DGIdb - TIMOLOL Drug Record

TIMOLOL chembl:CHEMBL499 Approved

Alternate Names:

BETIMOL
ISTALOL
TIMOLOL
TIMOPTIC-XE
NYOGEL
BLOCADREN
TIMOLOL HEMIHYDRATE
TIMOPTIC
TIOPEX
GLAUCOL
BETIM
GLAU-OPT
TIMOLOL ANHYDROUS
(-)-S-TIMOLOL
NYO142
(S)-1-(TERT-BUTYLAMINO)-3-[(4-MORPHOLIN-4-YL-1,2,5-THIADIAZOL-3-YL)OXY]PROPAN-2-OL
chemidplus:26839-75-8
pubchem.compound:33624
drugbank:00373
chembl:CHEMBL499
rxcui:1546004

Drug Info:

Drug Class	antihypertensive agents
Year of Approval	approved before 1982
Drug Class	anti-arrhythmia agents
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	for treatment of glaucoma

(3 More Sources)

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Ferro et al., 1997, A prospective study of the effects of prolonged timolol therapy on alpha- and beta-adrenoceptor and angiotensin II receptor mediated responses in normal subjects., Br J Clin Pharmacol
Fuchsjager-Mayrl et al., 2005, Polymorphism of the beta-2 adrenoceptor and IOP lowering potency of topical timolol in healthy subjects., Mol. Vis.
Borger et al., 1998, Beta-adrenoceptor-mediated inhibition of IFN-gamma, IL-3, and GM-CSF mRNA accumulation in activated human T lymphocytes is solely mediated by the beta2-adrenoceptor subtype., Am. J. Respir. Cell Mol. Biol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Rotmensch et al., 1993, Comparisons of beta-adrenergic blocking properties of S- and R-timolol in humans., J Clin Pharmacol
Van der Graaf et al., 1995, Exposure and characterization of the action of noradrenaline at dopamine receptors mediating endothelium-independent relaxation of rat isolated small mesenteric arteries., Br. J. Pharmacol.
Wang et al., 1996, (--)-Timolol is a more potent antagonist of the positive inotropic effects of (--)-adrenaline than of those of (--)-noradrenaline in human atrium., Br J Clin Pharmacol
Nieminen et al., 2005, Polymorphisms of genes CYP2D6, ADRB1 and GNAS1 in pharmacokinetics and systemic effects of ophthalmic timolol. A pilot study., Eur. J. Clin. Pharmacol.
Bhattacharyya et al., 2002, (-)-Isoproterenol modulation of maxi-K(+) channel in nonpigmented ciliary epithelial cells through a G-protein gated pathway., Curr. Eye Res.
Hirooka et al., 2000, Suppressive actions of betaxolol on ionic currents in retinal ganglion cells may explain its neuroprotective effects., Exp. Eye Res.
Varma et al., 1999, Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium., Br. J. Pharmacol.
el Tayar N et al., 1988, Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists., J Med Chem
Edeki TI et al., 1995, Pharmacogenetic explanation for excessive beta-blockade following timolol eye drops. Potential for oral-ophthalmic drug interaction., JAMA

TIMOLOL ADRB1

Interaction Score: 3.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Beta-1 adrenergic receptor antagonist

Direct Interaction yes

Trial Name brimonidine tartrate/timolol maleate,Combigan

PMIDs:
8864321 16315032 12221524 11752352 10870519 10433496 2903243

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD
TIMOLOL ADRB2

Interaction Score: 1.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name brimonidine tartrate/timolol maleate,Combigan

Novel drug target Established target

Trial Name latanoprost + timolol,Xalcom, Xalacom

PMIDs:
10592235 9088585 16205624 9730867 11752352 8103526 8719802

Sources:
TdgClinicalTrial ChemblInteractions TEND
TIMOLOL CYP2D6

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7474246 16315032

Sources:
DTC PharmGKB

TEND: TIMOLOL
- Version: 01-August-2011
Alternate Names:

TIMOLOL Primary Drug Name

Drug Info:

Drug Class anti-arrhythmia agents

Year of Approval approved before 1982

Drug Class antihypertensive agents

Publications:
TdgClinicalTrial: TIMOLOL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications for treatment of glaucoma

Drug Class Small Molecule

FDA Approval approved

Publications:
DTC: TIMOLOL
- Version: 02-September-2020
Alternate Names:

CHEMBL499 ChEMBL Drug ID

Drug Info:

Publications:

el Tayar N et al., 1988, Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists., J Med Chem

PharmGKB: timolol

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Nieminen et al., 2005, Polymorphisms of genes CYP2D6, ADRB1 and GNAS1 in pharmacokinetics and systemic effects of ophthalmic timolol. A pilot study., Eur. J. Clin. Pharmacol.

Edeki TI et al., 1995, Pharmacogenetic explanation for excessive beta-blockade following timolol eye drops. Potential for oral-ophthalmic drug interaction., JAMA

TTD: Timolol
- Version: 2020.06.01
Alternate Names:

D05UVD TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL499
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL499
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Beta-1 adrenergic receptor antagonist
Direct Interaction	yes
Trial Name	brimonidine tartrate/timolol maleate,Combigan

Trial Name	brimonidine tartrate/timolol maleate,Combigan
Novel drug target	Established target
Trial Name	latanoprost + timolol,Xalcom, Xalacom

TIMOLOL Drug Record

TIMOLOL chembl:CHEMBL499 Approved

Alternate Names:

Drug Info:

Publications:

TIMOLOL ADRB1

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Beta-1 adrenergic receptor antagonist Direct Interaction yes Trial Name brimonidine tartrate/timolol maleate,Combigan

PMIDs: 8864321 16315032 12221524 11752352 10870519 10433496 2903243

Sources: DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

TIMOLOL ADRB2

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name brimonidine tartrate/timolol maleate,Combigan Novel drug target Established target Trial Name latanoprost + timolol,Xalcom, Xalacom

PMIDs: 10592235 9088585 16205624 9730867 11752352 8103526 8719802

Sources: TdgClinicalTrial ChemblInteractions TEND

TIMOLOL CYP2D6

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7474246 16315032

Sources: DTC PharmGKB

TEND: TIMOLOL

Alternate Names: TIMOLOL Primary Drug Name

Drug Info: Drug Class anti-arrhythmia agents Year of Approval approved before 1982 Drug Class antihypertensive agents

Publications:

TdgClinicalTrial: TIMOLOL

Alternate Names:

Drug Info: Drug Indications for treatment of glaucoma Drug Class Small Molecule FDA Approval approved

Publications:

DTC: TIMOLOL

Alternate Names: CHEMBL499 ChEMBL Drug ID

Drug Info:

Publications: el Tayar N et al., 1988, Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists., J Med Chem

PharmGKB: timolol

Alternate Names:

Drug Info:

TTD: Timolol

Alternate Names: D05UVD TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL499

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL499

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Beta-1 adrenergic receptor antagonist

Direct Interaction yes

Trial Name brimonidine tartrate/timolol maleate,Combigan

PMIDs:
8864321 16315032 12221524 11752352 10870519 10433496 2903243

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name brimonidine tartrate/timolol maleate,Combigan

Novel drug target Established target

Trial Name latanoprost + timolol,Xalcom, Xalacom

PMIDs:
10592235 9088585 16205624 9730867 11752352 8103526 8719802

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

PMIDs:
7474246 16315032

Sources:
DTC PharmGKB

Alternate Names:

TIMOLOL Primary Drug Name

Drug Info:

Drug Class anti-arrhythmia agents

Year of Approval approved before 1982

Drug Class antihypertensive agents

Drug Info:

Drug Indications for treatment of glaucoma

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL499 ChEMBL Drug ID

Publications:

el Tayar N et al., 1988, Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists., J Med Chem

Alternate Names:

D05UVD TTD Drug ID