A non-selective β-adrenergic receptor antagonist with log Kd values of -8.27

Timolol (maleate) – 100 mg

Brand:
Cayman
CAS:
26921-17-5
Storage:
-20
UN-No:
Non-Hazardous - /

Timolol is a non-selective β-adrenergic receptor antagonist with log Kd values of -8.27, -9.86, and -6.8 for binding to human β1-, β2-, and β3-adrenoceptors, respectively.{25151} It has been reported that only the (S) enantiomer contributes to the β-blocking effects of racemic timolol, but the weakly active (R) isomer maintains a beneficial effect on intraocular pressure without the undesirable side-effect of bronchial constriction caused by non-selective action of (S)-timolol on β1 and β2 receptors.{13497,25396} Timolol has been use alone and in fixed combinations with either prostaglandin analogs or carbonic anhydrase inhibitors to reduce intraocular pressure in research models of ocular hypertension and glaucoma.{23436,16983}  

 

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Description

A non-selective β-adrenergic receptor antagonist with log Kd values of -8.27, -9.86, and -6.8 for binding to human β1-, β2-, and β3-adrenoceptors, respectively; used to reduce intraocular pressure in research models of ocular hypertension and glaucoma

Formal name: (2S)-1-[(1,1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol, 2Z-butenedioate

Synonyms:  (S)-Timolol (maleate)|MK-950|WP934

Molecular weight: 432.5

CAS: 26921-17-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Ophthalmology

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