KRM-II-81

KRM-II-81 is a chemical compound that belongs to the class of benzodiazepine derivatives. It is a potent and selective positive allosteric modulator (PAM) of the alpha-1 subunit of the gamma-aminobutyric acid type A receptor (GABA_AR). KRM-II-81 was developed by researchers at the University of Wisconsin–Madison and is used in scientific research.

Chemistry

KRM-II-81 is a synthetic compound that is structurally related to the benzodiazepine class of drugs, which includes substances like diazepam and alprazolam. However, unlike these drugs, KRM-II-81 does not bind to the benzodiazepine binding site on the GABA_AR, but instead binds to a different site on the alpha-1 subunit of the receptor.

Pharmacology

As a PAM of the alpha-1 subunit of the GABA_AR, KRM-II-81 enhances the effect of the neurotransmitter GABA on this receptor. This results in an increase in the inhibitory effect of GABA on neuronal activity, which can lead to effects such as sedation, anxiolysis, and anticonvulsant activity.

Research

KRM-II-81 has been used in scientific research to study the role of the alpha-1 subunit of the GABA_AR in various physiological and pathological processes. For example, it has been used to investigate the role of this receptor subunit in the effects of benzodiazepine drugs and in conditions such as anxiety disorders and epilepsy.

See also

• Benzodiazepine
• Positive allosteric modulator
• [[GABA_A receptor]]
• University of Wisconsin–Madison