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

General Information of Drug (ID: DMW8YDR)

• Drug Name: GR138676 Drug Info
• Synonyms: GR 138676; GR-138676

Indication

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

• Cross-matching ID:
  PubChem CID: 25088319
  TTD Drug ID: DMW8YDR

Molecule-Related Drug Atlas

Drug(s) Targeting Neuromedin-K receptor (TACR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fezolinetant	DMHDQZD	Hot flushes	GA30	Approved	[3]
Elinzanetant	DMC6EFI	Hot flushes	GA30	Phase 3	[4]
Senktide	DMOH8LD	Epilepsy	8A60-8A68	Phase 2	[5]
AZD2624	DMZLGQV	Multiple sclerosis	8A40	Phase 2	[6]
Talnetant	DMQKZDT	Schizophrenia	6A20	Phase 2	[7]
GSK1144814	DMK3S9J	Alcohol dependence	6C40.2	Phase 1	[8]
Osanetant	DMMT4PB	Schizoaffective disorder	6A21	Discontinued in Phase 2b	[7]
CS-003	DM1AEVT	Chronic obstructive pulmonary disease	CA22	Discontinued in Phase 2	[9]
SSR-146977	DMR9JA8	Psychotic disorder	6A20-6A25	Discontinued in Phase 1	[10]
SB222200	DM6X0PZ	Schizoaffective disorder	6A21	Preclinical	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Neuromedin-K receptor (TACR3)	TTBPGLU	NK3R_HUMAN	Antagonist	[2]

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: 2128).
• [2] GR138676, a novel peptidic tachykinin antagonist which is potent at NK3 receptors. Neuropeptides. 1994 Dec;27(6):333-41.
• [3] Fezolinetant for treatment of moderate-to-severe vasomotor symptoms associated with menopause (SKYLIGHT 1): a phase 3 randomised controlled study. Lancet. 2023 Apr 1;401(10382):1091-1102.
• [4] Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
• [5] Implication of nigral tachykinin NK3 receptors in the maintenance of hypertension in spontaneously hypertensive rats: a pharmacologic and autoradiographic study. Br J Pharmacol. 2003 Feb;138(4):554-63.
• [6] The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study.J Clin Psychopharmacol.2014 Apr;34(2):199-204.
• [7] Pharmacological characterization of senktide-induced tail whips. Neuropharmacology. 2010 Jan;58(1):259-67.
• [8] Pharmacokinetics and central nervous system effects of the novel dual NK1 /NK3 receptor antagonist GSK1144814 in alcohol-intoxicated volunteers.Br J Clin Pharmacol.2013 May;75(5):1328-39.
• [9] Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
• [10] Biochemical and pharmacological activities of SSR 146977, a new potent nonpeptide tachykinin NK3 receptor antagonist. Can J Physiol Pharmacol. 2002 May;80(5):482-8.
• [11] Evidence for mediation of nociception by injection of the NK-3 receptor agonist, senktide, into the dorsal periaqueductal gray of rats. Psychopharmacology (Berl). 2009 May;204(1):13-24.