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

General Information of Drug (ID: DM8LNMY)

• Drug Name: N-methyl-2-(pyridin-2-yl)ethanamine Drug Info
• Synonyms: betahistine; 5638-76-6; 2-(2-METHYLAMINOETHYL)PYRIDINE; Vasomotal; Serc base; 2-Pyridineethanamine, N-methyl-; beta-Histine; PT 9 base; Sinmenier (free base); methyl[2-(pyridin-2-yl)ethyl]amine; Betahistina; Betahistinum; 2-[2-(Methylamino)ethyl]pyridine; N-Methyl-2-pyridineethylamine; N-Methyl-2-pyridineethanamine; Betaistina [DCIT]; Serc; Betahistine [INN:BAN]; 2-(2-(Methylamino)ethyl)pyridine; N-methyl-2-pyridin-2-ylethanamine; Betahistinum [INN-Latin]; Betahistina [INN-Spanish]

Indication

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

• Cross-matching ID:
  PubChem CID: 2366
  ChEBI ID: CHEBI:35677
  CAS Number: CAS 5638-76-6
  TTD Drug ID: DM8LNMY

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine H3 receptor (H3R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pitolisant	DM8RFNJ	Excessive daytime sleepiness	MG42	Approved	[3]
SUVN-G3031	DM3BO8G	Cognitive impairment	6D71	Phase 3	[4]
JNJ-17216498	DM1GRCU	Narcolepsy	7A20	Phase 2	[5]
GSK239512	DMBJMZC	Alzheimer disease	8A20	Phase 2	[6]
JNJ-39220675	DM0WY3H	Alcohol dependence	6C40.2	Phase 2	[7]
AZD-5213	DMOZ04X	Alzheimer disease	8A20	Phase 2	[8]
Bavisant	DM6CVZ5	Attention deficit hyperactivity disorder	6A05.Z	Phase 2	[9]
ABT-288	DM7X54F	Alzheimer disease	8A20	Phase 2	[10]
SAR-110894	DMCLEXM	Alzheimer disease	8A20	Phase 2	[8]
ABT-652	DMLEO2Z	Diabetic neuropathy	8C0Z	Phase 2	[11]

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	[12]
Quinidine	DMLPICK	N. A.	N. A.	Approved	[13]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[14]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[15]
Clarithromycin	DM4M1SG	Acute maxillary sinusitis		Approved	[15]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[16]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[17]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[18]
Dofetilide	DMPN1TW	Sinus rhythm disorder	BC9Y	Approved	[19]
Flecainide	DMSQDLE	Tachyarrhythmias	BC71	Approved	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H3 receptor (H3R)	TT9JNIC	HRH3_HUMAN	Inhibitor	[1]

Drug Off-Target (DOT)

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

References

• [1] 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem. 2009 Jul 9;52(13):3855-68.
• [2] 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.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
• [6] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [7] JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41.
• [8] SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
• [9] Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
• [10] A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)
• [12] 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.
• [13] 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.
• [14] 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.
• [15] 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.
• [16] 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.
• [17] 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.
• [18] 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.
• [19] 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.