MDMA or 4-FA's analogues 4-CA and 4-BA.
It is also worth noting that 4-FA is particularly caustic in comparison to other compounds and can therefore cause chemical burns within the nasal passage and throat if it is insufflated.
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
As with other stimulants, the chronic use of 4-FA can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage.
Tolerance to many of the effects of 4-FA develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). 4-FA presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of 4-FA all stimulants will have a reduced effect.
Psychosis
Abuse of compounds within the amphetamine chemical class at high dosages for prolonged periods of time can result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[9] A review on treatment for amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[10][11] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[12] Psychosis very rarely arises from therapeutic use.[13][14]
Dangerous interactions
Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.
- Stimulants - 4-FA can be potentially dangerous in combination with other stimulants as it can increase one's heart rate and blood pressure to dangerous levels.
- 25x-NBOMe - Both the NBOMe series and amphetamines induce powerful stimulation. Side effects such as thought loops, seizures, increased blood pressure, vasoconstriction, increased heart rate, and heart failure (in extreme cases) may occur.
- Alcohol - It is dangerous to combine alcohol, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of alcohol which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of alcohol will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - This combination may cause increased heart rate and panic attacks (in extreme cases).
- MXE - Increased heart rate and blood pressure may occur.
- Tramadol - This combination can increase the risk of seizures.
- Cocaine - This combination will increase strain on the heart.
Serotonin syndrome risk
Combinations in the list below may increase the amount of neurotransmitters such as serotonin and dopamine to dangerous or even fatal levels.
- MAOIs such as syrian rue, banisteriopsis caapi, 2C-T-2, 2C-T-7, αMT, and some antidepressants[15]
- Serotonin releasers such as MDMA, 4-FA, MDAI and αMT
- Selective serotonin re-uptake inhibitors (SSRIs)
- 5-HTP
Legal issues
- Arizona: The drug was added to the "Dangerous Drug" list in April 2014.
- Louisiana: 4-FA is currently listed as a Schedule I drug as of June 2013.
- Virginia: The drug is classified as a Schedule I drug.
- Germany: 4-fluoroamphetamine was added to "Anlage I" in January 2012.
- Hungary: In January 2012, 4-flouroamphetamine became controlled in Hungary.
- France: 4-fluoroamphetamine was added to the list of illicit substances in March 2011.
- Israel: In December 2007, 4-flouroamphetamine was added to Israel's list of controlled substances, making it illegal to buy, sell, or possess.
- Poland: 4-Fluoroamphetamine is controlled in Poland.
- Slovak Republic: Beginning March 1, 2011, 4-Fluoroamphetamine is controlled in the Slovak Republic.
- United Kingdom: 4-fluoroamphetamine is a Class A drug under the Misuse of Drugs Act. 4-FA is covered by the 1977 addition to the Misuse of Drugs Act of 1971.
Experience reports
Anecdotal reports which describe this compound within our experience index include:
See also
External links
References
- ↑ The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain | https://www.ncbi.nlm.nih.gov/pubmed/17223101
- ↑ Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues (designer drugs). | http://www.ncbi.nlm.nih.gov/pubmed/15639609
- ↑ http://www.sciencedirect.com/science/article/pii/0028390875900994 | Comparison of 4-chloro-, 4-bromo-and 4-fluoroamphetamine in rats: drug levels in brain and effects on brain serotonin metabolism
- ↑ http://www.sciencedirect.com/science/article/pii/S0014299906013811
- ↑ http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain
- ↑ 2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands | http://pubs.acs.org/doi/abs/10.1021/jm00169a015
- ↑ Effect of fluorine substitution on the agonist specificity of norepinephrine | http://www.sciencemag.org/content/204/4398/1217.short
- ↑ E. Costa and S. Garattini (1970). Amphetamines and Related Compounds. New York: Raven Press. p. 28.
- ↑ Treatment for amphetamine psychosis | [1]
- ↑ Treatment for amphetamine psychosis | [2]
- ↑ Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
- ↑ Treatment for amphetamine psychosis | [3]
- ↑ Stimulant Misuse: Strategies to Manage a Growing Problem | http://www.acha.org/prof_dev/ADHD_docs/ADHD_PDprogram_Article2.pdf
- ↑ http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
- ↑ Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity | http://bja.oxfordjournals.org/content/95/4/434