JPC0323
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JPC0323, also known as ''N''-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)oleamide, is a dual
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-HT2C and 5-HT2A receptor positive allosteric modulator related to oleamide. It showed negligible
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 roughly 50other targets and did not bind to the orthosteric sites of these receptors. The drug does not affect the serotonin 5-HT2B receptor. JPC0323 showed favorable
pharmacokinetic Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to describing how the body affects a specific subs ...
properties in
preclinical research In drug development, preclinical development (also termed preclinical studies or nonclinical studies) is a stage of research that begins before clinical trials (testing in humans) and during which important feasibility, iterative testing and dr ...
. It produced hypolocomotion in a serotonin 5-HT2C receptor-dependent but not serotonin 5-HT2A receptor-dependent manner in rats, suggesting that it might be a preferential serotonin 5-HT2C receptor positive allosteric modulator ''
in vivo Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, an ...
''. The drug was not assessed in terms of
head-twitch response The head-twitch response (HTR), also sometimes known as wet dog shakes (WDS) in rats, is a rapid side-to-side head movement that occurs in mice and rats in association with serotonin 5-HT2A receptor activation. Serotonergic psychedelics like lys ...
, an animal behavioral proxy of psychedelic effects. It is unknown whether it might have
hallucinogen Hallucinogens, also known as psychedelics, entheogens, or historically as psychotomimetics, are a large and diverse class of psychoactive drugs that can produce altered states of consciousness characterized by major alterations in thought, mo ...
ic effects via serotonin 5-HT2A receptor potentiation, but its developers speculated that it might have reduced potential in this regard compared to orthosteric
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 ...
s. JPC0323 was derived as an analogue of the fatty acid amide oleamide and 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 2023. It was described as a "first-in-class" dual serotonin 5-HT2C and 5-HT2A receptor positive allosteric modulator.


See also

* 5-HT2C receptor § Positive allosteric modulators * 5-HT2A receptor § Positive allosteric modulators


References

{{Serotonin receptor modulators 5-HT2A receptor positive allosteric modulators 5-HT2C receptor positive allosteric modulators Fatty acid amides Serotonin receptor allosteric modulators Triols