RU-24,969 is a
serotonin receptor modulator
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both ex ...
related to
5-MeO-DMT
5-MeO-DMT (5-methoxy-''N'',''N''-dimethyltryptamine), also known as ''O''-methylbufotenin or mebufotenin (), is a naturally occurring psychedelic of the tryptamine family. It is found in a wide variety of plant species, and is also secreted by ...
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 is a
selective agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
of the
serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...
5-HT1A and
5-HT1B receptors, with 5-fold preference for the latter receptor over the former.
In studies, its
affinities (K
i) were 2nM for the serotonin
5-HT1 receptor, 5nM for the serotonin 5-HT
1A receptor, 4nM for the serotonin 5-HT
1B receptor, 780 to 1,000nM for the serotonin
5-HT2 receptor, and 400nM for the serotonin
5-HT2C receptor.
It also has
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 ...
for the serotonin
5-HT5A,
5-HT5B, and
5-HT7 receptors.
The drug produces
MDMA
3,4-Methylenedioxymethamphetamine (MDMA), commonly known as ecstasy (tablet form), and molly (crystal form), is an empathogen–entactogenic drug with stimulant and minor Psychedelic drug, psychedelic properties. In studies, it has been used ...
-like
locomotor hyperactivity
Locomotor activity is a measure of animal behavior which is employed in scientific research.
Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in whi ...
in animals and this is thought to be mediated by activation of both serotonin 5-HT
1A and 5-HT
1B receptors.
As with other serotonin 5-HT
1B receptor agonists such as
CP-94,253
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 has also been found to increase the
reinforcing
In behavioral psychology, reinforcement refers to consequences that increase the likelihood of an organism's future behavior, typically in the presence of a particular '' antecedent stimulus''. For example, a rat can be trained to push a lever ...
properties of
cocaine
Cocaine is a tropane alkaloid and central nervous system stimulant, derived primarily from the leaves of two South American coca plants, ''Erythroxylum coca'' and ''Erythroxylum novogranatense, E. novogranatense'', which are cultivated a ...
in animals, suggesting a role for serotonin 5-HT
1B receptors in
cocaine addiction
Cocaine dependence is a neurological disorder that is characterized by withdrawal symptoms upon cessation from cocaine use. It also often coincides with cocaine addiction which is a biopsychosocial disorder characterized by persistent use of ...
as well.
RU-24,969 was first described in the
scientific literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical ...
by 1980.
See also
*
EMD-386088
EMD-386088 is an indole derivative which is used in scientific research. It acts as a potent 5-HT6 receptor partial agonist, with a Ki of 1 nM, a significantly higher affinity than older 5-HT6 agonists such as EMDT, although it possesses mode ...
*
RS134-49
RS134-49 is a tetrahydropyridine derivative related to psychedelic tryptamines which acts as a 5-HT2A receptor agonist, with a 5-HT2A Ki of 11.5nM and an EC50 of 22nM. It is a biased agonist selective for activation of the Gq coupled signalling ...
*
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 ...
*
RU-28306
RU-28306 is a synthetic indole alkaloid derivative which acts as a serotonin receptor agonist, with selectivity for 5-HT1 and 5-HT2 subtypes. It can be regarded as a conformationally restricted tricyclic derivative of DMT or a structurally simp ...
*
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 ...
References
External links
RU-24969 - Isomer Design
5-HT1A agonists
5-HT1B agonists
5-HT7 agonists
Methoxy compounds
Phenol ethers
Tetrahydropyridinylindoles
{{Nervous-system-drug-stub