gaboxadol
Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP), as well as by its former developmental code names LU-2-030 and OV101, is a conformationally constrained derivative of the alkaloid and Amanita muscaria constituent muscimol. It acts as a direct GABAA receptor agonist. At lower doses, the drug has sedative and hypnotic effects, and at higher doses, it has hallucinogenic effects. Gaboxadol was studied for potential medical use as a pharmaceutical drug for a variety of indications, most notably treatment of insomnia, but was ultimately never marketed. — Wikipedia
Clinical trial activity
23 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 2003 (NCT00209937)
Timeline
Indications
Mechanism of action
- GABA receptor delta subunitAGONIST
GABRD agonist
GABA-A receptor; agonist GABA site agonist
Potent agonist at alpha4beta3delta-containing receptors.
- Gamma-aminobutyric acid receptor subunit alpha-1 (GABRA1) ↗
- Gamma-aminobutyric acid receptor subunit beta-2 (GABRB2) ↗
- Gamma-aminobutyric acid receptor subunit beta-3 (GABRB3) ↗
- Gamma-aminobutyric acid receptor subunit alpha-4 (GABRA4) ↗
- Gamma-aminobutyric acid receptor subunit alpha-3 (GABRA3) ↗
- Gamma-aminobutyric acid receptor subunit beta-1 (GABRB1) ↗
- Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2) ↗
- Gamma-aminobutyric acid receptor subunit alpha-5 (GABRA5) ↗
- Gamma-aminobutyric acid receptor subunit alpha-6 (GABRA6) ↗
- GABA receptor alpha-1 subunit
- GABA receptor beta-2 subunit
- GABA receptor alpha-4 subunit
- GABA receptor alpha-5 subunit
- GABA receptor alpha-6 subunit
- GABA receptor beta-3 subunit
- GABA receptor alpha-3 subunit
- GABA receptor alpha-2 subunit
- GABA-A receptor; GABA-A site (alpha1/beta2 interface)
- Gamma-aminobutyric acid receptor subunit alpha-1/ beta-1
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-6/beta-3
- GABA-A receptor alpha-1/beta-3
- Gamma-aminobutyric acid receptor subunit beta-1/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3
- GABA receptor beta-1 subunit
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-3
Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta agonist
Chemistry & pharmacology
SMILES
Oc1noc2c1CCNC2- Mol. weight
- 140.14 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaGaboxadol ↗
- ChEMBLCHEMBL312443 ↗
Also known as
- 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol
- 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol
- 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol
- gaboxadol
- gaboxadol
- gaboxadol
- gaboxadol
- gaboxadol
- lu-02030
- lu-02030
- lu 2030
- lu-2-030
- mk-0928
- mk-0928
- ov101
- thip
- thip
- thip
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06334419 | Phase 2 | Jan 29, 2024 | Healx Limited, University of Cincinnati |
| NCT05901480 | N/A | Jun 26, 2023 | — |
| NCT04106557 | Phase 3 | Sep 9, 2019 | Ovid Therapeutics Inc. |
| NCT03882918 | Phase 2 | Feb 25, 2019 | Ovid Therapeutics Inc. |
| NCT03697161 | Phase 2 | Sep 17, 2018 | Ovid Therapeutics Inc. |
| NCT03109756 | Phase 1 | Apr 3, 2017 | Ovid Therapeutics Inc. |
| NCT02996305 | Phase 2 | Jan 1, 2016 | Ovid Therapeutics Inc. |
| NCT00807248 | Phase 2 | Nov 1, 2008 | Lundbeck |
| NCT00420810 | Phase 3 | Sep 1, 2006 | Lundbeck, Merck |
| NCT00266344 | Phase 2 | Nov 1, 2005 | Lundbeck, Merck |
| NCT00266357 | Phase 2 | Nov 1, 2005 | Lundbeck, Merck |
| NCT00103818 | Phase 3 | Feb 1, 2005 | Lundbeck, Merck |
| NCT00102167 | Phase 3 | Feb 1, 2005 | Lundbeck, Merck |
| NCT00102154 | Phase 3 | Jan 1, 2005 | Lundbeck, Merck |
| NCT00094627 | Phase 3 | Nov 1, 2004 | Lundbeck, Merck |
| NCT00094666 | Phase 3 | Nov 1, 2004 | Lundbeck, Merck |
| NCT00095043 | Phase 3 | Oct 1, 2004 | Lundbeck, Merck |
| NCT00095069 | Phase 3 | Oct 1, 2004 | Lundbeck, Merck |
| NCT00209950 | Phase 3 | Jul 1, 2004 | Lundbeck |
| NCT00209846 | Phase 3 | Jun 1, 2004 | Lundbeck |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Lundbeck | For profit | 16 | 16 | 2 | 2003 |
| Merck | For profit | 10 | 0 | 2 | 2004 |
| Ovid Therapeutics Inc. | For profit | 5 | 5 | 3 | 2016 |
| Healx Limited | For profit | 1 | 0 | 1 | 2024 |
| University of Cincinnati | Academic/Hospital | 1 | 1 | 1 | 2024 |