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Biomedical subjects

A Onodera

Publications and source records attributed to A Onodera.

At least 37 records · Page 2Linked to original sources
PubMed1992

Studies on cephalosporin antibiotics. VI. Synthesis, antibacterial activity and oral efficacy in mice of new 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(hydroxyimino)-acetamido]-3- (substituted alkylthio)cephalosporins.

A series of new 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(hydroxyimino)acetamido] cephalosporins (1) having various substituted alkylthio groups at the C-3 position of the cephem nucleus were prepared and evaluated for antibacterial activity and oral absorption in rats. Of these, the cephalosporin with a cyanomethylthio group (1a) showed the greatest activity against Staphylococcus aureus and Gram-negative bacteria. Its pivaloyloxymethyl ester (6a), a representative prodrug, exhibited good in vivo efficacy in mice by oral administration. The structure-activity relationships of 1 are also presented.

Administration, Oral↗
PubMed1992

Studies on cephalosporin antibiotics. V. Synthesis, antibacterial activity and oral absorption of new 3-[(Z)-2-methoxycarbonylvinylthio]-7 beta- [(Z)-2-(2-aminothiazol-4-yl)-2-(oxyimino)acetamido]cephalosporins.

A series of new 3-[(Z)-2-methoxycarbonylvinylthio]-7 beta-[(2- aminothiazol-4-yl)acetamido]-cephalosporins (1) having various oxyimino groups (Z-form) at the alpha position of the C-7 side chain was synthesized and evaluated for antibacterial activity and oral absorption in rats. Of these, the cephalosporin (1a) with a hydroxyimino group in the C-7 side chain showed a potent antibacterial activity against Gram-negative bacteria and Gram-positive Staphylococcus aureus as well as good oral absorption in rats. The structure-activity relationships of 1 are also presented.

Absorption↗
PubMed1992

Airway response by neurokinin A.

We studied the effect of neurokinin A (NKA) on tracheal smooth muscle (TSM) contraction induced by the administration of acetylcholine (ACh) intra-arterially (ia) into the tracheal circulation or bilateral vagal stimulation in 18 mongrel dogs. In five dogs, 10(-12) to 10(-7) mol of NKA was injected selectively into the tracheal circulation. The tracheal contractile response to 10(-7) mol NKA was 3.12 +/- 0.48 g/cm, 6.3 +/- 0.7% AChmax. Plasma histamine concentration in the right atrium was measured at the peak response to NKA. Plasma histamine concentration was 3.33 +/- 2.05 ng/ml after 10(-7) mol NKA (vs 0.32 +/- 0.08 ng/ml for control, p > 0.10). In the other 5 dogs, dose-response was obtained with 10(-12) to 10(-7) mol ACh 10 min before and 10 min after administration of 10(-8) mol NKA. Frequency-response relationship also was induced by electrical stimulation of the distal cut ends of the cervical vagi in the range of frequencies 1-20 Hz (constant 30 V) at 15-s intervals 10 min before and after administration of 10(-8) NKA. Considerable potentiation of the tracheal contractile response to 10(-18) to 10(-7) mol ia ACh occurred 10 min after administration of 10(-8) mol NKA (p < 0.05). Significant potentiation of the tracheal contraction to vagal stimulation at 10-20 Hz was also observed 10 min after administration of 10(-8) mol NKA (p < 0.05). We demonstrate that the substantial contractile effects of NKA on canine tracheal smooth muscle are not related to histamine release from mast cells in the respiratory tract.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetylcholine↗
PubMed1991

Studies on cephalosporin antibiotics. IV. Synthesis, antibacterial activity and oral absorption of new 3-(2-substituted-vinylthio)-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2- (carboxymethoxyimino)acetamido]cephalosporins.

A series of new 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)ace tamido] cephalosporins (1) having various substituted-vinylthio groups at the C-3 position of the cephen nucleus was synthesized and evaluated for antibacterial activity and oral absorption in rats in comparison with cefixime. Of these, the cephalosporins (1a and 1c) with a lower alkoxycarbonylvinylthio group (Z-form) at the C-3 position showed a potent antibacterial activity against Gram-negative bacteria, improved activity against Staphylococcus aureus as well as good oral absorption in rats. The structure-activity relationships of 1 are also presented.

Administration, Oral↗
PubMed1991

Studies on cephalosporin antibiotics. III. Synthesis, antibacterial activity and oral absorption of new 3-(substituted-alkylthio)-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2- (carboxymethoxyimino)acetamido]cephalosporins.

The synthesis, antibacterial activity and oral absorption in rats of new 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)ace tamido] cephalosporins (1) having various substituted-alkylthio groups at the C-3 position of the cephem nucleus are described. Of these, the cephalosporins with a cyanomethylthio group (1d) and fluoroethylthio group (1p) at the C-3 position showed a potent in vitro antibacterial activity against Gram-positive and Gram-negative bacteria as well as good oral absorption in rats. When administered orally to mice infected with Klebsiella pneumoniae, 1d had stronger protective effect than 1p. The structure-activity relationships of 1 are also presented.

Administration, Oral↗
PubMed1991

[Measurement of isometric tracheal tension induced by injection into tracheal arterial circulation in vivo].

In order to evaluate isometric tension in segments of tracheal smooth muscle in vivo, we first investigated the anatomical distribution of arteries supplying the tracheal smooth muscle in 52 dogs. The patterns of the cranial thyroid arteries were classified into the following four types. A) Common type: the cranial thyroid artery leaves the muscular branch, and then divides into the thyroid branch and the tracheal branch. B) The cranial thyroid artery leaves the tracheal branch, and then divides into the muscular branch and the thyroid branch. C) The cranial thyroid artery divides into the muscular branch, the thyroid branch, and the tracheal branch. D) The cranial thyroid artery divides into the tracheal branch and thyroid branch, and lacks a muscular branch. Out of 52 dogs, 62% had common type bilaterally, and 23% had common type unilaterally. All dogs had a tracheal branch. We demonstrated tracheal smooth muscle contraction by intra-arterial administration of acetylcholine, histamine, 5-hydroxy-tryptamine, phenylephrine, and clonidine using isometric technique in vivo. These results suggest that tracheal contraction induced by sympathetic amines is mediated through two subtypes of receptors, alpha 1 and alpha 2, in tracheal smooth muscle.

Acetylcholine↗
PubMed1991

[The bronchodilating effect of pirenzepine].

The purpose of this study was to clarify the bronchodilating effect of pirenzepine (PZ) and to verify its mechanism. Ten asthmatic patients (6 men, 4 women: aged 20 to 65, 5 atopic 5 non-atopic) and ten non-asthmatic volunteers (8 men, 2 women: aged 25 to 60) were studied. Forced vital capacity (FVC), forced expiratory volume in one second (FEV1.0) and peak expiratory flow rate (PEFR) were measured after intravenous administration of 20 mg PZ. PZ increased FVC, FEV1.0 and PEFR significantly by 15%, 29% and 37% respectively in asthmatic patients (p less than 0.01). We also studied the effects of PZ on the contractile responses of tracheal smooth muscle to intra-arterially administered acetylcholine (ACh) and the electrical stimulation of the vagus nerves (VNS) using isometric technique in situ in 5 mongrel dogs. PZ significantly inhibited the contractile responses elicited with ACh at doses larger than 1000 micrograms/kg (p less than 0.01). PZ also significantly inhibited the contractile responses elicited by VNS at doses larger than 100 micrograms/kg (p less than 0.01). These data demonstrate that intravenously administered PZ dilates the airway in asthmatic patients and also suggest that the bronchodilating effect of PZ related to inhibition of the M1 and M3 muscarinic receptors.

Acetylcholine↗
PubMed1990

Toxicity of root canal sealers on rat bone cells in primary culture.

The cytotoxic effects on cultured rat bone cells of newly-developed root canal sealers and commercially available sealers were compared. Various root canal sealers were applied to cultured bone cells obtained from rat calvaria by the enzyme digestion method. Measurement of [3H]-thymidine incorporation, alkaline phosphatase activity, and calcium release were performed after 24 and 48 h. No significant difference was found in cellular DNA synthesis and alkaline phosphatase activity between cells exposed to New B-1, New B-5 and controls after exposure for 24 and 48 h. Cells in contact with Tubliseal, Diaket and AH-26 demonstrated a significant difference from controls in DNA synthesis and alkaline phosphatase activity. Calcium release at 24 h was significantly different in the cells treated with New B-1 and New B-5 than in controls. No appreciable difference was found, however, between New B-6, Sealapex and controls. At 48 h, cells treated with New B-1, New B-5 and New B-6 showed differed significantly difference from controls, but the cells exposed to Sealapex did not. The newly-developed root canal sealers had lower toxicity in vitro than five types of commercially available root canal sealers.

Alkaline Phosphatase↗
PubMed1988

Studies on cephalosporin antibiotics. I. Synthesis, antibacterial activity and oral absorption of new 3-(O-substituted)-7 beta-[D-alpha-amino-alpha-(4-hydroxyphenyl)acetamido]cephalosporins.

The synthesis, antibacterial activity and oral absorption of new 7 beta-[D-alpha-amino-alpha-(4-hydroxyphenyl)acetamido]cephalosporins (1) with various O-substituents at the C-3 position of a cephalosporin nucleus are described. Of these, the cephalosporins (1b-1e) having an alkoxycarbonylmethoxy group at the C-3 position showed good oral absorption in rats as well as potent activity against Gram-positive bacteria. The structure-activity relationships of 1 are also presented.

Administration, Oral↗
PubMed1988

Studies on cephalosporin antibiotics. II. Synthesis, antibacterial activity and oral absorption of 3-alkoxycarbonylmethoxy-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)-acetamido]cephalosporins.

The synthesis, antibacterial activity and oral absorption in rats of 3-alkoxycarbonyl-methoxy-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]cephalosporins (1) are described. In this cephalosporin series, 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxy-methoxyimino)acetamid o] cephalosporins (1b, 1i and 1j) with a lower alkoxycarbonylmethoxy group at the C-3 position of a cephem nucleus exhibited not only potent activity against Gram-negative bacteria but also good oral absorption in rats. Structure-activity relationships of 1 are also presented.

Administration, Oral↗
PubMed1988

[A case of bronchial carcinoma showing regression upon intratumoral administration of OK-432].

A 38-year-old female suffering from chronic respiratory symptoms due to lung cancer occupying the left main bronchus was treated by frequent intratumoral injections of OK-432. The immune-modifying therapy was performed as follows; 0.2 KE of OK-432 was injected intracutaneously once a week, then the dose was gradually increased to 3.0 KE once a week. Following immunization, intratumoral injection was done under endoscopy at a dose of 3.0 KE every two weeks. Three months later, the tumor showed remarkable regression, and clinical symptoms were diminished. In conclusion, intratumoral injection of OK-432 was considered to be very beneficial in lung cancer.

Adult↗