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

General Information of Drug (ID: DM8THU2)

• Drug Name: Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info
• Synonyms: Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2; CCK-Opioid Peptide, 5; CHEMBL382409; BDBM21135; (3S)-3-[(2S)-2-[(2S)-2-(2-{[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidin-2-yl]formamido}acetamido)-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid

Indication

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

• Cross-matching ID:
  PubChem CID: 11629355
  TTD Drug ID: DM8THU2

Molecule-Related Drug Atlas

Drug(s) Targeting Gastrin/cholecystokinin type B receptor (CCKBR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pentagastrin	DMRCLZB	Diagnostic imaging	N.A.	Approved	[2]
Ceruletide	DM2WE5K	Caerulein stimulated gastric and pancreatic secretion	5A4Y	Approved	[3]
GASTRAZOLE	DMO3ITF	Duodenal ulcer	DA63	Phase 3	[4]
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[5]
Spiroglumide	DM7NJWY	Stomach disease	DA43-DA4Y	Phase 2	[6]
TT-223	DMCDMFP	Type-1 diabetes	5A10	Phase 2	[7]
Z 360	DM2M80G	Discovery agent	N.A.	Phase 2	[8]
S-0509	DM4KWEF	Ulcerative colitis	DD71	Phase 2	[9]
YF-476	DM54MAJ	Stomach ulcer	DA60.Z	Phase 2	[10]
Itriglumide	DM5UFRO	Anxiety disorder	6B00-6B0Z	Phase 2	[11]

Drug(s) Targeting Opioid receptor delta (OPRD1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Codeine	DMJX6ZG	Allergic rhinitis	CA08.0	Approved	[12]
Hydromorphone	DMHP21E	Back pain	ME84.Z	Approved	[13]
Loperamide	DMOJZQ9	Diarrhea	ME05.1	Approved	[14]
Eluxadoline	DMYZ0P1	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[15]
Oxycodone	DMXLKHV	Osteoarthritis	FA00-FA05	Approved	[16]
Butorphanol	DM5KYPJ	Pain	MG30-MG3Z	Approved	[12]
Carfentanil	DM7ADGX	N. A.	N. A.	Phase 2	[17]
Met-enkephalin	DMSZFTP	Pain	MG30-MG3Z	Phase 2	[18]
AZD-2327	DM8FZOG	Anxiety disorder	6B00-6B0Z	Phase 2	[19]
ADL-5747	DMMUPTN	Pain	MG30-MG3Z	Phase 2	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gastrin/cholecystokinin type B receptor (CCKBR)	TTVFO0U	GASR_HUMAN	Inhibitor	[1]
Opioid receptor delta (OPRD1)	TT27RFC	OPRD_HUMAN	Inhibitor	[1]

References

• [1] Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem. 2006 May 18;49(10):2868-75.
• [2] Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21.
• [3] Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
• [4] Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115.
• [5] Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
• [6] Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9.
• [7] The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98.
• [8] Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22.
• [9] Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88.
• [10] CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
• [11] Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231.
• [12] Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16.
• [13] Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. J Med Chem. 2004 Mar 11;47(6):1400-12.
• [14] Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8.
• [15] Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
• [16] Oxycodone: a pharmacological and clinical review. Clin Transl Oncol. 2007 May;9(5):298-307.
• [17] Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.
• [18] Delta-opioid receptor agonists inhibit neuromuscular transmission in human colon. Eur J Pharmacol. 1994 Sep 1;262(1-2):33-9.
• [19] Preclinical pharmacology of AZD2327: a highly selective agonist of the delta-opioid receptor. J Pharmacol Exp Ther. 2011 Jul;338(1):195-204.
• [20] 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: 317).