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Psychoplastogen
Psychoplastogens, also known as neuroplastogens, are a group of small molecule drugs that produce rapid and sustained effects on neuronal structure and function, intended to manifest therapeutic benefit after a single administration.
Several existing psychoplastogens have been identified and their therapeutic effects demonstrated; several are presently at various stages of development as medications including ketamine, MDMA, scopolamine, and the serotonergic psychedelics, including LSD, psilocin (the active metabolite of psilocybin), DMT, and 5-MeO-DMT.
Compounds of this sort are being explored as therapeutics for a variety of brain disorders including depression, addiction, and PTSD. The ability to rapidly promote neuronal changes via mechanisms of neuroplasticity was recently discovered as the common therapeutic activity and mechanism of action.
The term psychoplastogen comes from the Greek roots psych- (mind), -plast (molded), and -gen (producing) and covers a variety of chemotypes and receptor targets. It was coined by David E. Olson in collaboration with Valentina Popescu, both at the University of California, Davis.
The term neuroplastogen is sometimes used as a synonym for psychoplastogen, especially when speaking to the biological substrate rather than the therapeutic.
Recently, zelquistinel, a synaptic plasticity-enhancing NMDA receptor modulator, has also been identified as a neuroplastogen, owing to its rapid onset and sustained duration of action after just one administration. Zelquistinel because of its sustained duration of action has been described as having "event-driven pharmacology" a term originally used to describe targeted protein degraders.
Psychoplastogens come in a variety of chemotypes and chemical families, but, by definition, are small-molecule drugs. Ketamine has been described as, "the prototypical psychoplastogen".
Psychoplastogens exert their effects by promoting structural and functional neural plasticity through diverse targets including, but not limited to, 5-HT2A, NMDA, and muscarinic receptors. Some are biased agonists. While each compound may have a different receptor binding profile, signaling appears to converge at the tyrosine kinase B (TrkB) and mammalian target of rapamycin (mTOR) pathways. Convergence at TrkB and mTOR parallels that of traditional antidepressants with known efficacies, but with more rapid onset. Although many serotonin 5-HT2A receptor agonists are known to produce psychoplastogenic effects, serotonin itself is not psychoplastogenic owing to poor lipophilicity and inability to activate intracellular serotonin 5-HT2A receptors.
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Psychoplastogen
Psychoplastogens, also known as neuroplastogens, are a group of small molecule drugs that produce rapid and sustained effects on neuronal structure and function, intended to manifest therapeutic benefit after a single administration.
Several existing psychoplastogens have been identified and their therapeutic effects demonstrated; several are presently at various stages of development as medications including ketamine, MDMA, scopolamine, and the serotonergic psychedelics, including LSD, psilocin (the active metabolite of psilocybin), DMT, and 5-MeO-DMT.
Compounds of this sort are being explored as therapeutics for a variety of brain disorders including depression, addiction, and PTSD. The ability to rapidly promote neuronal changes via mechanisms of neuroplasticity was recently discovered as the common therapeutic activity and mechanism of action.
The term psychoplastogen comes from the Greek roots psych- (mind), -plast (molded), and -gen (producing) and covers a variety of chemotypes and receptor targets. It was coined by David E. Olson in collaboration with Valentina Popescu, both at the University of California, Davis.
The term neuroplastogen is sometimes used as a synonym for psychoplastogen, especially when speaking to the biological substrate rather than the therapeutic.
Recently, zelquistinel, a synaptic plasticity-enhancing NMDA receptor modulator, has also been identified as a neuroplastogen, owing to its rapid onset and sustained duration of action after just one administration. Zelquistinel because of its sustained duration of action has been described as having "event-driven pharmacology" a term originally used to describe targeted protein degraders.
Psychoplastogens come in a variety of chemotypes and chemical families, but, by definition, are small-molecule drugs. Ketamine has been described as, "the prototypical psychoplastogen".
Psychoplastogens exert their effects by promoting structural and functional neural plasticity through diverse targets including, but not limited to, 5-HT2A, NMDA, and muscarinic receptors. Some are biased agonists. While each compound may have a different receptor binding profile, signaling appears to converge at the tyrosine kinase B (TrkB) and mammalian target of rapamycin (mTOR) pathways. Convergence at TrkB and mTOR parallels that of traditional antidepressants with known efficacies, but with more rapid onset. Although many serotonin 5-HT2A receptor agonists are known to produce psychoplastogenic effects, serotonin itself is not psychoplastogenic owing to poor lipophilicity and inability to activate intracellular serotonin 5-HT2A receptors.