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.
Abe
T
T
Department of Pharmacology, Gifu Pharmaceutical University, Japan.
Omata
T
T
Yoshida
K
K
Segawa
Y
Y
Matsuda
K
K
Nagai
H
H
D000818:Animals; D000911:Antibodies, Monoclonal / Q000032:analysis; D001200:Ascaris / Q000276:immunology; D001565:Benzoates / Q000627:therapeutic use*; D002199:Capillary Permeability / Q000187:drug effects; D002351:Carrageenan; D003877:Dermatitis, Contact / Q000188:drug therapy*; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D006636:Histamine Release / Q000187:drug effects; D007073:Immunoglobulin E / Q000032:analysis; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D009297:Nasal Mucosa / Q000098:blood supply / Q000187:drug effects; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010880:Piperidines / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy*
D000911:Antibodies, Monoclonal; D001565:Benzoates; D010880:Piperidines; C091433:ZCR 2060; D007073:Immunoglobulin E; D002351:Carrageenan