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

General Information of Drug (ID: DM3YG5P)

• Drug Name: GYKI-52466 Drug Info
• Synonyms: Gyki-52466; 102771-26-6; GYKI 52466; UNII-471V8NZ5X3; GYKI 52466 HCl; CHEMBL275006; CHEBI:79560; 471V8NZ5X3; 1-(p-Aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride; 4-(8-methyl-9h-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)aniline; 4-(8-Methyl-9H-1,3-dioxolo(4,5-h)(2,3)benzodiazepin-5-yl)benzenamine; Benzenamine,4-(8-methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-; Benzenamine, 4-(8-methyl-9H-1,3-dioxolo(4,5-h)(2,3)benzodiazepin-5-yl)-; C17H15N3O2

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Terminated	[1] , [2]

• Cross-matching ID:
  PubChem CID: 3538
  ChEBI ID: CHEBI:79560
  CAS Number: CAS 102771-26-6
  TTD Drug ID: DM3YG5P

Molecule-Related Drug Atlas

Drug(s) Targeting Glutamate receptor AMPA 1 (GRIA1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
E-2007	DMJDYNQ	Diabetic neuropathy	8C0Z	Approved	[4]
NBQX	DMPHZI5	Neurological disorder	6B60	Phase 1	[5]
YM-90K	DMWRT4L	Convulsion	8A68.Z	Discontinued in Phase 2	[6]
Farampator	DM76GRQ	Major depressive disorder	6A70.3	Discontinued in Phase 1	[7]
GYKI-53655	DMC0JN8	N. A.	N. A.	Terminated	[8]
Zonampanel	DM70HZD	N. A.	N. A.	Terminated	[6]
SORETOLIDE	DMTDLHG	Convulsion	8A68.Z	Terminated	[9]
[3H]kainate	DMMK7XU	Discovery agent	N.A.	Investigative	[10]
DNQX	DMQXPA5	Discovery agent	N.A.	Investigative	[11]
RPR-118723	DMLDWCB	Discovery agent	N.A.	Investigative	[12]

Drug(s) Targeting Glutamate receptor AMPA (GRIA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Halothane	DM80OZ5	Anaesthesia	9A78.6	Approved	[13]
E-2007	DMJDYNQ	Diabetic neuropathy	8C0Z	Approved	[14]
Zopiclone	DMPI6Z0	Insomnia	7A00-7A0Z	Approved	[15]
Sevoflurane	DMC9O43	Anaesthesia	9A78.6	Approved	[16]
Enflurane	DM0YJSB	Anaesthesia	9A78.6	Approved	[17]
Isoflurane	DMY6T31	Anaesthesia	9A78.6	Approved	[18]
Bromazepam	DMY9TCW	Anxiety disorder	6B00-6B0Z	Approved	[19]
Artemisinin SP	DMFETDK	Malaria	1F40-1F45	Approved	[20]
Dihydroergotoxine	DM5D6WZ	Alzheimer disease	8A20	Approved	[21]
Barbiturate	DMJIA6T	Anaesthesia	9A78.6	Approved	[22]

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	[3]
Glutamate receptor AMPA 1 (GRIA1)	TTVPQTF	GRIA1_HUMAN	Inhibitor	[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: 4210).
• [2] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005470)
• [3] New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. Bioorg Med Chem Lett. 2006 Jan 1;16(1):167-70.
• [4] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [5] Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Syn... J Med Chem. 2006 Oct 5;49(20):6015-26.
• [6] Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl gr... Bioorg Med Chem Lett. 2004 Oct 18;14(20):5107-11.
• [7] The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
• [8] Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor. J Med Chem. 1996 Jan 19;39(2):343-6.
• [9] Preclinical pharmacology of perampanel, a selective non-competitive AMPA receptor antagonist. Acta Neurol Scand Suppl. 2013;(197):19-24.
• [10] 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of pot... J Med Chem. 2008 Oct 23;51(20):6614-8.
• [11] 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.
• [12] Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity. J Med Chem. 2000 Jun 15;43(12):2371-81.
• [13] 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.
• [14] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [15] Eszopiclone: its use in the treatment of insomnia. Neuropsychiatr Dis Treat. 2007 Aug;3(4):441-453.
• [16] Effects of sevoflurane on carrageenan- and fentanyl-induced pain hypersensitivity in Sprague-Dawley rats. Can J Anaesth. 2009 Feb;56(2):126-35.
• [17] 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.
• [18] Transmembrane residues define the action of isoflurane at the GABAA receptor alpha-3 subunit. Brain Res. 2005 Jan 25;1032(1-2):30-5.
• [19] Glutamatergic and GABAergic modulations of ultrasonic vocalizations during maternal separation distress in mouse pups. Psychopharmacology (Berl). 2009 May;204(1):61-71.
• [20] GABA(A) receptor ligands and their therapeutic potentials. Curr Top Med Chem. 2002 Aug;2(8):817-32.
• [21] Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.
• [22] Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.