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

General Information of Drug (ID: DMAUHQX)

• Drug Name: Methdilazine Drug Info
• Synonyms: Disyncram; Methdilazinum; Methodilazine; Metodilazina; Tacaryl; Tacazyl; Tacryl; Methilazine hydrochloride; Methdilazine (INN); Methdilazinum [INN-Latin]; Metodilazina [INN-Spanish]; Tacaryl (TN); Methdilazine [USAN:INN:BAN]; 10-((1-Methyl-3-pyrrolidinyl)methyl)phenothiazine; 10-((1-methyl-3-pyrrolidinyl)methyl)-10H-phenothiazine; 10-[(1-Methylpyrrolidin-3-yl)methyl]phenothiazine; 10-[(1-methylpyrrolidin-3-yl)methyl]-10H-phenothiazine

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Approved	[1]
Angioedema	4A00.15	Approved	[2]
Urticaria	EB00-EB05	Approved	[2]
Pruritus	EC90	Investigative	[2]

• Therapeutic Class: Antihistamines
• Cross-matching ID:
  PubChem CID: 14677
  ChEBI ID: CHEBI:6823
  CAS Number: CAS 1982-37-2
  TTD Drug ID: DMAUHQX

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	[5]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[6]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[7]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[8]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[9]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[7]
Doxepin	DMPI98T	Anxiety		Approved	[10]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[7]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[11]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[12]

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	[13]
Quinidine	DMLPICK	N. A.	N. A.	Approved	[14]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[15]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[16]
Clarithromycin	DM4M1SG	Acute maxillary sinusitis		Approved	[16]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[17]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[18]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[19]
Dofetilide	DMPN1TW	Sinus rhythm disorder	BC9Y	Approved	[20]
Flecainide	DMSQDLE	Tachyarrhythmias	BC71	Approved	[16]

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
Potassium voltage-gated channel subfamily H member 2 (KCNH2)	OTZX881H	KCNH2_HUMAN	Gene/Protein Processing	[4]

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: 7231).
• [2] Methdilazine FDA Label
• [3] Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4.
• [4] 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.
• [5] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [6] 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.
• [7] 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.
• [8] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [9] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [10] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [11] 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.
• [12] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
• [13] 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.
• [14] 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.
• [15] 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.
• [16] 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.
• [17] 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.
• [18] 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.
• [19] 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.
• [20] 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.