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MS-245 is a
tryptamine Tryptamine is an indolamine metabolite of the essential amino acid, tryptophan. The chemical structure is defined by an indole ─ a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the f ...
derivative used in
scientific research The scientific method is an empirical method for acquiring knowledge that has characterized the development of science since at least the 17th century (with notable practitioners in previous centuries; see the article history of scientific ...
. It acts as a selective 5-HT6 receptor antagonist with a Ki of 2.3 nM, and was derived through structure-activity relationship development of the selective 5-HT6 agonist
EMDT 2-Ethyl-5-methoxy-''N'',''N''-dimethyltryptamine (EMDT) is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 16 nM, and was one of the first selective agonists developed ...
. It has been used as a
lead compound A lead compound (, i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but ...
for further development of tryptamine-derived 5-HT6 antagonists. In animal studies it has been shown to boost the activity of, but not substitute for, both
amphetamine Amphetamine (contracted from alpha- methylphenethylamine) is a strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. It is also commonly used ...
and nicotine.


See also

*
EMDT 2-Ethyl-5-methoxy-''N'',''N''-dimethyltryptamine (EMDT) is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 16 nM, and was one of the first selective agonists developed ...


References

{{Tryptamines 5-HT6 antagonists Tryptamines Phenol ethers