Categories
MRK-409
Topic: Chemistry
From HandWiki - Reading time: 5 min
MRK-409, also known as MK-0343, is a GABAA receptor partial agonist.[1]
It was designed to be a non-sedative anxiolytic, however its development was halted because it produced sedation in humans.[2]
Pharmacodynamics
Despite lacking the benzodiazepine chemical structure, MRK-409 acts on the benzodiazepine binding site, it is therefore a nonbenzodiazepine.
MRK-409 binds to the α1, α2, α3 and α5 subunits of the GABAA receptor.[3]
In rats, it produces minimal to no sedation, however it produces sedation in humans at doses above 1 mg.[2][4]
References
- ↑ "MRK-409" (in en). https://go.drugbank.com/drugs/DB13993.
- ↑ 2.0 2.1 Atack, John R. (2010). "GABAA Receptor α2/α3 Subtype-Selective Modulators as Potential Nonsedating Anxiolytics". GABAA receptor alpha2/alpha3 subtype-selective modulators as potential nonsedating anxiolytics. Current Topics in Behavioral Neurosciences. 2. pp. 331–360. doi:10.1007/7854_2009_30. ISBN 978-3-642-02911-0.
- ↑ Atack, J. R.; Wafford, K. A.; Street, L. J.; Dawson, G. R.; Tye, S.; Van Laere, K.; Bormans, G.; Sanabria-Bohórquez, S. M. et al. (2011). "MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans". Journal of Psychopharmacology 25 (3): 314–328. doi:10.1177/0269881109354927. ISSN 1461-7285. PMID 20147571.
- ↑ Atack, J. R.; Hallett, D. J.; Tye, S.; Wafford, K. A.; Ryan, C.; Sanabria-Bohórquez, S. M.; Eng, Wai-Si; Gibson, R. E. et al. (2011). "Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist". Journal of Psychopharmacology 25 (3): 329–344. doi:10.1177/0269881109354928. ISSN 1461-7285. PMID 20156926.
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