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

General Information of Drug (ID: DMIY51U)

• Drug Name: M-241247 Drug Info
• Synonyms: M-244249; NMDA/glycine antagonists, Zeneca

Indication

Disease Entry	ICD 11	Status	REF
Cerebrovascular ischaemia	8B1Z	Terminated	[1]

• Cross-matching ID: TTD Drug ID: DMIY51U

Molecule-Related Drug Atlas

Drug(s) Targeting Glycine receptor (GlyR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[3]
ZD-9379	DM3KYO4	Cerebrovascular ischaemia	8B1Z	Phase 1	[4]
UK-240455	DMSCXB7	Nerve injury	ND56.4	Phase 1	[5]
MDL-27531	DMC60S8	Epilepsy	8A60-8A68	Phase 1	[6]
Gavestinel	DM8IL1U	Nerve injury	ND56.4	Discontinued in Phase 2	[7]
GV-196771	DMFN21T	Migraine	8A80	Discontinued in Phase 2	[8]
GW 468816	DMQ92WF	Tobacco dependence	6C4A.2	Discontinued in Phase 2	[9]
GINKOLIDE B	DMLIM7B	Sepsis	1G40-1G41	Terminated	[10]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine	DME8VPC	Discovery agent	N.A.	Investigative	[3]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine	DMXFVD1	Discovery agent	N.A.	Investigative	[3]

Drug(s) Targeting N-methyl-D-aspartate receptor (NMDAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
L-glutamic acid	DM4PUDW	Schizophrenia	6A20	Approved	[11]
Cycloserine	DMT1I52	Bacterial infection	1A00-1C4Z	Approved	[12]
Benzphetamine	DMIJATC	Obesity	5B81	Approved	[13]
Ketamine	DMT5HA4	Anaesthesia	9A78.6	Approved	[14]
Felbamate	DM1V5ZS	Epilepsy	8A60-8A68	Approved	[15]
Memantine	DMD9WSC	Alzheimer disease	8A20	Approved	[16]
Huperzine A	DMMAWLU	Alzheimer disease	8A20	Approved	[17]
Levorphanol	DMGS80V	Pain	MG30-MG3Z	Approved	[18]
Magnesium Sulfate	DMVEK07	Acute pain	MG31	Approved	[19]
Magnesium	DMU4ORS	Ischemic stroke	8B11.5Z	Approved	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glycine receptor (GlyR)	TTZ8EM9	GLRA1_HUMAN; GLRA2_HUMAN; GLRA3_HUMAN; GLRA4_HUMAN; GLRB_HUMAN	Antagonist	[2]
N-methyl-D-aspartate receptor (NMDAR)	TT9IK2Z	NOUNIPROTAC	Antagonist	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)
• [2] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)
• [3] 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
• [4] Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotox Res. 2002 Mar;4(2):119-26.
• [5] UK-315716/UK-240455. Pfizer. Curr Opin Investig Drugs. 2001 Dec;2(12):1737-9.
• [6] MDL 27,531 reduces spontaneous hindlimb contractions in rats with chronic transections of the spinal cord. Neurosci Lett. 1992 Nov 23;147(1):101-5.
• [7] Glycine antagonist (gavestinel) in neuroprotection (GAIN International) in patients with acute stroke: a randomised controlled trial.GAIN International Investigators.Lancet.2000 Jun 3;355(9219):1949-54.
• [8] First time in human for GV196771: interspecies scaling applied on dose selection. J Clin Pharmacol. 1999 Jun;39(6):560-6.
• [9] A double-blind, placebo-controlled trial of the NMDA glycine site antagonist, GW468816, for prevention of relapse to smoking in females.J Clin Psychopharmacol.2011 Oct;31(5):597-602.
• [10] Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007 Apr 5;50(7):1610-7.
• [11] Altered expression of genes involved in GABAergic transmission and neuromodulation of granule cell activity in the cerebellum of schizophrenia pati... Am J Psychiatry. 2008 Dec;165(12):1594-603.
• [12] How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73.
• [13] Amphetamine inhibits the N-methyl-D-aspartate receptor-mediated responses by directly interacting with the receptor/channel complex. J Pharmacol Exp Ther. 2002 Mar;300(3):1008-16.
• [14] Ketamine modulates theta and gamma oscillations. J Cogn Neurosci. 2010 Jul;22(7):1452-64.
• [15] Molecular determinants of the anticonvulsant felbamate binding site in the N-methyl-D-aspartate receptor. J Med Chem. 2008 Mar 27;51(6):1534-45.
• [16] The NMDA receptor antagonist memantine as a symptomatological and neuroprotective treatment for Alzheimer's disease: preclinical evidence. Int J Geriatr Psychiatry. 2003 Sep;18(Suppl 1):S23-32.
• [17] Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43.
• [18] Neuroprotective agents for the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2003 Jan;3(1):9-20.
• [19] Magnesium sulfate diminishes the effects of amide local anesthetics in rat sciatic-nerve block. Reg Anesth Pain Med. 2007 Jul-Aug;32(4):288-95.
• [20] Emerging drugs for acute ischemic stroke. Expert Opin Emerg Drugs. 2009 Mar;14(1):33-42.