General Information of Drug (ID: DM5LRKC)

Drug Name
L-368899 Drug Info
Synonyms
UNII-ER33G946JT; L-368899; ER33G946JT; CHEMBL1253853; L 368,899; L 368899; 148927-60-0; (S)-2-amino-N-((1S,2S,4R)-7,7-dimethyl-1-((4-o-tolylpiperazin-1-ylsulfonyl)methyl)bicyclo[2.2.1]heptan-2-yl)-4-(methylsulfonyl)butanamide; GTPL2249; SCHEMBL17423276; ZINC3923061; BDBM50326719; NCGC00485193-01; 1-(((7,7-Dimethyl-2-(2-amino-4-(methylsulfonyl)butyramido)bicyclo(2.2.1)heptan-1-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine; Butanamide, 2-amino-N-(7,7-dimethyl-1-(((4-(2-methylphenyl)-1-piperazinyl)sulfonyl)methyl)bicyclo
Indication
Disease Entry ICD 11 Status REF
Miscarriage JA00.0 Discontinued in Phase 1 [1]
Cross-matching ID
PubChem CID
9872389
CAS Number
CAS 148927-60-0
TTD Drug ID
DM5LRKC

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug(s) Targeting Oxytocin receptor (OTR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Desmopressin DMS3GVE Diabetic complication 5A2Y Approved [3]
Oxytocin DMDL27I Autism spectrum disorder 6A02 Approved [4]
Carbetocin DMUSLW3 Postpartum haemorrhage JA43 Approved [5]
ATOSIBAN DMB7WYM N. A. N. A. Phase 4 [6]
Retosiban DMOYGZF Preterm labour JB00 Phase 3 [7]
SSR149415 DMCMD93 Anxiety disorder 6B00-6B0Z Phase 2 [8]
Barusiban DMWI0X3 Androgen deficiency 5A81.1 Phase 2 [9]
FE-202767 DMDGZ1C Erectile dysfunction HA01.1 Phase 2 [4]
GSK-557296 DM3ZL2O Premature ejaculation HA03.0Z Phase 2 [10]
Pyrrolidine derivative 13 DM3VA8P N. A. N. A. Patented [11]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Oxytocin receptor (OTR) TTSCIUP OXYR_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: 2249).
2 Pharmacokinetics and disposition of the oxytocin receptor antagonist L-368,899 in rats and dogs. Drug Metab Dispos. 1997 Oct;25(10):1113-8.
3 Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88.
4 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: 369).
5 Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res. 2008;170:473-512.
6 Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9.
7 The Effect of an Oxytocin Receptor Antagonist (Retosiban, GSK221149A) on the Response of Human Myometrial Explants to Prolonged Mechanical Stretch.Endocrinology.2015 Oct;156(10):3511-6.
8 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
9 The effect of barusiban, a selective oxytocin antagonist, in threatened preterm labor at late gestational age: a randomized, double-blind, placebo-controlled trial. Am J Obstet Gynecol. 2009 Jun;200(6):627.e1-10.
10 Inhibition of ejaculation by the non-peptide oxytocin receptor antagonist GSK557296: a multi-level site of action. Br J Pharmacol. 2013 Aug;169(7):1477-85.
11 A patent review of oxytocin receptor antagonists 2013-2017.Expert Opin Ther Pat. 2017 Dec;27(12):1287-1290.