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].
Andolast (CR 2039) (i.v. or i.m.) inhibits rat passive cutaneous anaplaxis (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 anaplaxis induced by aerosolized antigen in anesthetized guinea-pigs. Delayed dose dependently the onset of bronchoconstriction induced by aerosolized antigen. |
[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.
[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.