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

General Information of Drug (ID: DM1FX74)

• Drug Name: Bretylium Drug Info
• Synonyms: Bretylum; Bretylium tolsylate; Bretylium tosylate(USAN); N-(2-bromobenzyl)-N,N-dimethylethanaminium; N-ethyl-N,N-dimethyl-2-bromobenzenemethanaminium; Benzenemethanaminium, 2-bromo-N-ethyl-N,N-dimethyl-, salt with 4-methylbenzenesulfonic acid (1:1); (2-bromobenzyl)ethyldimethylaminium; (2-bromophenyl)methyl-ethyl-dimethylazanium; (o-Bromobenzyl)ethyldimethylammonium p-toluenesulfonate; 2-bromo-N-ethyl-N,N-dimethylbenzenemethanaminium

Indication

Disease Entry	ICD 11	Status	REF
Long QT syndrome	BC65.0	Approved	[1]
Ventricular fibrillation	BC71.1	Approved	[2]

• Therapeutic Class: Antiarrhythmic Agents
• Cross-matching ID:
  PubChem CID: 2431
  ChEBI ID: CHEBI:3172
  CAS Number: CAS 59-41-6
  TTD Drug ID: DM1FX74
  VARIDT Drug ID: DR01325
  ACDINA Drug ID: D00890

Molecule-Related Drug Atlas

Drug(s) Targeting Adrenergic receptor beta-1 (ADRB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[5]
Epinephrine	DM3KJBC	Acute asthma	CA23	Approved	[6]
Norepinephrine	DMOUC09	Alopecia	ED70	Approved	[7]
Atenolol	DMNKG1Z	Angina pectoris	BA40	Approved	[8]
Acebutolol	DM0TI4U	Hypertension	BA00-BA04	Approved	[8]
Metoprolol	DMOJ0V6	Acute coronary syndrome	BA41	Approved	[8]
Timolol	DM3NXRU	High blood pressure	BA00	Approved	[9]
Isoproterenol	DMK7MEY	Atrioventricular block		Approved	[10]
Betaxolol	DM6EUL5	Hypertension	BA00-BA04	Approved	[11]
Sotalol	DML60TN	Sinus rhythm disorder	BC9Y	Approved	[12]

Drug(s) Transported By Sodium-dependent dopamine transporter (SLC6A3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[13]
Amphetamine	DMSZQAK	Attention deficit hyperactivity disorder	6A05.Z	Approved	[14]
OPC-34712	DMHG57U	Major depressive disorder	6A70.3	Approved	[15]
Benztropine	DMGZOVN	Parkinson disease	8A00.0	Approved	[16]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor beta-1 (ADRB1)	TTR6W5O	ADRB1_HUMAN	Antagonist	[3]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Sodium-dependent dopamine transporter (SLC6A3)	DT3BA8L	SC6A3_HUMAN	Substrate	[4]

References

• [1] Bretylium FDA Label
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [3] Components of functional sympathetic control of heart rate in neonatal rats. Am J Physiol. 1985 May;248(5 Pt 2):R601-10.
• [4] Which form of dopamine is the substrate for the human dopamine transporter: the cationic or the uncharged species? J Biol Chem. 1999 Feb 19;274(8):4876-82.
• [5] Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8.
• [6] Adrenergic activation of electrogenic K+ secretion in guinea pig distal colonic epithelium: involvement of beta1- and beta2-adrenergic receptors. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G269-77.
• [7] Impact of exogenous beta-adrenergic receptor stimulation on hepatosplanchnic oxygen kinetics and metabolic activity in septic shock. Crit Care Med. 1999 Feb;27(2):325-31.
• [8] Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6.
• [9] Topical dorzolamide 2%/timolol 0.5% ophthalmic solution: a review of its use in the treatment of glaucoma and ocular hypertension. Drugs Aging. 2006;23(12):977-95.
• [10] Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404.
• [11] beta-adrenergic enhancement of brain kynurenic acid production mediated via cAMP-related protein kinase A signaling. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Apr 30;33(3):519-29.
• [12] beta(2)-adrenoceptors are critical for antidepressant treatment of neuropathic pain. Ann Neurol. 2009 Feb;65(2):218-25.
• [13] Characterization of VNTRs Within the Entire Region of SLC6A3 and Its Association with Hypertension. DNA Cell Biol. 2017 Mar;36(3):227-236.
• [14] Amphetamines, new psychoactive drugs and the monoamine transporter cycle. Trends Pharmacol Sci. 2015 Jan;36(1):41-50.
• [15] Brexpiprazole reduces hyperactivity, impulsivity, and risk-preference behavior in mice with dopamine transporter knockdown-a model of mania. Psychopharmacology (Berl). 2017 Mar;234(6):1017-1028.
• [16] Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist. J Pharmacol Exp Ther. 2014 Jan;348(1):106-15.