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LABETALOL Drug Record

  • Summary
  • Interactions
  • Claims
  • LABETALOL chembl:CHEMBL429 Approved

    Alternate Names:

    NORMODYNE
    AH-5158A FREE BASE
    NORMOZIDE
    LABETALOL
    TRANDATE
    SCH-15719W FREE BASE
    LABETOLOL
    TRANDATE®
    5-(1-HYDROXY-2-(1-METHYL-3-PHENYLPROPYLAMINO)ETHYL)SALICYLAMIDE
    3-CARBOXAMIDO-4-HYDROXY-ALPHA-((1-METHYL-3-PHENYLPROPYLAMINO)METHYL)BENZYL ALCOHOL
    AH-5158A
    SCH-15719W
    LABETALOLUM
    NORMODYNE®
    rxcui:6185
    chembl:CHEMBL429
    pubchem.compound:3869
    chemidplus:36894-69-6
    drugbank:00598

    Drug Info:

    Year of Approval 1984
    Drug Class antihypertensive agents
    FDA Approval 1984
    Drug Class small molecule
    Drug Indications Antihypertensive Agents
    (3 More Sources)

    Publications:

    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Chan SW et al., 2013, CYP2C19 genotype has a major influence on labetalol pharmacokinetics in healthy male Chinese subjects., Eur J Clin Pharmacol
    Rosendorff, 1993, Beta-blocking agents with vasodilator activity., J Hypertens Suppl
    Doggrell, 1988, Relaxant and beta 2-adrenoceptor blocking activities of labetalol, dilevalol, amosulalol and KF-4317 on the rat isolated aorta., J. Pharm. Pharmacol.
    Sassard et al., 1983, [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient]., J Pharmacol
    Doggrell, 1992, The effects of labetalol and dilevalol on isolated cardiovascular preparations of the guinea-pig and rat., J. Pharm. Pharmacol.
    van Zwieten, 1993, An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists., Drugs
    Pujos et al., 2009, Comparison of the analysis of beta-blockers by different techniques., J. Chromatogr. B Analyt. Technol. Biomed. Life Sci.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Monopoli et al., 1984, Effects of the R, R-isomer of labetalol, SCH 19927, in isolated tissues and in spontaneously hypertensive rats during a repeated treatment., Arch Int Pharmacodyn Ther
    Nakagawa et al., 1981, [Antihypertensive effects of labetalol in three types of hypertensive models of rats (author's transl)]., Nippon Yakurigaku Zasshi
    Riva et al., 1991, The alpha- and beta-adrenoceptor blocking activities of labetalol and its RR-SR (50:50) stereoisomers., Br. J. Pharmacol.
    Gozalbes R et al., 2013, Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches., Bioorg Med Chem
    Nakamura et al., 1999, Tamsulosin: assessment of affinityof (3)H-P razosin binding to two alpha-1- adrenoceptor subtypes in the canine aorta., Pharmacology
    Bernstein et al., 1989, Partial attenuation of hemodynamic responses to rapid sequence induction and intubation with labetalol., J Clin Anesth
    Shiraishi et al., 1992, Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta--do they distinguish between subtypes?, Gen. Pharmacol.
    Pedersen et al., 2007, The vasodilatory beta-blockers., Curr. Hypertens. Rep.
    Hylander et al., 1985, Effects of long-term therapy with labetalol on lipoprotein metabolism in patients with mild hypertension., Acta Med Scand
    Yeh et al., 2006, Reduced expression of endothelial connexins 43 and 37 in hypertensive rats is rectified after 7-day carvedilol treatment., Am. J. Hypertens.
  • LABETALOL   GJA1

    Interaction Score: 1.72

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16448880


    Sources:
    NCI

  • LABETALOL   HPSE

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23415087


    Sources:
    DTC

  • LABETALOL   ADRB1

    Interaction Score: 0.62

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    8104240 6151824 7286847 6355664 7684671 1687367 19879818 11752352


    Sources:
    TdgClinicalTrial TEND

  • LABETALOL   LPL

    Interaction Score: 0.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    4050551


    Sources:
    NCI

  • LABETALOL   ADRA1A

    Interaction Score: 0.53

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10529655 8104240 2696507 1358746 6355664 7684671 17686376


    Sources:
    TdgClinicalTrial TEND

  • LABETALOL   ADRB2

    Interaction Score: 0.36

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    8104240 2907566 6355664 1361547 7684671 19879818 11752352


    Sources:
    TdgClinicalTrial TEND

  • LABETALOL   ADRA1B

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TEND

  • LABETALOL   CYP2C19

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300 23090703


    Sources:
    DTC PharmGKB

  • LABETALOL   CYP2C9

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LABETALOL   CYP1A2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LABETALOL   CYP2D6

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • LABETALOL   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TEND: LABETALOL

    • Version: 01-August-2011

    Alternate Names:
    LABETALOL Primary Drug Name

    Drug Info:
    Drug Class antihypertensive agents
    Year of Approval 1984

    Publications:

  • TdgClinicalTrial: LABETALOL

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Antihypertensive Agents
    Drug Class small molecule
    FDA Approval 1984

    Publications:

  • NCI: LABETALOL

    • Version: 14-September-2017

    Alternate Names:
    C29146 NCI drug code

    Drug Info:

    Publications:
    Hylander et al., 1985, Effects of long-term therapy with labetalol on lipoprotein metabolism in patients with mild hypertension., Acta Med Scand
    Yeh et al., 2006, Reduced expression of endothelial connexins 43 and 37 in hypertensive rats is rectified after 7-day carvedilol treatment., Am. J. Hypertens.

  • DTC: LABETALOL

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL429 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Gozalbes R et al., 2013, Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches., Bioorg Med Chem

  • PharmGKB: labetalol

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Chan SW et al., 2013, CYP2C19 genotype has a major influence on labetalol pharmacokinetics in healthy male Chinese subjects., Eur J Clin Pharmacol

  • TTD: Labetalol

    • Version: 2020.06.01

    Alternate Names:
    D0A8XN TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL429

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21