MRK-016

MRK-016 is an anxiolytic drug which is a novel type of GABA-A receptor positive allosteric modulator. It was developed by Merck & Co and has been researched for potential medical use but never marketed.

Pharmacology

MRK-016 is a subtype-selective GABA-A receptor positive allosteric modulator. Unlike most GABA-A modulators, which usually produce strong sedation and ataxia in addition to anxiolytic effects, MRK-016 is anxiolytic but with little or no sedative effects, because it is selective for the α2 and α3 subtypes of the GABA-A receptor, which are responsible for the anxiolytic effects of these drugs, but does not affect the α1 subtype, which produces the sedative and ataxic effects.

Development

MRK-016 was developed by Merck & Co as part of their research program into subtype-selective GABA-A modulators. It has been researched in animal studies and shown to produce anxiolytic effects without sedation, but has not been developed for medical use and is not currently marketed.

See also

• GABA-A receptor
• Anxiolytic
• Merck & Co

MRK-016 Resources
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