Basic information Safety Supplier Related

4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide

Basic information Safety Supplier Related

4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide Basic information

Product Name:
4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide
Synonyms:
  • 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]-
  • Andolast (Synonyms: CR 2039
  • Dizolast)
  • CR 2039
  • CR2039
  • CR-2039
  • Andolast free base
CAS:
132640-22-3
MF:
C15H11N9O
MW:
333.31
Mol File:
132640-22-3.mol
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4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide Chemical Properties

Density 
1.551±0.06 g/cm3(Predicted)
pka
3.78±0.10(Predicted)
form 
Solid
color 
White to off-white
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4-(1H-tetrazol-5-yl)-N-(4-(1H-tetrazol-5-yl)phenyl)benzamide Usage And Synthesis

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.

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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