Home Neuronal Signaling Adrenergic Receptor antagonist Timolol Maleate For research use only.

Timolol Maleate

Synonyms: MK-950,(S)-Timolol Maleate

Timolol Maleate (MK-950,(S)-Timolol Maleate) is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.

Timolol Maleate Chemical Structure

Timolol Maleate Chemical Structure

CAS No. 26921-17-5

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Timolol Maleate Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Biological Activity

Description Timolol Maleate (MK-950,(S)-Timolol Maleate) is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.
Targets
β1-adrenergic receptor [2] β2-adrenergic receptor [2]
1.97 nM(Ki) 2.0 nM(Ki)
In vitro
In vitro

Timolol Maleate is a beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. [1] Timolol has a higher affinity for the beta 2-adrenoceptor than for the beta 1-adrenoceptor in human atrium. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. [3] Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. [4] Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at β1-adrenergic receptors in the heart and vascular smooth muscle and β2-receptors in the bronchial and vascular smooth muscle. β1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. β2-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04828057 Completed
Ocular Surface Disease|Primary Open Angle Glaucoma
Santen Pharmaceutical (Taiwan) Co. LTD
 September 1 2021 --
NCT03282981 Completed
Chronic Diabetic Foot Ulcers|Diabetic Neuropathic Ulcers|Non Healing Wound
VA Office of Research and Development|VA Northern California Health Care System
 June 14 2018 Phase 3
NCT04903366 Completed
Glaucoma Open-Angle|Chronic Wounds
VA Northern California Health Care System
 November 21 2017 --

Chemical Information & Solubility

Molecular Weight 432.49 Formula

C13H24N4O3S.C4H4O4
CAS No. 26921-17-5 SDF Download Timolol Maleate SDF
Smiles CC(C)(C)NCC(COC1=NSN=C1N2CCOCC2)O.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (198.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble


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