H Fujisawa

Shin Nippon Biomedical Laboratories, Ltd., Kagosima, Kagoshima, Japan

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Publications (11)7.94 Total impact

  • [Show abstract] [Hide abstract]
    ABSTRACT: An antigenicity study of (+/-)-4-diethylamino-1,1-dimethylbut-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate monohydrochloride monohydrate (NS-21), a new drug for the treatment of urinary frequency and incontinence, was conducted in Hartley guinea pigs and BALB/cAnN mice. The following results were obtained. No active systemic anaphylaxis reactions were found in guinea pigs immunized by subcutaneous injection of NS-21 alone or in combination with Freund's complete adjuvant (FCA). No 24-hr heterologous passive cutaneous anaphylaxis reactions were elicited in rats by sera from mice immunized by intraperitoneal injection of NS-21 alone or in combination with 3% aluminum hydroxide gel. No passive hemagglutination reactions were elicited by sera from mice immunized by subcutaneous injection of NS-21 in combination with FCA. These results show that NS-21 has no antigenicity under the present experimental conditions.
    The Journal of Toxicological Sciences 05/1997; 22 Suppl 1(SupplementI):307-13. DOI:10.2131/jts.22.SupplementI_307 · 1.38 Impact Factor
  • Hiroshi FUJISAWA · Takeshi NISHIMURA · Kiyoshi KIMURA
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    ABSTRACT: An antigenicity study of montirelin hydrate (NS-3), a new drug for the treatment of disturbance of consciousness, was conducted in Hartley guinea pigs. Animals were sensitized twice by subcutaneous injections of montirelin hydrate in combination with Freund's complete adjuvant and twice by intramuscular injections of montirelin hydrate alone. Montirelin hydrate was found to be negative in the homologous passive cutaneous anaphylaxis test carried out with sera from the sensitized guinea pigs. Negative results were also obtained in the active cutaneous anaphylaxis test and the active systemic anaphylaxis test in guinea pigs sensitized with montilerin hydrate. These results show that montirelin hydrate has no antigenicity under the present experimental conditions.
    The Journal of Toxicological Sciences 01/1996; 20 Suppl 2(SupplementII):341-8. DOI:10.2131/jts.20.SupplementII_341 · 1.38 Impact Factor
  • Hiroshi Fujisawa · Takeshi Nishimura · Muneo Inaba · Susumu Ikehara
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    ABSTRACT: We examined the effects of actarit, a new antirheumatic drug, on antibody production after LPS stimulation in mice. Actarit did not affect the proliferative response of B-cells stimulated with LPS or anti-mouse mu-chain antibody plus rIL-4. Lymphocytes in the Peyer's patches (PP) of mice with oral administration of actarit suppressed the production of IgA (not IgM and IgG) by B-cells stimulated with LPS. Actarit affected neither the serum level of IgA nor IgA secretion from the gut of mice without LPS stimulation. Actarit did not change the percentage of Thy-1+ cells in the PP lymphocyte population or that of CD4+ or CD8+ cells in the Thy-1+ fraction of PP lymphocytes. The suppressive effect of PP lymphocytes from mice treated with actarit was abrogated by the elimination of CD4+ cells (not CD8+ cells) from PP lymphocytes. These results suggest that actarit activates CD4+ suppressor T-cells in the PP, resulting in a specific suppression of IgA production after LPS stimulation.
    International Journal of Immunopharmacology 08/1995; 17(7):611-7. DOI:10.1016/0192-0561(95)00044-3
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    ABSTRACT: The anti-inflammatory effects of etodolac (Eto) were compared with those of 6 other anti-inflammatory drugs: indomethacin (Ind), diclofenac Na (Dic), piroxicam (Pir), naproxen (Nap), ketoprofen (Ket) and aspirin (Asp). Eto inhibited carrageenin-induced edema in rats, adjuvant-induced arthritis in rats, acetic acid-induced writhing in mice and brewer's yeast-induced hyperalgesia and fever in rats. In the adjuvant arthritis test, the ED30 value (1.88 mg/kg) on day 3 and ED50 values (adjuvant-injected paw: 1.18 mg/kg and non-injected paw: 0.96 mg/kg) on day 18 for Eto were comparable to those for Dic (2.16, 1.72 and 1.28) when given prophylactically and the ED50 values for Eto (adjuvant-injected paw: 1.61 and non-injected paw: 1.20 mg/kg) were comparable to those for Ket (1.24 and 1.22) when used therapeutically. The analgesic activity of Eto (ED50 value: 3.67 mg/kg) in the acetic acid-induced writhing test was greater than that of Nap (9.83) or Asp (31.6) and less than that of Ind (0.71), Dic (1.54), Pir (0.92) or Ket (1.34). In the antipyretic test, the minimum effective dose (MED: 1 mg/kg) for Eto was comparable to that for Ind (1.0), Nap (1.0) or Ket (1.0). Eto was less potent in inhibiting carrageenin-induced edema (ED30 value: 6.99 mg/kg) and inflammatory pain (ED50 value: 9.24 mg/kg) than the other drugs (Ind: 2.32 and 3.47, Dic: 0.69 and 3.80, Pir: 1.31 and 1.94, Nap: 1.83 and 2.78, Ket: 1.12 and 0.63), except for Asp (167 and 51.8).(ABSTRACT TRUNCATED AT 250 WORDS)
    Biological & Pharmaceutical Bulletin 01/1995; 17(12):1577-83. DOI:10.1248/bpb.17.1577 · 1.78 Impact Factor
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    ABSTRACT: Lactitol hydrate (lactitol) was tested for its antigenicity in guinea pigs and mice. The following results were obtained. 1. No active systemic anaphylaxis reactions were found in guinea pigs sensitized subcutaneously with lactitol alone or in combination with Freund's complete adjuvant (FCA). 2. No 24 hr heterologous passive cutaneous anaphylaxis reactions were elicited in rats by sera from mice sensitized intraperitoneally with lactitol alone or in combination with 3% aluminum hydroxide gel. 3. No passive hemagglutination reactions were elicited by sera from mice sensitized subcutaneously with lactitol in combination with FCA. From these results, it is concluded that lactitol has no antigenicity under the present experimental conditions.
    The Journal of Toxicological Sciences 12/1994; 19 Suppl 3(SupplementIII):499-505. DOI:10.2131/jts.19.SupplementIII_499 · 1.38 Impact Factor
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    ABSTRACT: The effect of actarit (MS-932, CAS 18699-02-0), an antirheumatic drug, on type II collagen (CII)-induced arthritis in DBA/1J mice was studied. Mice were immunized twice with bovine CII, actarit being given orally once a day for 35 days after the 1st immunization. Clinical assessment showed that actarit had no effect on the incidence or day of onset of arthritis but that it lowered the arthritis score dose-dependently. Radiography showed that actarit reduced new bone formation in the limbs, and a histopathologic examination showed that it reduced synovitis, erosion of cartilage and bone destruction. Actarit suppressed the delayed-type mouse ear skin reaction to CII but had no effect on the level of serum anti-CII antibodies. These results suggest that actarit inhibits the development of CII-induced arthritis in mice by suppressing delayed-type hypersensitivity to CII.
    Arzneimittel-Forschung 02/1994; 44(1):64-8. · 0.51 Impact Factor
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    ABSTRACT: We tested the effect of etodolac on the development of type-II collagen-induced arthritis in DBA/1J mice. It was administered orally once daily for 35 days after the primary immunization with type-II collagen. Etodolac (10 mg/kg) significantly inhibited the development of signs of arthritis on day 28 to day 35. Indomethacin (1 mg/kg) also significantly inhibited it on day 29 to day 34. Radiographic examination showed that etodolac (10 mg/kg) significantly prevented the development of osteopenia, bone erosion and new bone formation of the joints on day 35, while indomethacin (1 mg/kg) significantly prevented only the development of bone erosion. Histopathological examination showed that both etodolac (10 mg/kg) and indomethacin (1 mg/kg) significantly prevented the development of synovitis, erosion of cartilage of the joints and bone destruction of the limbs on day 35. Etodolac and indomethacin did not affect the serum level of anti-type-II collagen antibodies. These results suggest that etodolac and indomethacin suppress type-II collagen-induced arthritis without affecting humoral immune responses.
    Agents and Actions 08/1993; 39(3-4):187-94. DOI:10.1007/BF01998973
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    ABSTRACT: We examined the effects of long-term administration of a newly developed anti-rheumatic drug, 4-acetylaminophenylacetic acid (actarit), on adjuvant- induced arthritis in rats and spontaneously developed arthritis in MRL/MpJ- lpr/lpr (MRL/l) mice. Actarit or lobenzarit was administered daily for 42 days starting on day 12 after adjuvant injection. Actarit at 0.1 to 100 mg/kg suppressed hind paw swelling in a dose-dependent manner on day 26 to 54. On the other hand, lobenzarit showed slight, but not significant suppression only at 100 mg/kg in the same model. Then, the effect of actarit on arthritis in MRL/l mice was studied histopathologically. Actarit was administered daily for 12 weeks starting from age 8 weeks. Actarit at 0.1 to 3 mg/kg lowered total arthritic score in a dose-dependent manner. Dose-dependent suppression of arthritis was also observed in synovial and periarticular damages. In conclusion, actarit showed dose-dependent and sustained suppressive activities on the arthritis during the long-term treatment.
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    ABSTRACT: The anti-inflammatory, analgesic, antipyretic and ulcerogenic activities of etodolac (CAS 41340-25-4), a new nonsteroidal anti-inflammatory agent, were compared with those of indometacin and other anti-inflammatory drugs in experimental animals. Etodolac had a remarkable anti-inflammatory effect in various experimental models: ultraviolet erythema, carrageenin-induced edema and swelling of adjuvant arthritis. In these models, the effective dose of etodolac was several fold that of indometacin. Etodolac inhibited prostaglandin E2 formation in a concentration-dependent manner, and its inhibitory potency was about 1/5 of that of indometacin. Etodolac also caused marked inhibition of granuloma formation and leucocyte functions such as chemotaxis, lysosomal enzyme release and active oxygen generation. These effects of etodolac were observed at similar doses of indometacin. Etodolac suppressed inflammatory pain but not non-inflammatory pain, and had an antipyretic effect but did not lower normal rectal temperature. Etodolac had no effect on delayed hypersensitivity reactions and was much less ulcerogenic than indometacin. These results indicate that etodolac is a low ulcerogenic anti-inflammatory agent with suppressing activities on leucocyte functions to the same extent as indometacin and prostaglandin biosynthesis.
    Arzneimittel-Forschung 04/1991; 41(3):228-35. · 0.51 Impact Factor
  • K Inoue · A Motonaga · T Nishimura · M Yokota · N Miki · H Fujisawa · F Ueda · Y Shibata · K Kimura
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    ABSTRACT: The effect of etodolac (CAS 41340-25-4) on the inflammatory reactions induced by histamine and bradykinin was compared with that of indomethacin and other nonsteroidal anti-inflammatory drugs. Etodolac (50 mg/kg p.o.), indomethacin (20 mg/kg p.o.), diclofenac Na (20 mg/kg p.o.) and acetylsalicylic acid (200 mg/kg p.o.) had no effect on the increase of vascular permeability induced by histamine or bradykinin and on passive cutaneous anaphylaxis in rats. Etodolac (5, 10 and 20 mg/kg p.o.) suppressed concanavalin A-induced paw edema in rats. Etodolac (10 mg/kg p.o.) and bromelain (10 mg/kg i.v.) significantly suppressed the heat-induced elevation of bradykinin in perfusates of rat paws, but indomethacin (20 mg/kg p.o.) and diclofenac Na (20 mg/kg p.o.) did not. Etodolac inhibited bradykinin-forming enzyme activity in a concentration-dependent manner (IC50 = 1.5 x 10[-4) mol/l). These results suggest that etodolac is a unique nonsteroidal anti-inflammatory drug which can inhibit bradykinin formation, unlike indomethacin or diclofenac Na.
    Arzneimittel-Forschung 04/1991; 41(3):235-9. · 0.51 Impact Factor
  • H Fujisawa · T Nishimura · Y Inoue · S Ogaya · Y Shibata · Y Nakagawa · S Sato · K Kimura
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    ABSTRACT: The antiinflammatory activity of 4-acetylaminophenylacetic acid (MS-932) was investigated. MS-932 did not suppress the acute inflammation of carrageenin-induced paw edema in rats or of primary swelling in adjuvant arthritic rats. However, prophylactic treatment with MS-932 inhibited secondary inflammation in adjuvant arthritic rats. MS-932 also restored to normal the weight of the spleen and the serum albumin/globulin ratio of adjuvant arthritic rats. In addition to its prophylactic effect, MS-932 had a therapeutic effect on adjuvant arthritis. In in vitro tests, MS-932 did not inhibit prostaglandin E2 biosynthesis from arachidonic acid by sheep seminal vesicle microsomal enzyme or superoxide generation by guinea pig neutrophils stimulated with opsonized zymosan. MS-932 had no analgesic effect in mice and no antipyretic effect in rats. These results indicate that MS-932 suppresses adjuvant arthritis through modulation of the immune system.
    Arzneimittel-Forschung 07/1990; 40(6):693-7. · 0.51 Impact Factor