Details of the Drug

General Information of Drug (ID: DMGLZ26)

• Drug Name: Practolol
• Synonyms: Dalzic; Eraldin; Practololo; Practololum; Praktololu; Teranol; Eralzdin Practolol; Practololo [DCIT]; Praktololu [Polish]; AY 21011; Cardiol (TN); Cordialina (TN); Dalzic (TN); Eraldin (TN); Eraldina (TN); Practololum [INN-Latin]; Praktol (TN); Pralon (TN); Teranol (TN); Practolol [USAN:BAN:INN]; N-{4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl}acetamide; N-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide; N-[4-({2-hydroxy-3-[(1-methylethyl)amino]propyl}oxy)phenyl]acetamide; N-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide; N-(4-(2-Hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)acetamide; (+-)-Practolol; 1-(4-Acetamidophenoxy)-3-isopropylamino-2-propanol; 4'-(2-Hydroxy-3-(isopropylamino)propoxy)acetanilide

Indication

Disease Entry	ICD 11	Status	REF
Cardiac arrhythmias	BC9Z	Approved	[1], [2]

• Therapeutic Class: Antiarrhythmic Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 266.34
  Topological Polar Surface Area (xlogp); 0.8
  Rotatable Bond Count (rotbonds); 7
  Hydrogen Bond Donor Count (hbonddonor); 3
  Hydrogen Bond Acceptor Count (hbondacc); 4
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [3]
  Bioavailability: 99% of drug becomes completely available to its intended biological destination(s) [4]
  Clearance: The drug present in the plasma can be removed from the body at the rate of 2.28 mL/min/kg [5]
  Half-life: The concentration or amount of drug in body reduced by one-half in 12.2 hours [5]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.93% [5]
• Chemical Identifiers:
  Formula: C14H22N2O3
  IUPAC Name: N-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide
  Canonical SMILES: CC(C)NCC(COC1=CC=C(C=C1)NC(=O)C)O
  InChI: InChI=1S/C14H22N2O3/c1-10(2)15-8-13(18)9-19-14-6-4-12(5-7-14)16-11(3)17/h4-7,10,13,15,18H,8-9H2,1-3H3,(H,16,17)
  InChIKey: DURULFYMVIFBIR-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 4883
  ChEBI ID: CHEBI:258351
  CAS Number: 6673-35-4
  DrugBank ID: DB01297
  TTD ID: D0KD1U
  INTEDE ID: DR1318

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	[2], [6]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2D6 (CYP2D6) Main DME	DECB0K3	CP2D6_HUMAN	Substrate	[7]

References

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• [5] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
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• [17] Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
• [18] Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8.
• [19] 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.
• [20] 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.
• [21] Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6.
• [22] 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.
• [23] Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404.
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