Endozepine

Endozepines are endogenous compounds that bind to the benzodiazepine binding site on the GABA_A receptor complex. That is to say, endozepines are the natural ligands of the benzodiazepine receptor. Endozepines may have sedative effects similar to benzodiazepine medications such as diazepam, or they may have opposite effects, depending on whether they are agonists, antagonists, or inverse agonists.

Endozepines have been linked to hepatic encephalopathy and have controversially been linked to some cases of recurrent stupor.^[1] Initially, the key diagnostic test is stupor which is sensitive to the benzodiazepine receptor antagonist flumazenil in the absences of exogenous benzodiazepines.

Potential candidates for these compounds are:^[2]

oleamides
nonpeptidic endozepines such as inosine
the protein Diazepam binding inhibitor (DBI)

References

^ Cortelli, P.; Avallone, R.; Baraldi, M.; Zeneroli, ML.; Mandrioli, J.; Corsi, L.; Riva, R.; Tinuper, P.; et al. (Dec 2005). "Endozepines in recurrent stupor". Sleep Med Rev. 9 (6): 477–87. doi:10.1016/j.smrv.2005.07.003. PMID 16233983.
^ Farzampour, Z; Reimer, RJ; Huguenard, J (2015). "Endozepines". Diversity and Functions of GABA Receptors: A Tribute to Hanns Möhler, Part A. Advances in Pharmacology (San Diego, Calif.). Vol. 72. pp. 147–64. doi:10.1016/bs.apha.2014.10.005. ISBN 9780128026601. PMC 4550098. PMID 25600369.

[Cortelli-2005-1] Cortelli, P.; Avallone, R.; Baraldi, M.; Zeneroli, ML.; Mandrioli, J.; Corsi, L.; Riva, R.; Tinuper, P.; et al. (Dec 2005). "Endozepines in recurrent stupor". Sleep Med Rev. 9 (6): 477–87. doi:10.1016/j.smrv.2005.07.003. PMID 16233983.

[2] Farzampour, Z; Reimer, RJ; Huguenard, J (2015). "Endozepines". Diversity and Functions of GABA Receptors: A Tribute to Hanns Möhler, Part A. Advances in Pharmacology (San Diego, Calif.). Vol. 72. pp. 147–64. doi:10.1016/bs.apha.2014.10.005. ISBN 9780128026601. PMC 4550098. PMID 25600369.

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