4-FA: Difference between revisions

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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 [[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>

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 ~~lead~~ 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]].

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]].

==Subjective effects==

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 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 [[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>
-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 lead 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]].
+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]].
 ==Subjective effects==