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4-Methylthioamphetamine
4-Methylthioamphetamine (4-MTA), also known as para-methylthioamphetamine (MTA), is a designer drug of the substituted amphetamine class developed in the 1990s by a team led by David E. Nichols, an American pharmacologist and medical chemist, at Purdue University. It acts as a non-neurotoxic highly selective serotonin releasing agent (SSRA) in animals. 4-MTA is the methylthio derivative of amphetamine.
4-MTA is a strong serotonin releaser similar to para-methoxyamphetamine (PMA), which can cause pronounced hyperthermia potentially resulting in organ failure and death.[better source needed] Therefore, the major neuropharmacological effect is an increased release of serotonin, and the inhibition of serotonin uptake of monoamine oxidase A (MAO-A). The combination of the releasing of serotonin from neurons and the prevention of breaking this neurotransmitter down again, leads to dangerous serotonin syndrome. The serotonin syndrome is a hyper serotonergic state, which can become fatal and is a side effect of serotonergic drugs. The symptoms of serotonin syndrome caused by 4-MTA are described in the Report on the Risk Assessment of 4-MTA
Symptoms of the serotonin syndrome caused by 4-MTA
Another effect is the increase of the secretion of several hormones, like adrenocorticotropic hormone (ACTH), corticosterone, prolactin, oxytocin, and renin induced by 4-MTA through stimulation of serotonergic neurotransmission.
There has been suggested that 4-MTA because of its slow onset of action, is more dangerous than other designer drugs. Users of the drug rapidly take another dose because they assume the first was inadequate; thus increasing the possibility of an overdose. (EMCDDA, 1999)
Today the knowledge about the effects of 4-MTA is narrow, because of very limited research and experimental data. The only four studies that are conducted show a weak effect on dopamine and noradrenaline. This study was executed with a single dose of 4-MTA, no study where the effect of multiple doses 4-MTA where researched exist up to date.[citation needed]
4-MTA is a monoamine releasing agent (MRA). It was originally characterized as a selective serotonin releasing agent (SRA). However, the drug was subsequently found to more weakly induce the release of dopamine as well. 4-MTA shows a similar balance of monoamine reuptake inhibition as MDMA.
In addition to its MRA activity, 4-MTA is a potent monoamine oxidase A (MAO-A) inhibitor. Its IC50 for MAO-A inhibition has been reported to be 250 nM. The combination of serotonin release induction and MAOI activity is likely responsible for the severe serotonergic toxicity and hyperthermia that has occurred with 4-MTA.
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4-Methylthioamphetamine
4-Methylthioamphetamine (4-MTA), also known as para-methylthioamphetamine (MTA), is a designer drug of the substituted amphetamine class developed in the 1990s by a team led by David E. Nichols, an American pharmacologist and medical chemist, at Purdue University. It acts as a non-neurotoxic highly selective serotonin releasing agent (SSRA) in animals. 4-MTA is the methylthio derivative of amphetamine.
4-MTA is a strong serotonin releaser similar to para-methoxyamphetamine (PMA), which can cause pronounced hyperthermia potentially resulting in organ failure and death.[better source needed] Therefore, the major neuropharmacological effect is an increased release of serotonin, and the inhibition of serotonin uptake of monoamine oxidase A (MAO-A). The combination of the releasing of serotonin from neurons and the prevention of breaking this neurotransmitter down again, leads to dangerous serotonin syndrome. The serotonin syndrome is a hyper serotonergic state, which can become fatal and is a side effect of serotonergic drugs. The symptoms of serotonin syndrome caused by 4-MTA are described in the Report on the Risk Assessment of 4-MTA
Symptoms of the serotonin syndrome caused by 4-MTA
Another effect is the increase of the secretion of several hormones, like adrenocorticotropic hormone (ACTH), corticosterone, prolactin, oxytocin, and renin induced by 4-MTA through stimulation of serotonergic neurotransmission.
There has been suggested that 4-MTA because of its slow onset of action, is more dangerous than other designer drugs. Users of the drug rapidly take another dose because they assume the first was inadequate; thus increasing the possibility of an overdose. (EMCDDA, 1999)
Today the knowledge about the effects of 4-MTA is narrow, because of very limited research and experimental data. The only four studies that are conducted show a weak effect on dopamine and noradrenaline. This study was executed with a single dose of 4-MTA, no study where the effect of multiple doses 4-MTA where researched exist up to date.[citation needed]
4-MTA is a monoamine releasing agent (MRA). It was originally characterized as a selective serotonin releasing agent (SRA). However, the drug was subsequently found to more weakly induce the release of dopamine as well. 4-MTA shows a similar balance of monoamine reuptake inhibition as MDMA.
In addition to its MRA activity, 4-MTA is a potent monoamine oxidase A (MAO-A) inhibitor. Its IC50 for MAO-A inhibition has been reported to be 250 nM. The combination of serotonin release induction and MAOI activity is likely responsible for the severe serotonergic toxicity and hyperthermia that has occurred with 4-MTA.