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

General Information of Drug (ID: DMQKGL3)

• Drug Name: 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) Drug Info
• Synonyms: CHEMBL1094129; BDBM50318264

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 46237944
  TTD Drug ID: DMQKGL3

Molecule-Related Drug Atlas

Drug(s) Targeting Glutamate receptor AMPA (GRIA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Halothane	DM80OZ5	Anaesthesia	9A78.6	Approved	[2]
E-2007	DMJDYNQ	Diabetic neuropathy	8C0Z	Approved	[3]
Zopiclone	DMPI6Z0	Insomnia	7A00-7A0Z	Approved	[4]
Sevoflurane	DMC9O43	Anaesthesia	9A78.6	Approved	[5]
Enflurane	DM0YJSB	Anaesthesia	9A78.6	Approved	[6]
Isoflurane	DMY6T31	Anaesthesia	9A78.6	Approved	[7]
Bromazepam	DMY9TCW	Anxiety disorder	6B00-6B0Z	Approved	[8]
Artemisinin SP	DMFETDK	Malaria	1F40-1F45	Approved	[9]
Dihydroergotoxine	DM5D6WZ	Alzheimer disease	8A20	Approved	[10]
Barbiturate	DMJIA6T	Anaesthesia	9A78.6	Approved	[11]

Drug(s) Targeting Glutamate receptor ionotropic kainate 1 (GRIK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Topiramate	DM82Z30	Alcohol dependence	6C40.2	Approved	[12]
LY293558	DM4N6EK	Pain	MG30-MG3Z	Phase 2	[13]
NS 1209	DM9EFH0	Epilepsy	8A60-8A68	Phase 2	[14]
NBQX	DMPHZI5	Neurological disorder	6B60	Phase 1	[15]
YM-90K	DMWRT4L	Convulsion	8A68.Z	Discontinued in Phase 2	[15]
[3H]kainate	DMMK7XU	Discovery agent	N.A.	Investigative	[16]
[3H]quisqualate	DMDQBTX	Discovery agent	N.A.	Investigative	[17]
SYM2081	DM30WDL	Discovery agent	N.A.	Investigative	[16]
DNQX	DMQXPA5	Discovery agent	N.A.	Investigative	[18]
dysiherbaine	DM0EBAF	Discovery agent	N.A.	Investigative	[16]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glutamate receptor AMPA (GRIA)	TTAN6JD	NOUNIPROTAC	Inhibitor	[1]
Glutamate receptor ionotropic kainate 1 (GRIK1)	TT0MYE2	GRIK1_HUMAN	Inhibitor	[1]

References

• [1] 4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological charact... J Med Chem. 2010 May 27;53(10):4110-8.
• [2] Reduced inhibition of cortical glutamate and GABA release by halothane in mice lacking the K+ channel, TREK-1. Br J Pharmacol. 2007 Nov;152(6):939-45.
• [3] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [4] Eszopiclone: its use in the treatment of insomnia. Neuropsychiatr Dis Treat. 2007 Aug;3(4):441-453.
• [5] Effects of sevoflurane on carrageenan- and fentanyl-induced pain hypersensitivity in Sprague-Dawley rats. Can J Anaesth. 2009 Feb;56(2):126-35.
• [6] Enflurane directly depresses glutamate AMPA and NMDA currents in mouse spinal cord motor neurons independent of actions on GABAA or glycine receptors. Anesthesiology. 2000 Oct;93(4):1075-84.
• [7] Transmembrane residues define the action of isoflurane at the GABAA receptor alpha-3 subunit. Brain Res. 2005 Jan 25;1032(1-2):30-5.
• [8] Glutamatergic and GABAergic modulations of ultrasonic vocalizations during maternal separation distress in mouse pups. Psychopharmacology (Berl). 2009 May;204(1):61-71.
• [9] GABA(A) receptor ligands and their therapeutic potentials. Curr Top Med Chem. 2002 Aug;2(8):817-32.
• [10] Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.
• [11] Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.
• [12] Development of medications for alcohol use disorders: recent advances and ongoing challenges. Expert Opin Emerg Drugs. 2005 May;10(2):323-43.
• [13] Pharmacogenetics of new analgesics. Br J Pharmacol. 2011 Jun;163(3):447-60.
• [14] The efficacy of the AMPA receptor antagonist NS1209 and lidocaine in nerve injury pain: a randomized, double-blind, placebo-controlled, three-way crossover study. Anesth Analg. 2009 Apr;108(4):1311-9.
• [15] 4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with... Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.
• [16] 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: 450).
• [17] Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotr... J Med Chem. 2008 Jul 24;51(14):4093-103.
• [18] Synthesis of chiral 1-(2'-amino-2'-carboxyethyl)-1,4-dihydro-6,7-quinoxaline-2,3-diones: alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate recep... J Med Chem. 1996 Oct 25;39(22):4430-8.