We investigated the effects of F-1322 (N-[2-[4-(benzhydryloxy)piperidino]ethyl]-3-hydroxy-5-(3-pyridylmethoxy)-2-naphthamide), a new compound that inhibits both thromboxane A2 synthetase and 5-lipoxygenase and that functions as a histamine antagonist, on the Ascaris antigen-induced late asthmatic response and pulmonary eosinophilia in guinea pigs. Oral administration of F-1322 (10-100 mg/kg) inhibited the antigen-induced late asthmatic response in a dose-dependent manner. Histological analysis revealed that F-1322 prevented the accumulation of eosinophils in the airways and this was paralleled by a decrease in the number of eosinophils and lymphocytes recovered in bronchoalveolar lavage fluid. F-1322 (0.1-10 microM) inhibited eotaxin-induced chemotaxis and actin polymerization of eosinophils in vitro in a concentration-dependent manner, while oral administration of F-1322 dose-dependently suppressed the migration of eosinophils into the airways in vivo in response to infusion of interleukin 5 and eotaxin in combination. F-1322 may, thus, improve the late asthmatic response in this model, in part, by preventing the accumulation of eosinophils in the airways. The pharmacological profile of F-1322 indicates that this drug is likely to be useful in the treatment of allergic diseases such as asthma.

01 Feb 1998·European Journal of PharmacologyQ3 · MEDICINE

Inhibitory effect of F-1322 on allergic eosinophil infiltration in airways

Q3 · MEDICINE

Article

Author: Akinori Mochizuki ; Tooru Tanaka ; Itsuo Iwamoto ; Masaaki Kasai ; Bunsho Lee ; Masahiro Shibata

The effects of F-1322 (N-[2-[4-(benzhydryloxy)piperidino]ethyl]-3-hydroxy-5-(3-pyridy lmethoxy)-2-naphthamide) on antigen-induced eosinophil infiltration and interleukin-5 production in the airways and on in vitro eosinophil migration were investigated. F-1322 (10-30 mg/kg, p.o.) inhibited antigen-induced eosinophil infiltration and interleukin-5 production in the airways of sensitized mice in a dose-dependent manner. Furthermore, F-1322 (0.1-10 microM) prevented the in vitro migration of eosinophils from guinea-pigs and humans induced by recombinant human interleukin-5, platelet-activating factor, and leukotriene B4 in a concentration-dependent manner. These results indicate that F-1322 has an inhibitory effect on allergic eosinophil infiltration of the airways by preventing both eosinophil migration and interleukin-5 production. These pharmacological profiles suggest that F-1322 will be a useful therapeutic for allergic diseases, especially asthma.

01 Jan 1995·Folia Pharmacologica Japonica

Pharmacological profiles of F-1322, a novel anti-asthmatic agent. (1). Mechanisms of action.

Article

Author: Kazuhiko Takasaki ; Yasushi Higashide ; Tetsuaki Yamaura ; Bunsho Lee ; Akinori Mochizuki ; Norihiko Tamura

The pharmacological effects of N-[2-(4-(benzhydryloxy)piperidino)ethyl]-3-hydroxy-5-(3-pyridyl methoxy)-2- naphthamide (F-1322), a novel anti-asthmatic agent, was investigated in vitro. The results obtained were as follows: 1) In the isolated trachea of guinea pigs, F-1322 showed a markedly potent antagonistic action against the contraction induced by histamine, while it had little or no effect on 5-hydroxytryptamine-, acetylcholine-, leukotriene D4- or U-46619-induced contractions. 2) In rabbit platelets, F-1322 did not affect the platelet aggregation induced by platelet activating factor. 3) F-1322 significantly inhibited the thromboxane (TX) A2 synthetase (IC50 value: 1.7 x 10(-8) M) and 5-lipoxygenase (IC50 value: 9 x 10(-7) M) activities. 4) F-1322 had no effect on phospholipase A2, cyclooxygenase, Ca2+/calmodulin-dependent phosphodiesterase and phosphodiesterase activities. These in vitro studies suggest that the anti-asthmatic action of F-1322 is associated with histamine antagonism and an inhibitory action on TXA2 synthetase and 5-lipoxygenase activities.

100 Deals associated with F-1322

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	-	Nippon Chemiphar Co., Ltd.	-
Asthma	Phase 2	-	Nxera Pharma Co., Ltd.	-
Asthma	Phase 2	-	UCB SA	-
Rhinitis, Allergic	Phase 2	-	Nxera Pharma Co., Ltd.	-
Rhinitis, Allergic	Phase 2	-	UCB SA	-
Rhinitis, Allergic	Phase 2	-	Nippon Chemiphar Co., Ltd.	-

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