Antiallergic effects of ZCR-2060: effect on allergic cutaneous reactions and rhinitis models in mice and rats.

The antiallergic action of 2-[2-[4-(diphenylmethyl)-1-piperadinyl] ethoxy] benzoic acid maleate (ZCR-2060) was investigated on allergic cutaneous reactions and nasal vascular permeability in mice and rats. ZCR-2060 markedly inhibited immediate allergic cutaneous reactions, including passive cutaneous anaphylaxis (PCA) in rats and mice; histamine-, compound 48/80- and calcium ionophore A 23187-induced cutaneous reactions in rats; and biphasic skin reactions mediated by monoclonal IgE antibody and epicutaneous challenge with antigen in mice, but did not affect 5-hydroxytryptamine-induced cutaneous reaction in rats. The antigen-induced nasal vascular permeability increase in actively and passively sensitized rats and histamine-induced nasal vascular permeability increase in rats (allergic rhinitis model) were clearly inhibited in a dose-dependent fashion by ZCR-2060. Moreover, ZCR-2060 significantly inhibited antigen-induced anaphylactic histamine release from rat peritoneal mast cells and carrageenin-induced paw edema in rats. These results suggest that ZCR-2060 has antiallergic effects on allergic cutaneous reactions and experimental rhinitis, probably due to histamine H1-receptor blockage and the inhibition of histamine release.
AuthorsT Abe, T Omata, K Yoshida, Y Segawa, K Matsuda, H Nagai
JournalJapanese journal of pharmacology (Jpn J Pharmacol) Vol. 66 Issue 1 Pg. 95-103 (Sep 1994) ISSN: 0021-5198 [Print] JAPAN
PMID7532246 (Publication Type: Journal Article)
Chemical References
  • Antibodies, Monoclonal
  • Benzoates
  • Piperidines
  • ZCR 2060
  • Immunoglobulin E
  • Carrageenan
  • Animals
  • Antibodies, Monoclonal (analysis)
  • Ascaris (immunology)
  • Benzoates (therapeutic use)
  • Capillary Permeability (drug effects)
  • Carrageenan
  • Dermatitis, Contact (drug therapy)
  • Edema (chemically induced, prevention & control)
  • Female
  • Histamine Release (drug effects)
  • Immunoglobulin E (analysis)
  • Male
  • Mast Cells (drug effects, metabolism)
  • Mice
  • Mice, Inbred BALB C
  • Nasal Mucosa (blood supply, drug effects)
  • Passive Cutaneous Anaphylaxis (drug effects)
  • Piperidines (therapeutic use)
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Rhinitis, Allergic, Seasonal (drug therapy)

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