Hydroxynorketamine Blocks N-Methyl-d-Aspartate Receptor Currents by Binding to Closed Receptors

• Published in: Molecular pharmacology Vol. 98; no. 3; pp. 203 - 210
• Main Authors: Abbott, Jamie A., Popescu, Gabriela K.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.09.2020; The American Society for Pharmacology and Experimental Therapeutics
• Subjects: Animals; Antidepressive Agents - chemistry; Antidepressive Agents - pharmacology; Cyclohexanes - chemistry; Cyclohexanes - pharmacology; HEK293 Cells; Humans; Hydrogen-Ion Concentration; Ketamine - analogs & derivatives; Rats; Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors; Recombinant Proteins - metabolism; Synaptic Transmission - drug effects; CTR; NMDA; KET; HNK; CI; HEK

Ketamine, a dissociative anesthetic, is experiencing a clinical resurgence as a fast-acting antidepressant. In the central nervous system, ketamine acts primarily by blocking NMDA receptor currents. Although it is generally safe in a clinical setting, it can be addictive, and several of its derivati...