(''R'')-69 (3IQ) is a tetrahydropyridine derivative which acts as a
5-HT2A receptor agonist, with 4.6x selectivity over
5-HT2B and 49x selectivity over
5-HT2C. It has a 5-HT
2A K
i of 680nM and an EC
50 of 41nM. (''R'')-69 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 referen ...
selective for activation of the
Gq coupled signalling pathway, with much weaker activation of the
β-arrestin 2
Beta-arrestin-2, also known as arrestin beta-2, is an intracellular protein that in humans is encoded by the ''ARRB2'' gene.
Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G prot ...
coupled pathway. In animal studies it produces
antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
-like activity but without producing the
head-twitch response The head-twitch response (HTR) is a rapid side-to-side head movement that occurs in mice and rats after the serotonin 5-HT2A receptor is activated. The prefrontal cortex may be the neuroanatomical locus mediating the HTR. Many serotonergic hallucino ...
associated with
psychedelic
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary states of consciousness (known as psychedelic experiences or "trips").Pollan, Michael (2018). ''How to Change Your Mind: What the New Science of ...
effects.
See also
*
AAZ-A-154
AAZ-A-154 is a novel isotryptamine derivative which acts as a 5-HT2A receptor, 5-HT2A receptor agonist discovered and synthesized by the lab of Professor David E. Olson at University of California, Davis, UCDavis. Animal studies suggest that it ...
*
RU-24969
*
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 19nM at 5HT2 subtypes vs 514 nM at 5-HT1A receptors. Many related derivatives are known, most of which are ligand ...
References
Designer drugs
Pyrrolopyridines
Tetrahydropyridines
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