DGIdb - LABETALOL Drug Record

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:

Novel drug target	Established target
Trial Name	-

Trial Name	-
Novel drug target	Established target

Novel drug target	Established target
Trial Name	-

Trial Name	-
Novel drug target	Established target

LABETALOL Drug Record

LABETALOL chembl:CHEMBL429 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16448880

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23415087

Sources: DTC

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 4050551

Sources: NCI

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

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

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300 23090703

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

TEND: LABETALOL

Alternate Names: LABETALOL Primary Drug Name

Drug Info: Drug Class antihypertensive agents Year of Approval 1984

Publications:

TdgClinicalTrial: LABETALOL

Alternate Names:

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

Publications:

NCI: LABETALOL

Alternate Names: C29146 NCI drug code

Drug Info:

DTC: LABETALOL

Alternate Names: CHEMBL429 ChEMBL Drug ID

Drug Info:

PharmGKB: labetalol

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

Alternate Names: D0A8XN TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL429

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
16448880

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
23415087

Sources:
DTC

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

Interaction Types & Directionality:

n/a

PMIDs:
4050551

Sources:
NCI

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

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

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
22931300 23090703

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Alternate Names:

LABETALOL Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1984

Drug Info:

Drug Indications Antihypertensive Agents

Drug Class small molecule

FDA Approval 1984

Alternate Names:

C29146 NCI drug code

Alternate Names:

CHEMBL429 ChEMBL Drug ID

Publications:

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

Alternate Names:

D0A8XN TTD Drug ID