Chemistry:YZG-331
YZG-331, also known as N6-[(S)-1-(phenyl)propyl]adenosine, is an adenosine receptor agonist which is or was under investigation for the potential treatment of insomnia.[1][2][3]
Pharmacology
The drug appears to act through the adenosine A1 and A2A receptors.[3] It produces sedative and hypnotic effects and hypolocomotion in animals.[3] The drug is orally active and crosses the blood–brain barrier, although its intestinal absorption and central permeability may be reduced by its P-glycoprotein substrate activity.[4][5] It is a synthetic derivative of adenosine and of N6-(4-hydroxybenzyl)adenine riboside (NHBA).[5][3] The latter compound is found in the traditional Chinese medicinal herb Gastrodia elata.[5][3]
Development
YZG-331 was first described in the scientific literature by at least 2014.[6] As of 2025, it has reached the preclinical research stage of development.[1]
See also
- List of investigational insomnia drugs
References
- ↑ 1.0 1.1 "Delving into the Latest Updates on YZG-331 with Synapse". 8 May 2025. https://synapse.patsnap.com/drug/5e65914168974601accb3e1169e4fb23.
- ↑ "Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery". Pharmacological Reviews 70 (2): 197–245. April 2018. doi:10.1124/pr.117.014381. PMID 29487083. "1. Adenosine Receptor Agonist. YZG-331 is a promising sedative hypnotic and adenosine analog that exerts its effects by binding to the adenosine receptor. (See the Other Receptors section for a review of the pharmacology of A1A and A2A.)".
- ↑ 3.0 3.1 3.2 3.3 3.4 "The mechanism study of YZG-331 on sedative and hypnotic effects". Behavioural Brain Research 428. June 2022. doi:10.1016/j.bbr.2022.113885. PMID 35398229.
- ↑ "Neuropharmacokinetics: a bridging tool between CNS drug development and therapeutic outcome". Drug Discovery Today 24 (5): 1166–1175. May 2019. doi:10.1016/j.drudis.2019.02.007. PMID 30898661.
- ↑ 5.0 5.1 5.2 "Effects of P-glycoprotein on the intestine and blood-brain barrier transport of YZG-331, a promising sedative-hypnotic compound". European Journal of Pharmacology 791: 339–347. November 2016. doi:10.1016/j.ejphar.2016.08.039. PMID 27612629.
- ↑ "Determination of YZG-331 in mouse plasma using liquid chromatography-tandem mass spectrometry". Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences 944: 6–10. January 2014. doi:10.1016/j.jchromb.2013.10.041. PMID 24291606.
 |  |
