Jpn. J. Pharmacol. 78 (1), 1-10 (1998)


Pharmacological Studies on the Novel Antiallergic Drug HQL-79: I. Antiallergic and Antiasthmatic Effects in Various Experimental Models

Nobutoshi Matsushita (#), Masanori Hizue, Kosuke Aritake, Kumi Hayashi, Ayumi Takada, Kazuhiko Mitsui, Masatoshi Hayashi, Ichiro Hirotsu, Yoshiyuki Kimura, Tadato Tani and Hiromichi Nakajima



New Drug Research Department, High Quality-Life Research Laboratories, Bio-Medical Division, Sumitomo Metal Industries, Ltd., 3-5 Hikaridai, Seika-cho, Souraku-gun, Kyoto 619-0237, Japan
(#) Present address for correspondence: Pharmacological Research Group, Bioclinical Research, Rohto Pharmaceutical Co., Ltd., 1-8-1, Tatsumi-nishi, Ikuno-ku, Osaka 544-8666, Japan


Abstract: The effects of oral administration of 4-benzhydryloxy-1-{3-(1H-tetrazol-5-yl)-propyl}piperidine (HQL-79), a newly synthesized antiallergic drug, in various experimental allergic and asthmatic models were investigated. HQL-79 markedly inhibited immediate hypersensitivity reactions such as passive cutaneous anaphylaxis in rats, antigen-induced bronchoconstriction and nasal vascular permeability in actively sensitized guinea pigs, like epinastine and ketotifen did. Airway eosinophilia in repeatedly antigen-exposed guinea pigs was suppressed by chronic administration of HQL-79 for 2 weeks. In another experiment, the antigen-induced late asthmatic response (LAR) in metyrapone-treated guinea pigs was also ameliorated by chronic treatment with HQL-79. Moreover, HQL-79 partially inhibited the toluene diisocyanate-induced delayed-type hypersensitivity (DTH) reaction in mice when administered chronically during the immunization period. The corticosteroid dexamethasone inhibited the airway inflammatory responses in guinea pigs and the DTH in mice. These results indicate that HQL-79 has potent inhibitory effects on the immediate hypersensitivity reactions, and when administered chronically, it also inhibits airway eosinophilia, LAR and DTH, similarly to corticosteroids.


Keywords: Antiallergic drug, Late asthmatic response, Airway inflammation, Delayed-type hypersensitivity, HQL-79


Copyrightę The Japanese Pharmacological Society 1998

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