ROD-188 is a
sedative drug that was structurally derived from the
GABAA antagonist bicuculline by a team at Roche. Unlike bicuculline, ROD-188 acts as an
agonist at GABA
A receptors, being a positive allosteric modulator acting at a novel binding site distinct from those of
benzodiazepines,
barbiturates or
muscimol
Muscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of '' Amanita muscaria'' and related species of mushroom. Muscimol is a potent and selective orthosteric agonist for the GABAA receptors and displa ...
, with its strongest effect produced at the α6β2γ2 subtype of the GABA
A receptor. ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.
See also
*
Bicuculline
References
Sedatives
Tetrahydroisoquinolines
Tetrahydrofurans
Furanones
GABAA receptor positive allosteric modulators
GABAA-rho receptor negative allosteric modulators
p-Tosyl compounds
Sulfonamides
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