Details of the Drug-Related molecule(s) Interaction Atlas

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] , [2]

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 Type:

DTT

DTP

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Transported By Proton-coupled amino acid transporter 1 (SLC36A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Glycine	DMIOZ29	Malnutrition	5B50-5B71	Approved	[5]
L-Proline	DMKSTWR	Malnutrition	5B50-5B71	Approved	[6]
Cycloserine	DMT1I52	Bacterial infection	1A00-1C4Z	Approved	[7]
Aminolevulinic acid hci	DMS4BLQ	Acne vulgaris	ED80	Approved	[8]
Vigabatrin	DMYT0OG	Complex partial seizure	8A68.0	Approved	[9]
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Drug(s) Targeting GABA(A) receptor delta (GABRD)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	Approved	[10]
Ganaxolone	DMXJMKF	Complex partial seizure	8A68.0	Phase 3	[11]
SAGE-217b	DMRFK0B	Major depressive disorder	6A70.3	Phase 2	[10]
PF-4480682	DMWYJHC	Neuropathic pain	8E43.0	Discontinued in Phase 2	[12]
PF-2393296	DM5R2MG	Neuropathic pain	8E43.0	Discontinued in Phase 1	[13]
Co-60549	DMGIZHX	Anxiety disorder	6B00-6B0Z	Terminated	[14]
Org-20599	DMQU8AR	Anaesthesia	9A78.6	Terminated	[15]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[13]
RU-5135	DMCASRD	Discovery agent	N.A.	Investigative	[16]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
GABA(A) receptor delta (GABRD)	TTGXH6N	GBRD_HUMAN	Modulator	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Proton-coupled amino acid transporter 1 (SLC36A1)	DT48WEM	S36A1_HUMAN	Substrate	[4]

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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	Highway driving performance and cognitive functioning the morning after bedtime and middle-of-the-night use of gaboxadol, zopiclone and zolpidem. J Sleep Res. 2009 Dec;18(4):387-96.
3	Gaboxadol--a new awakening in sleep.Curr Opin Pharmacol.2006 Feb;6(1):30-6.
4	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.
5	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.
6	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.
7	Indirect regulation of the intestinal H+-coupled amino acid transporter hPAT1 (SLC36A1). J Cell Physiol. 2005 Aug;204(2):604-13.
8	Delta-aminolevulinic acid is a substrate for the amino acid transporter SLC36A1 (hPAT1). Br J Pharmacol. 2010 Mar;159(6):1339-53.
9	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.
10	Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
11	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.
12	WO patent application no. 2014,1515,17, Methods of improving microvascular integrity.
13	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).
14	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012)
15	The anaesthetic action and modulation of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology. 1996;35(9-10):1209-22.
16	Complex interactions between the steroid derivative RU 5135 and the GABAA-receptor complex. Eur J Pharmacol. 1992 Oct 1;227(2):147-51.