| Identification | Back Directory | [Name]
4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide | [CAS]
132640-22-3 | [Synonyms]
CR2039
CR-2039
CR 2039
Dizolast)
Andolast free base
Andolast (Synonyms: CR 2039
4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide
Benzamide, 4-(2H-tetrazol-5-yl)-N-[4-(2H-tetrazol-5-yl)phenyl]- | [Molecular Formula]
C15H11N9O | [MDL Number]
MFCD00864642 | [MOL File]
132640-22-3.mol | [Molecular Weight]
333.31 |
| Hazard Information | Back Directory | [Uses]
Andolast (CR 2039) (free base) is an anti-allergic agent. Andolast can inhibit cAMP-phosphodiesterase with an IC50 value of 50 μM. Andolast can be used for the research of asthma[1]. | [in vivo]
Andolast (CR 2039) (i.v. or i.m.) inhibits rat passive cutaneous anaphylaxis (PCA) with an ED50 of 0.1 mg/kg[1].
CR 2039 (10-100 mg/kg; i.v. or i.m.) inhibits the microvascular permeability changes in a model of allergic conjunctivitis in sensitized guinea-pigs[1].
CR 2039 (0-1000 μM; i.v.) inhibits dose dependently guinea-pig lung cAMP-phosphodiesterase with an IC50 value of 50 μM[1]. | Animal Model: | Male Hartley guinea-pigs (300-500 g) [1] | | Dosage: | 10-100 mg/kg | | Administration: | I.M; I.V. | | Result: | Showed dose-related significant protection against lgE-dependent bronchial anaphylaxis induced by aerosolized antigen in anesthetized guinea-pigs.
Delayed dose dependently the onset of bronchoconstriction induced by aerosolized antigen.
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| [References]
[1] Revel L, Colombo S, Ferrari F, Folco G, Rovati LC, Makovec F. CR 2039, a new bis-(1H-tetrazol-5-yl)phenylbenzamide derivative with potential for the topical treatment of asthma. Eur J Pharmacol. 1992;229(1):45-53. DOI:10.1016/0014-2999(92)90284-b
[2] Czuczwar SJ, Gasior M, Kozicka M, Pietrasiewicz T, Turski WA, Kleinrok Z. A potential anti-asthmatic drug, CR 2039, enhances the anticonvulsive activity of some antiepileptic drugs against pentetrazol in mice. Eur Neuropsychopharmacol. 1998;8(3):233-238. DOI:10.1016/s0924-977x(97)00077-1 |
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