General Information of Drug (ID: DMI53FU)

Drug Name
Gaboxadol Drug Info
Synonyms
Gaboxadolum; Gaboxadolum [Latin]; LU 2030; Gaboxadol [USAN:INN]; Lu 02-030; MK-0928; Gaboxadol (USAN/INN); LU-2-030; Lu-02-030; Isoxazolo(5,4-c)pyridin-3(2H)-one, 4,5,6,7-tetrahydro-, hydrate; 4,5,6,7-Tetrahydroisoxazole(5,4-c)pyridin-3-ol; 4,5,6,7-tetrahydro-[1,2]oxazolo[5,4-c]pyridin-3-one
Indication
Disease Entry ICD 11 Status REF
Insomnia 7A00-7A0Z Approved [1]
Therapeutic Class
Hypnotics and Sedatives
Cross-matching ID
PubChem CID
3448
ChEBI ID
CHEBI:34373
CAS Number
CAS 64603-91-4
TTD Drug ID
DMI53FU
VARIDT Drug ID
DR00004

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Allopregnanolone DMNLHAC Depression 6A70-6A7Z approved [4]
Ganaxolone DMXJMKF Epileptic seizures 8A61-8A6Z Approved [5]
SAGE-217b DMRFK0B Major depressive disorder 6A70.3 Phase 2 [4]
PF-4480682 DMWYJHC Neuropathic pain 8E43.0 Discontinued in Phase 2 [6]
PF-2393296 DM5R2MG Neuropathic pain 8E43.0 Discontinued in Phase 1 [7]
Co-60549 DMGIZHX Anxiety disorder 6B00-6B0Z Terminated [8]
Org-20599 DMQU8AR Anaesthesia 9A78.6 Terminated [9]
TBPS DMFC3XP Discovery agent N.A. Investigative [7]
RU-5135 DMCASRD Discovery agent N.A. Investigative [10]
⏷ Show the Full List of 9 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glycine DMIOZ29 Allergic rhinitis CA08.0 Approved [11]
L-Proline DMKSTWR Malnutrition 5B50-5B71 Approved [12]
Cycloserine DMT1I52 Bacterial infection 1A00-1C4Z Approved [13]
Aminolevulinic acid hci DMS4BLQ Acne vulgaris ED80 Approved [14]
Vigabatrin DMYT0OG Alcohol dependence 6C40.2 Approved [15]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
GABA(A) receptor delta (GABRD) TTGXH6N GBRD_HUMAN Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Proton-coupled amino acid transporter 1 (SLC36A1) DT48WEM S36A1_HUMAN Substrate [3]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4322).
2 Gaboxadol--a new awakening in sleep.Curr Opin Pharmacol.2006 Feb;6(1):30-6.
3 Intestinal gaboxadol absorption via PAT1 (SLC36A1): modified absorption in vivo following co-administration of L-tryptophan. Br J Pharmacol. 2009 Aug;157(8):1380-9.
4 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
5 Ganaxolone, a selective, high-affinity steroid modulator of the gamma-aminobutyric acid-A receptor, exacerbates seizures in animal models of absence. Ann Neurol. 1998 Oct;44(4):688-91.
6 WO patent application no. 2014,1515,17, Methods of improving microvascular integrity.
7 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 416).
8 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012)
9 The anaesthetic action and modulation of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology. 1996;35(9-10):1209-22.
10 Complex interactions between the steroid derivative RU 5135 and the GABAA-receptor complex. Eur J Pharmacol. 1992 Oct 1;227(2):147-51.
11 Transport of amino acids and GABA analogues via the human proton-coupled amino acid transporter, hPAT1: characterization of conditions for affinity and transport experiments in Caco-2 cells. Eur J Pharm Sci. 2008 Sep 2;35(1-2):86-95.
12 PAT1 (SLC36A1) shows nuclear localization and affects growth of smooth muscle cells from rats. Am J Physiol Endocrinol Metab. 2014 Jan 1;306(1):E65-74.
13 Indirect regulation of the intestinal H+-coupled amino acid transporter hPAT1 (SLC36A1). J Cell Physiol. 2005 Aug;204(2):604-13.
14 Delta-aminolevulinic acid is a substrate for the amino acid transporter SLC36A1 (hPAT1). Br J Pharmacol. 2010 Mar;159(6):1339-53.
15 Rectal absorption of vigabatrin, a substrate of the proton coupled amino acid transporter (PAT1, Slc36a1), in rats. Pharm Res. 2012 Apr;29(4):1134-42.