General Information of Drug (ID: DM4FKR1)

Drug Name
H-Arg-Arg-Pro-Tyr-Ile-N-Me-Leu-OH Drug Info
Synonyms CHEMBL508130; H-Arg-Arg-Pro-Tyr-Ile-N-Me-Leu-OH
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
44578943
TTD Drug ID
DM4FKR1

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Meclinertant DMBIO6E Inflammatory bowel disease DD72 Phase 2/3 [2]
ABS-212 DMZ52P6 Pain MG30-MG3Z Terminated [3]
CGX-1160 DMADYF7 Acute or chronic pain MG30-MG31 Terminated [4]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [5]
JMV458 DMC1ARG Discovery agent N.A. Investigative [6]
Neurotensin(8-13) DMOBU62 N. A. N. A. Investigative [7]
JMV449 DME9GF8 Discovery agent N.A. Investigative [8]
SR48527 DMUHQS9 Discovery agent N.A. Investigative [9]
HBN-2 DM5VDU2 Neurological disorder 6B60 Investigative [10]
[3H]meclinertant DMEX6GT Discovery agent N.A. Investigative [9]
⏷ 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
Neurotensin receptor type 1 (NTSR1) TTTUMEP NTR1_HUMAN Inhibitor [1]

References

1 Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensi... Bioorg Med Chem. 2008 Oct 15;16(20):9359-68.
2 Neurotensin inversely modulates maternal aggression. Neuroscience. 2009 Feb 18;158(4):1215-23.
3 Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic. J Med Chem. 2010 Jun 24;53(12):4623-32.
4 Clinical status of anti-cancer agents derived from marine sources. Anticancer Agents Med Chem. 2008 Aug;8(6):603-17.
5 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
6 Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2. Mol Pharmacol. 2001 Dec;60(6):1392-8.
7 Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy. J Med Chem. 2009 Apr 9;52(7):1803-13.
8 Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus. Mol Pharmacol. 2003 Aug;64(2):421-9.
9 [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor. Mol Pharmacol. 1995 May;47(5):1050-6.
10 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: 309).