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

General Information of Drug (ID: DMZBU15)

• Drug Name: Tripelennamine Drug Info
• Synonyms: Benzoxale; Cizaron; Dehistin; Piribenzil; Pyribenzamin; Pyribenzamine; Pyridbenzamine; Resistamine; Tonaril; Tripelannamine; Tripelenamina; Tripelenamine; Tripelennamin; Tripelennamina; Tripelennaminum; Tripellenamine; Triplennamine; Vetibenzamina; Pyrinamine base; Tripelennamina [Italian]; Tripelennamine [BAN]; Tripelennamine [INN]; Ts and Blues; Pyribenzamine (TN); Pyristine (piristina); Tripelenamina [INN-Spanish]; Tripelennamine (INN); Tripelennaminum [INN-Latin]; Tripelennamine Citrate (1:1); Beta-Dimethylaminoethyl-2-pyridylaminotoluene; Beta-Dimethylaminoethyl-2-pyridylbenzylamine; Benzyl-(alpha-pyridyl)-dimethylaethylendiamin; Benzyl-(alpha-pyridyl)-dimethylaethylendiamin [German]; Benzyl-(alpha.-pyridyl)-dimethylaethylendiamin; Benzyl-.alpha.-pyridyl-dimethyl-aethylendiamin; N-benzyl-N-[2-(dimethylamino)ethyl]pyridin-2-amine; N-Benzyl-N',N'-dimethyl-N-2-pyridylethylenediamine; N,N-Dimethyl-N'-benzyl-N'-(2-pyridyl)ethylenediamine; N,N-Dimethyl-N'-benzyl-N'-(alpha-pyridyl)ethylenediamine; N-Benzyl-N',N'-dimethyl-N-(2-pyridyl)ethylenediamine; N-Benzyl-N',N'-dimethyl-N-2-(pyridylethylene)diamine; N-Benzyl-N-(2-pyridyl)-N',N'-dimethyl ethylenediamine; N,N-Dimethyl-N'-benzyl-N'-(alpha.-pyridyl)ethylenediamine; N'-benzyl-N,N-dimethyl-N'-pyridin-2-ylethane-1,2-diamine; N,N-Dimethyl-N'-(phenylmethyl)-N'-2-pyridinyl-1,2-ethanediamine; N,N-dimethyl-N'-(phenylmethyl)-N'-pyridin-2-ylethane-1,2-diamine; N-Benzyl-N',N'-Dimethyl-N-Pyridin-2-Yl-Ethane-1,2-Diamine Hydrochloride; 1,2-Ethanediamine, N,N-dimethyl-N'-(phenylmethyl)-N'-2-pyridinyl-(9CI); 2-(Benzyl(2-dimethylaminoethyl)amino)pyridine; 2-(N-Benzyl-N-(2-dimethylaminoethyl)amino)pyridine; 2-(benzyl(2-(dimethylamino)ethyl)amino)pyridine; 2-[Benzyl(2-dimethylaminoethyl)amino]pyridine; 2-[N-Benzyl-N-(2-dimethylaminoethyl)amino]pyridine

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Approved	[1]
Hypersensitivity	4A80-4A85	Approved	[2]
Urticaria	EB00-EB05	Approved	[1]
Vasomotor/allergic rhinitis	CA08	Approved	[1]
Pruritus	EC90	Investigative	[1]

• Therapeutic Class: Antiallergic Agents
• Cross-matching ID:
  PubChem CID: 5587
  ChEBI ID: CHEBI:9741
  CAS Number: CAS 91-81-6
  TTD Drug ID: DMZBU15

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine H1 receptor (H1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[6]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[7]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[8]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[9]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[10]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[8]
Doxepin	DMPI98T	Anxiety		Approved	[11]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[8]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[12]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[13]

Drug(s) Affected By Cholinesterase (BCHE)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cocaine	DMSOX7I	Anaesthesia	9A78.6	Approved	[14]
Tacrine	DM51FY6	Alzheimer disease	8A20	Approved	[15]
Galantamine	DMEO794	Alzheimer disease	8A20	Approved	[16]
Rivastigmine	DMG629M	Alzheimer disease	8A20	Approved	[17]
Donepezil	DMIYG7Z	Advanced cancer	2A00-2F9Z	Approved	[18]
Succinylcholine	DM2ET1M	Plasma cell myeloma	2A83.1	Approved	[19]
Ethopropazine	DM0N3L7	Parkinson disease	8A00.0	Approved	[15]
Dimenhydrinate	DM264B3	Meniere disease	AB31.0	Approved	[4]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[20]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[4]

Drug(s) Affected By Potassium voltage-gated channel subfamily H member 2 (KCNH2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[21]
Quinidine	DMLPICK	N. A.	N. A.	Approved	[22]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[23]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[24]
Clarithromycin	DM4M1SG	Acute maxillary sinusitis		Approved	[24]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[25]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[26]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[27]
Dofetilide	DMPN1TW	Sinus rhythm disorder	BC9Y	Approved	[28]
Flecainide	DMSQDLE	Tachyarrhythmias	BC71	Approved	[24]

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	Antagonist	[3]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cholinesterase (BCHE)	OTOH3WQ9	CHLE_HUMAN	Gene/Protein Processing	[4]
Potassium voltage-gated channel subfamily H member 2 (KCNH2)	OTZX881H	KCNH2_HUMAN	Gene/Protein Processing	[5]

References

• [1] Tripelennamine FDA Label
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [3] Involvement of histamine H1 and H2 receptors in the regulation of STAT-1 phosphorylation: inverse agonism exhibited by the receptor antagonists. Int Immunopharmacol. 2005 Jul;5(7-8):1299-309.
• [4] Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: analysis of its postulated role in synergizing organophosphate toxicity. Toxicol Appl Pharmacol. 1975 Feb;31(2):179-90.
• [5] Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
• [6] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [7] 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.
• [8] 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.
• [9] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [10] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [11] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [12] 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.
• [13] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
• [14] Increased organophosphate scavenging in a butyrylcholinesterase mutant. Chem Biol Interact. 2008 Sep 25;175(1-3):376-9. doi: 10.1016/j.cbi.2008.04.012. Epub 2008 Apr 22.
• [15] Comparative effects of cationic triarylmethane, phenoxazine and phenothiazine dyes on horse serum butyrylcholinesterase. Arch Biochem Biophys. 2008 Oct 15;478(2):201-5.
• [16] Lichens of parmelioid clade as promising multitarget neuroprotective agents. Chem Res Toxicol. 2019 Jun 17;32(6):1165-1177.
• [17] Potencies and selectivities of inhibitors of acetylcholinesterase and its molecular forms in normal and Alzheimer's disease brain. Acta Biol Hung. 2003;54(2):183-9. doi: 10.1556/ABiol.54.2003.2.7.
• [18] ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
• [19] Response of the newborn to succinlycholine injection in homozygotic atypical mothers. Anesthesiology. 1975 Jul;43(1):115-6. doi: 10.1097/00000542-197507000-00028.
• [20] Qualitative defects of pseudocholinesterase activity. Anaesthesia. 1967 Jan;22(1):55-68.
• [21] Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
• [22] Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
• [23] Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
• [24] Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
• [25] Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
• [26] Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
• [27] Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
• [28] Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.