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

General Information of Drug (ID: DMQCL6Y)

• Drug Name: UR-PG146 Drug Info
• Synonyms: CHEMBL513056; UR-PG146; GTPL1200; BDBM50413173

Indication

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

• Cross-matching ID:
  PubChem CID: 25149519
  CAS Number: CAS 888491-51-8
  TTD Drug ID: DMQCL6Y

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine H2 receptor (H2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ranitidine	DM0GUSX	Gastric ulcer	DA60	Approved	[3]
Cimetidine	DMH61ZB	Acid-reflux disorder	DA22	Approved	[4]
Famotidine	DMRL3AB	Gastric ulcer	DA60	Approved	[4]
Nizatidine	DMGFV3Z	Acid-reflux disorder	DA22	Approved	[5]
Betazole	DMUFGAY	Gastric secretory disorder	DD90	Approved	[6]
Ebrotidine	DMV5KR3	Duodenal ulcer	DA63	Withdrawn from market	[7]
Pibutidine	DMXSTRM	Ulcerative colitis	DD71	Discontinued in Phase 3	[8]
Osutidine	DMN7TL8	Duodenal ulcer	DA63	Discontinued in Phase 3	[9]
KU-1257	DMZMFX6	Duodenal ulcer	DA63	Discontinued in Phase 3	[10]
Lavoltidine	DMTY5VE	Gastroesophageal reflux disease	DA22.Z	Discontinued in Phase 2	[11]

Drug(s) Targeting Histamine H1 receptor (H1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[12]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[13]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[14]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[15]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[16]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[14]
Doxepin	DMPI98T	Anxiety		Approved	[17]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[14]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[18]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Agonist	[2]
Histamine H2 receptor (H2R)	TTQHJ1K	HRH2_HUMAN	Agonist	[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: 1200).
• [2] Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines. J Pharmacol Exp Ther. 2006 Apr;317(1):139-46.
• [3] Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
• [4] Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5.
• [5] Does the use of nizatidine, as a pro-kinetic agent, improve gastric emptying in patients post-oesophagectomy J Gastrointest Surg. 2009 Mar;13(3):432-7.
• [6] Effect of nizatidine and cimetidine on betazole-stimulated gastric secretion of normal subjects: comparison of effects on acid, water, and pepsin. Am J Gastroenterol. 1988 Jan;83(1):32-6.
• [7] Histamine H2-receptor antagonist action of ebrotidine. Effects on gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat. Arzneimittelforschung. 1997 Apr;47(4A):439-46.
• [8] Comparative pharmacology of epibatidine: a potent agonist for neuronal nicotinic acetylcholine receptors. Mol Pharmacol. 1995 Oct;48(4):774-82.
• [9] Effects of osutidine (T-593) and its enantiomers on gastric mucosal hemodynamics and mucosal integrity in anesthetized rats. Arzneimittelforschung. 2001 Jan;51(1):46-50.
• [10] Pharmacological profiles of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy] propyl] urea. Arzneimittelforschung. 1993 Feb;43(2):129-33.
• [11] New and Future Drug Development for Gastroesophageal Reflux Disease. J Neurogastroenterol Motil. 2014 January; 20(1): 6-16.
• [12] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [13] Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
• [14] Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
• [15] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [16] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [17] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [18] Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
• [19] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.