Drug intelligence / Profile preview

deschloroketamine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intranasal, Intramuscular, Intravenous
01

Overview

Deschloroketamine is a small-molecule dissociative anesthetic of the arylcyclohexylamine class and a structural analogue of ketamine in which the 2-chloro substituent on the phenyl ring has been removed.[1][4][14] Like ketamine and other arylcyclohexylamines, it acts primarily as a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, producing dissociative, anesthetic, analgesic and hallucinogenic effects and has emerged on the grey/illicit market as a “research chemical” designer drug with higher potency and longer duration than ketamine.[1][4][9][16][20] Preclinical work indicates that racemic deschloroketamine and its enantiomers show NMDA receptor antagonist activity comparable to ketamine, with S-deschloroketamine somewhat more potent, and that the compound rapidly crosses the blood–brain barrier and alters locomotion, reward-related behavior and sensorimotor gating in rodents.[3][9][16][18] It has been proposed, largely at the patent/speculative level, for low-dose use as an antimicrobial and immunomodulatory agent and as a potential rapid-acting antidepressant analogous to ketamine, but there are no approved medical indications and it is primarily encountered as an abused dissociative with ketamine-like bladder toxicity and possible immunologic and antimicrobial effects of uncertain clinical significance.[1][3][4][9][16][19][20]

Other names
DCKDXE2'-Oxo-PCMO-PCM2-oxo-PCM2-oxo-phenylcyclohexylmethylamine2-phenyl-2-(methylamino)cyclohexanone
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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