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

General Information of Drug (ID: DMQ92WF)

Drug Name

GW 468816 Drug Info

Synonyms

GW468816; SCHEMBL5750612; CHEMBL1207366; (4e)-7-chloro-4-(2-oxo-1-phenyl-3-pyrrolidinylidene)-1,2,3,4-tetrahydro-2-quinolinecarboxylic acid

Indication

Disease Entry	ICD 11	Status	REF
Tobacco dependence	6C4A.2	Discontinued in Phase 2	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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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]
M-241247	DMIY51U	Cerebrovascular ischaemia	8B1Z	Terminated	[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]
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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
Glycine receptor (GlyR)	TTZ8EM9	GLRA1_HUMAN; GLRA2_HUMAN; GLRA3_HUMAN; GLRA4_HUMAN; GLRB_HUMAN	Modulator	[2]

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References

1	Executive summary: nicotine addiction. Drugs Today (Barc). 2005 Jun;41(6):419-25.
2	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.
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	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)
10	Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007 Apr 5;50(7):1610-7.