4-FA: Difference between revisions

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'''4-Fluoroamphetamine''' (abbreviated '''4-FA'''; also known as '''4-FMP''', '''PAL-303''' and colloquially as '''Flux''') is a synthetic [[Psychoactive class::stimulant]] of the [[Chemical class::substituted amphetamine]] class that produces [[stimulant]], [[empathogen]]ic, and [[entactogen]]ic effects. It is described subjectively as being between [[amphetamine]] and [[MDMA]].

4-FA 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-FA|2-fluoroamphetamine]] and [[4-FMA|4-fluoromethamphetamine]].<ref>The effects of non-medically used psychoactive ~~drugs~~ on monoamine neurotransmission in rat brain (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17223101</ref><ref>Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues ([[designer drug]]s). (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15639609</ref>

4-FA 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-FA|2-fluoroamphetamine]] and [[4-FMA|4-fluoromethamphetamine]].<ref>The effects of non-medically used psychoactive substances on monoamine neurotransmission in rat brain (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17223101</ref><ref>Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues ([[designer drug]]s). (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15639609</ref>

==Chemistry==

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==Pharmacology==

4-Fluoroamphetamine acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine producing stimulating amphetamine-like effects at lower doses and euphoric, entactogenic effects similar to MDMA at dosages above 100mg. 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 [[entactogen]]ic effects.<ref>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</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive ~~drugs~~ on monoamine neurotransmission in rat brain </ref>

4-Fluoroamphetamine acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine producing stimulating amphetamine-like effects at lower doses and euphoric, entactogenic effects similar to MDMA at dosages above 100mg. 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 [[entactogen]]ic effects.<ref>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</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive substances on monoamine neurotransmission in rat brain </ref>

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.<ref>2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands | http://pubs.acs.org/doi/abs/10.1021/jm00169a015</ref> 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.<ref>Effect of fluorine substitution on the agonist specificity of norepinephrine | http://www.sciencemag.org/content/204/4398/1217.short</ref> 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]].

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Abuse of compounds within the amphetamine chemical class at high dosages for prolonged periods of time can potentially result in a stimulant psychosis that may present with a variety of symptoms (e.g., [[Paranoia|paranoia]], [[External hallucinations|hallucinations]], or [[Delusions|delusions]]).<ref>Treatment for amphetamine psychosis | [http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD003026.pub3/abstract?systemMessage=Wiley+Online+Library+will+be+disrupted+Saturday%2C+15+March+from+10%3A00-12%3A00+GMT+%2806%3A00-08%3A00+EDT%29+for+essential+maintenance]</ref> A review on treatment for amphetamine, [[dextroamphetamine]], and [[methamphetamine]] abuse-induced psychosis states that about 5–15% of users fail to recover completely.<ref>Treatment for amphetamine psychosis | [http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD003026.pub3/abstract?systemMessage=Wiley+Online+Library+will+be+disrupted+Saturday%2C+15+March+from+10%3A00-12%3A00+GMT+%2806%3A00-08%3A00+EDT%29+for+essential+maintenance]</ref><ref>Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.</ref> The same review asserts that, based upon at least one trial, [[antipsychotic]] medications effectively resolve the symptoms of acute amphetamine psychosis.<ref>Treatment for amphetamine psychosis | [http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD003026.pub3/abstract?systemMessage=Wiley+Online+Library+will+be+disrupted+Saturday%2C+15+March+from+10%3A00-12%3A00+GMT+%2806%3A00-08%3A00+EDT%29+for+essential+maintenance]</ref> Psychosis very rarely arises from therapeutic use.<ref>Stimulant Misuse: Strategies to Manage a Growing Problem | http://www.acha.org/prof_dev/ADHD_docs/ADHD_PDprogram_Article2.pdf</ref><ref>http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf</ref>

===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. [https://www.google.com/ Independent research] should always be done to ensure that a combination of two or more substances is safe before consumption.

Although many substances 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. [https://www.google.com/ 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 [[stimulant]]s as it can [[increased heart rate|increase one's heart rate]] and [[increased blood pressure|blood pressure]] to dangerous levels.

@@ Line 7: / Line 7: @@
 '''4-Fluoroamphetamine''' (abbreviated '''4-FA'''; also known as '''4-FMP''', '''PAL-303''' and colloquially as '''Flux''') is a synthetic [[Psychoactive class::stimulant]] of the [[Chemical class::substituted amphetamine]] class that produces [[stimulant]], [[empathogen]]ic, and [[entactogen]]ic effects.  It is described subjectively as being between [[amphetamine]] and [[MDMA]].
--FA 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-FA|2-fluoroamphetamine]] and [[4-FMA|4-fluoromethamphetamine]].<ref>The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17223101</ref><ref>Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues ([[designer drug]]s). (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15639609</ref>
+-FA 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-FA|2-fluoroamphetamine]] and [[4-FMA|4-fluoromethamphetamine]].<ref>The effects of non-medically used psychoactive substances on monoamine neurotransmission in rat brain (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17223101</ref><ref>Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues ([[designer drug]]s). (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15639609</ref>
 ==Chemistry==
@@ Line 13: / Line 13: @@
 ==Pharmacology==
--Fluoroamphetamine acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine producing stimulating amphetamine-like effects at lower doses and euphoric, entactogenic effects similar to MDMA at dosages above 100mg.  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 [[entactogen]]ic effects.<ref>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</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain </ref>
+-Fluoroamphetamine acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine producing stimulating amphetamine-like effects at lower doses and euphoric, entactogenic effects similar to MDMA at dosages above 100mg.  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 [[entactogen]]ic effects.<ref>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</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811</ref><ref>http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive substances on monoamine neurotransmission in rat brain </ref>
 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.<ref>2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands | http://pubs.acs.org/doi/abs/10.1021/jm00169a015</ref> 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.<ref>Effect of fluorine substitution on the agonist specificity of norepinephrine | http://www.sciencemag.org/content/204/4398/1217.short</ref> 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]].
@@ Line 84: / Line 84: @@
 Abuse of compounds within the amphetamine chemical class at high dosages for prolonged periods of time can potentially result in a stimulant psychosis that may present with a variety of symptoms (e.g., [[Paranoia|paranoia]], [[External hallucinations|hallucinations]], or [[Delusions|delusions]]).<ref>Treatment for amphetamine psychosis | [http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD003026.pub3/abstract?systemMessage=Wiley+Online+Library+will+be+disrupted+Saturday%2C+15+March+from+10%3A00-12%3A00+GMT+%2806%3A00-08%3A00+EDT%29+for+essential+maintenance]</ref> A review on treatment for amphetamine, [[dextroamphetamine]], and [[methamphetamine]] abuse-induced psychosis states that about 5–15% of users fail to recover completely.<ref>Treatment for amphetamine psychosis | [http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD003026.pub3/abstract?systemMessage=Wiley+Online+Library+will+be+disrupted+Saturday%2C+15+March+from+10%3A00-12%3A00+GMT+%2806%3A00-08%3A00+EDT%29+for+essential+maintenance]</ref><ref>Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.</ref> The same review asserts that, based upon at least one trial, [[antipsychotic]] medications effectively resolve the symptoms of acute amphetamine psychosis.<ref>Treatment for amphetamine psychosis | [http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD003026.pub3/abstract?systemMessage=Wiley+Online+Library+will+be+disrupted+Saturday%2C+15+March+from+10%3A00-12%3A00+GMT+%2806%3A00-08%3A00+EDT%29+for+essential+maintenance]</ref> Psychosis very rarely arises from therapeutic use.<ref>Stimulant Misuse: Strategies to Manage a Growing Problem | http://www.acha.org/prof_dev/ADHD_docs/ADHD_PDprogram_Article2.pdf</ref><ref>http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf</ref>
 ===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. [https://www.google.com/ Independent research] should always be done to ensure that a combination of two or more substances is safe before consumption.
+Although many substances 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. [https://www.google.com/ 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 [[stimulant]]s as it can [[increased heart rate|increase one's heart rate]] and [[increased blood pressure|blood pressure]] to dangerous levels.
 {{DangerousInteractions/Stimulants}}