RS134-49 is a
tetrahydropyridine
Tetrahydropyridines (or piperideines) are heterocycles with the formula . Three isomers exist, which differ by the location of the double bond. None of the parent species occur widely, so they are mainly of theoretical interest. Although the pa ...
derivative related to
psychedelic
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic halluci ...
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 firs ...
s which acts as a
5-HT2A receptor agonist, with a 5-HT
2A K
i of 11.5nM and an EC
50 of 22nM. It is a
biased agonist
Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the end ...
selective for activation of the
Gq coupled signalling pathway with weaker activation of the
β-arrestin 2 coupled pathway, but shows a more balanced profile than related compounds such as
(R)-69.
See also
*
Cyclized tryptamine
Substituted tryptamines, or simply tryptamines, also known as serotonin analogues (i.e., 5-hydroxytryptamine analogues), are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all trypt ...
*
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 ...
*
4-Methyl-α-methyltryptamine
*
4-Methyl-α-ethyltryptamine
*
CP-94253
CP-94253 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular pro ...
*
RU-24,969
*
SN-22
SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of ...
*
VU6067416
References
Designer drugs
N-Monoalkyltryptamines
Tetrahydropyridinylindoles
{{nervous-system-drug-stub