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Esketamine, sold under the brand names Spravato (for depression) and Ketanest (for anesthesia) among others, [10] [12] is the S(+) enantiomer of ketamine. [5] [13] It is a dissociative hallucinogen drug used as a general anesthetic and as an antidepressant for treatment of depression.
Ketamine is a mixture of equal amounts of two enantiomers: esketamine and arketamine. Esketamine is a far more potent NMDA receptor pore blocker than arketamine. [11] Pore blocking of the NMDA receptor is responsible for the anesthetic, analgesic, and psychotomimetic effects of ketamine.
After the publication of the NIH-run antidepressant clinical trial, clinics began opening in which the intravenous ketamine is given for depression. [5] [6] This practice is an off label use of IV ketamine in the United States, though the intranasal version of esketamine has been approved by the FDA for treatment of depression [5] [7] In 2015 there were about 60 such clinics in the US; the ...
Ketamine-assisted psychotherapy (KAP) is the use of prescribed doses of ketamine as an adjunct to psychotherapy sessions. KAP shows significant potential in treating mental disorders such as treatment-resistant depression (TRD), anxiety, obsessive–compulsive disorders (OCD), post-traumatic stress disorders (PTSD), and other conditions. [1]
The drug is a novel esketamine analogue and conjugate that acts as a prodrug of esketamine. [3] Esketamine, and by extension XW10508, is an NMDA receptor antagonist and indirect AMPA receptor activator. [1] [5] XW10508 is being developed as once-daily orally administered extended-release and immediate-release formulations with misuse resistance ...
Arketamine (developmental code names PCN-101, HR-071603), also known as (R)-ketamine or (R)-(−)-ketamine, is the (R)-(−) enantiomer of ketamine. [1] [2] [3] Similarly to racemic ketamine and esketamine, the S(+) enantiomer of ketamine, arketamine is biologically active; however, it is less potent as an NMDA receptor antagonist and anesthetic and thus has never been approved or marketed for ...
NMDAR antagonists like ketamine, esketamine, tiletamine, phencyclidine, nitrous oxide, and xenon are used as general anesthetics. These and similar drugs like dextromethorphan and methoxetamine also produce dissociative, hallucinogenic, and euphoriant effects and are used as recreational drugs.
Esketamine (CLE-100) – ionotropic glutamate NMDA receptor antagonist and dissociative hallucinogen – major depressive disorder – Clexio Biosciences [14] GM-2505 – serotonin 5-HT 2A and 5-HT 2C receptor agonist, psychedelic hallucinogen, and serotonin releasing agent – major depressive disorder – Gilgamesh Pharmaceuticals [ 15 ]