GHB agonist
GHB receptor agonist
- Effects overlap substantially with GABA-B signaling
- Promotes slow-wave sleep — consolidates night sleep in narcolepsy
- Euphoria/abuse liability and steep dose-response
- GHB receptor effects are modest and hard to separate from GABA-B
- ➔ clinical effects of prescription GHB (oxybate) are mainly via GABA-B, not GHB-R
- May increase glutamatergic signaling
- Restorative slow-wave sleep
- Dose- and circuit-dependent dopamine effects
- Often produces early ↓ dopamine signaling → sedation, heaviness
- May produce later ↑ dopamine signaling → euphoria, sociability, reinforcement ◇ drives club drug use
- ↓ seizure threshold
Drugs with this mechanism (2)
- GHB (Oxybate) — Oxybate GHB/GABA-B agonist for narcolepsy; powerful respiratory depressant with abuse risk.
- Mixed-salt oxybates — Lower-sodium mixed oxybate for narcolepsy and idiopathic hypersomnia; dispensed under a REMS.
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