EMD-386088
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EMD-386088 is an
indole Indole is an organic compound with the formula . Indole is classified as an aromatic heterocycle. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indoles are derivatives of indole ...
derivative which is used in
scientific research The scientific method is an empirical method for acquiring knowledge that has been referred to while doing science since at least the 17th century. Historically, it was developed through the centuries from the ancient and medieval world. The ...
. It acts as a potent 5-HT6 receptor
partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...
, with a Ki of 1 nM, a significantly higher
affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ...
than older 5-HT6 agonists such as EMDT, although it possesses moderate affinity for the 5-HT3 receptor as well. Subsequent research has determined that EMD-386088 is also a
dopamine reuptake inhibitor A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dop ...
and that this action is involved in the
antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ...
-like effects of the drug in rodents. EMD-386088 can be further reacted with a butyrophenone sidechain.Genus Possanza, Kurt Freter, & Sven Luttke, (1976 to Boehringer Ingelheim GmbH).


See also

* 2-Methyltryptamine * EMDT * RU-24,969 *
RU-28253 RU-28253 is a non-selective serotonin receptor agonist of the tryptamine and 5-methoxytryptamine families. It is a tetrahydropyridylindole and a conformationally constrained analogue of 5-MeO-DMT. The drug shows high affinity for the serotonin ...
* ST-1936


References

5-HT6 agonists Chloroarenes Dopamine reuptake inhibitors Tetrahydropyridinylindoles {{Nervous-system-drug-stub