| Identification | Back Directory | [Name]
Tibenelast (sodium) | [CAS]
105102-18-9 | [Synonyms]
Tibenelast (sodium)
5,6-diethoxy-1-benzothiophene-2-carboxylate | [Molecular Formula]
C13H13NaO4S | [MDL Number]
MFCD00864802 | [MOL File]
105102-18-9.mol | [Molecular Weight]
290.31 |
| Hazard Information | Back Directory | [Uses]
Tibenelast sodium is a phosphodiesterase inhibitor. | [Brand name]
Tibenelast is INN. | [in vivo]
Tibenelast is a potent orally active compound against anaphylactic shock induced by high dose antigen aerosol. When a lower aerosol challenge (0.05 mg/mL) is employed, bronchoconstriction is observed with a concomitant increase in lung resistance (RL) and a fall in dynamic compliance (Cdyn). Tibenelast at 25 mg/kg p.o. prevents these changes. Tibenelast is 10 times more potent than Aminophylline by i.v. administration; normalization of pulmonary function is achieved at 1 mg/kg i.v. Tibenelast is synergistic with epinephrine. The oral dose response curve of Tibenelast is enhanced with the co-administration of epinephrine. Tibenelast may be of significant value in the treatment of asthma and other respiratory diseases[2]. | [storage]
Store at -20°C | [References]
[1] Schwertschlag US, et al. Effect of tibenelast (a phosphodiesterase inhibitor) and theophylline on isoproterenol-stimulated heart rate, cyclic AMP and norepinephrine levels. Pharmacology. 1993;46(3):142-7. DOI:10.1159/000139039
[2] Ho PP, et al. Tibenelast, 5,6-diethoxybenzo(B)thiophene-2-carboxylic acid, sodium salt (LY186655), is an orally active anti-asthma compound in the guinea pig. Life Sci. 1990;46(13):917-25. PMID:232991 |
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