L-4-chlorokynurenine

L-4-Chlorokynurenine (also known as AV-101 or 4-Cl-KYN) is a synthetic compound and a prodrug of 7-chlorokynurenic acid (7-Cl-KYNA). It is being researched for its potential use in the treatment of various neurological disorders, including major depressive disorder and neuropathic pain.

Chemistry

L-4-Chlorokynurenine is a derivative of kynurenine, an intermediate in the tryptophan metabolism pathway. The addition of a chlorine atom at the 4 position of the kynurenine molecule results in 4-chlorokynurenine.

Pharmacology

L-4-Chlorokynurenine is a prodrug, meaning it is metabolized in the body to produce an active compound. In this case, the active compound is 7-chlorokynurenic acid, a potent and selective antagonist of the N-methyl-D-aspartate receptor (NMDAR). NMDARs are a type of ionotropic glutamate receptor, and their overactivation is thought to play a role in a number of neurological disorders.

Clinical significance

Research into L-4-Chlorokynurenine has primarily focused on its potential use in the treatment of major depressive disorder and neuropathic pain. Preclinical studies have shown promising results, with the compound demonstrating both antidepressant and analgesic effects. However, as of 2021, L-4-Chlorokynurenine is still in the early stages of clinical development, and further research is needed to fully understand its efficacy and safety profile.

See also

• Kynurenine pathway
• Glutamate (neurotransmitter)
• NMDA receptor antagonist