Omega! benzodiazepine receptors

Langer SZ, ArbiUa S, Benavides J, et al Zolpidem and alpidem two imidazopyridines with selectivity for omega-1 and omega-3 receptor subtypes, in GABA and Benzodiazepine Receptor Subtypes. Edited by Biggio G, Costa E. New York, Raven,... 

Zolpidem and zaleplon are hypnotics that act at the omega-1 receptor of the central GABA receptor complex. This selectivity is hypothesized to be associated with a lower risk of dependence. Unlike benzodiazepines, zolpidem and zaleplon do not appear to have significant anxiolytic, muscle relaxant, or anticonvulsant properties. However, amnestic effects may occur. 

Zolpidem is a non-benzodiazepine hypnotic of the imidazopyridine class. It is a GABA receptor agonist selective for omega-1 receptor subunit. 

MOA Nonbenzodiazepine hypnotic but binds to benzodiazepine omega-1 receptor in vitro. No musde relaxant anxiolytic or anticonvuisant effects. 

Gama-aminobutyric acid (GABA) alpha-subunit or omega- or benzodiazepine-receptor. Modulation is toward enhanced function of this inhibitory CNS pathway. 

Zolpidem acts at the omega-1 subtype of the benzodiazepine receptor on the chloride channel. Like the benzodiazepines, it potentiates the actions of GABA. 

Other drugs The anxiolytic ding buspirone interacts with the S-HT, subclass of brain serotonin receptors as a partial agonist, but the precise mechanism of its anxiolytic effect is unknown. The hypnotics zolpidem and zaleplon are not benzodiazepines but appear to exert their CNS effects via interaction with certain benzodiazepine receptors, classified as BZ, or omega, subtypes their CNS depressant effects are antagonized by flumazenil. 

FIGURE 8-28. The hypnotic agent zaleplon is a rapid-onset, short-acting nonbenzodiazepine which binds to omega sites near benzodiazepine sites on GABA-A receptors. 

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