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Volume 95 (1990)
- Issue 6 Pages 279-
- Issue 5 Pages 229-
- Issue 4 Pages 139-
- Issue 3 Pages 83-
- Issue 2 Pages 47-
- Issue 1 Pages 7-
Volume 95, Issue 4
Displaying 1-9 of 9 articles from this issue
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Reizo INOKI1990 Volume 95 Issue 4 Pages 139-147
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSThis review describes: recent findings about the peripheral site of action and mechanism of the algesic action of narcotic and nonnarcotic analgesics. Special attention was given to the stimulatory or inhibitory actions of opiates and opioid peptides on the polymodal receptor of the sensory afferent fibers. Bradykinin, a pain producing substance, augmented the production of opioid peptides, for example, methionine and leucine enkephalins in in vitro and in vivo experiments. It was demonstrated that a pharmacological feed back reaction, the antinociceptive response, took place in the peripheral site of the primary afferent fibers.View full abstractDownload PDF (8536K) -
Kumeji TAKEUCHI, Koji ITO, Satuki NAMIKAWA1990 Volume 95 Issue 4 Pages 149-157
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSEffects of Glyteer (GL, 5%) on Type I-Type IV allergic reactions were investigated by its topical application to rats and mice, and the effects were compared with those of betamethasone 17-valerate (BV, 0.12%), indomethacin (ID, 1%), and bufexamac (BM, 5%), which were all prepared with the same ointment base. Type I: GL showed inhibitory effects on the 48 hr homologous passive cutaneous anaphylaxis (PCA) in rats. The inhibitory activity of GL on the PCA had the same potency as that of BV (0.12%). GL also inhibited the degranulation of mast cells induced by PCA. Type II: GL did not exert an inhibitory effect on the reversed cutaneous anaphylaxis (RCA) in rats, but BM, ID and BV had an inhibitory activity on the RCA. Type III: BV markedly inhibited the direct passive Arthus reaction in rats. On the other hand, GL, BM and ID had not an inhibitory activity on it. Type IV: GL (0.2, 1 and 5%) showed a concentration-dependent inhibition on the delayed-type hypersensitivity response induced by oxazolone in mice, and the activity was stronger than those of ID and BM. From these results, it is suggested that GL applied externally possesses a potent effect as an anti-allergic drug on Type I and Type IV allergic reactions.View full abstractDownload PDF (7989K) -
Terumasa HASHIMOTO, Kenichi EDANAMI, Akira NAITO, Kazuko SANO, Hiroko ...1990 Volume 95 Issue 4 Pages 159-166
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSWP-833 is an orally active new antiallergic drug. The effects of WP-833 metabolites on experimental allergic reactions were investigated in various animal models. MTCC [3'-(1H-tetrazol-5-yl) oxanilic acid], the main metabolite of WP-833, dose-dependently inhibited 48-hr homologous passive cutaneous anaphylaxis (PCA) in rats and 8-day PCA in guinea pigs after intravenous administration. The inhibitory effect of MTCC on PCA was nearly equal to that of WP-833. MTCC also inhibited 48 hr PCA in rats after the peroral administration, although its inhibitory effect was about 6 times weaker than that of WP-833. MTCC also showed a dose-dependent inhibition on the release of histamine or slow reacting substance of anaphylaxis (SRS-A) from passively sensitized rat peritoneal mast cells and guinea pig lung fragments in vitro with a similar potency to WP-833. MTA [3-(1H-tetrazol-5-yl) aniline] and MTAA [3'-(1H-tetrazol-5-yl)acetanilide], other metabolites of WP-833, inhibited PCA and anaphylactic histamine release from rat peritoneal mast cells at considerably higher doses than WP-833, and they showed no effects on the release of histamine and SRS-A from guinea pig lung fragments. Moreover, only small amounts of MTA and MTAA were detected in the blood after the oral administration of WP-833. From these results, it was suggested that MTCC may be the main active metabolite of WP-833.View full abstractDownload PDF (6093K) -
Tomoaki TAMURA, Toshietsu TANIGUCHI, Masaru AOKI, Isami WAKI1990 Volume 95 Issue 4 Pages 167-175
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSCerebral protective effect of eptazocine, a μ-antagonist-κ-agonist, was investigated using mice subjected to hypoxia-anoxia. Eptazocine (1 to 10 mg/kg) prolonged the survival time of mice subjected to KCN (3 mg/kg, i.v.) injection in a dose-dependent manner, and this effect was completely inhibited by naloxone (5 mg/kg). EKC, U50, 488H, opioid X-agonists, also had such an effect, but were weaker than eptazocine. In mice exposed to hypobaric hypoxia (190 mmHg), eptazocine (3, 10 mg/kg) and EKC (10 mg/kg) prolonged the survival time, but morphine (5 mg/kg) and pentazocine (10 mg/kg) shortened the time. The eptazocine effect was attenuated by either naloxone (5 mg/kg) or atropine (0.5 mg/kg), different from what was seen in the case of physostigmine and diazepam, and the combination of eptazocine (1 mg/kg) and physostigmine (0.075 mg/kg) had a potentiating effect. MR-2266, a selective κ-receptor antagonist, inhibited the eptazocine effect more potently than naloxone. These results suggest that eptazocine elicited its cerebral protective effect via its binding with opioid κ-receptors and probably an activation of the central cholinergic system.View full abstractDownload PDF (6314K) -
Hideaki KIDO, Yasumi UCHIDA, Fumitaka NAKAMURA, Tsuneaki SUGIMOTO1990 Volume 95 Issue 4 Pages 177-184
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSAE0047, a novel calcium antagonist, has mild and long-acting hypotensive effects. This drug also has more selective dilating action on cerebral arteries than on other systemic ones. We studied the cerebral vasodilatative effects of AE0047 by means of vertebral angiography in anesthetized dogs. Vertebral blood flow (VBF) was significantly increased by 91, 139 and 132% in 10, 30 and 60 min after intravenous administration of AE0047 at 30 μg/kg, respectively. No difference in vasodilating action was observed among basilar, posterior communicating, middle cerebral and internal carotid arteries. In basilar artery, the dilatative rate was about 30% between 10 and 60 min after injection of AE0047. Following intravertebral administration of endothelin at 100 pmol/kg, small vessels of the cerebral artery were constricted, and VBF was gradually decreased. AE0047 eliminated the vasoconstriction and increased VBF. Moreover, the vasoconstrictive effect of endothelin was prevented by pre-treatment of AE0047. These results indicate that AE0047 has potent vasodilating and spasmolytic actions on cerebral arteries.View full abstractDownload PDF (7490K) -
Masayuki UCHIDA, Naoyuki NISHIMURA, Noriyuki MISAKI, Yasuko IKARASHI, ...1990 Volume 95 Issue 4 Pages 185-190
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSThe effects of anti-ulcer drugs and PGE2 on the proliferation of rat gastric cultured cells were investigated. To study the cell proliferation, the rate of incorporation of 3H-thymidine into the cultured cells was measured. ULTROSER® G, corresponding to fetal bovine serum, was found to dose-dependently increase the incorporation of 3H-thymidine into the cultured cells at a dose range of 1 ?? 4%. The incorporation of 3H-thymidine was highest at 36 hr after the inoculation of cells. Therefore, the effect of the drugs on the proliferation was performed under the condition of 2% ULTROSER®G and evaluated at 36 hr. Aldioxa, cetraxate HCl, cimetidine (10-7 ?? 10-5M) and PGE2 (10-8 ?? 10-6M) had no effect on the cell proliferation, while indomethacin (0.35 ?? 1.41 × 10-3 M) inhibited the proliferation in a dose-dependent manner. Aldioxa, cetraxate HCl (10-5M) and PGE2 (10-6, 10-8M) antagonized the inhibitory effect by indomethacin at a concentration of 0.5 × 10-3M, but cimetidine (10-7 ?? 10-5M) did not. From the above results, it was concluded that this method was useful for investigating the effect of drugs on the proliferation of gastric cultured cells.View full abstractDownload PDF (5469K) -
β-Blocking effect, intrinsic sympathomimetic activity, vasodilating and hypotensive effectsAkira MIURA, Yutaka KIMURA, Kichiro INOUE, Takushi MATSUZAKI, Seishi O ...1990 Volume 95 Issue 4 Pages 191-200
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSThe β-blocking effect, intrinsic sympathomimetic activity (ISA), and vasodilating and hypotensive effects of celiprolol were tested. 1. Celiprolol competitively antagonized the isoproterenol-induced positive chronotropic and inotropic effects in guinea pig right atrial and papillary muscles and isoproterenol-induced guinea pig tracheal relaxation with pA2. values of 8.03, 7.98 and 6.43, respectively. 2. In dogs, isoproterenol-induced increases in cardiac contractility and heart rate were markedly inhibited by celiprolol (83.1 and 84.8%, respectively), . while isoproterenol-induced hypotension was suppressed only by 16.8%. 3. Celiprolol increased the beating rate of the right atrium and relaxed the trachea isolated from normal and reserpinized guinea pigs. Celiprolol also potentiated the contractility of the left atrium isolated from reserpinized animals. These effects of celiprolol were antagonized by propranolol. 4. Celiprolol concentration-dependently relaxed rat femoral arteries contracted by methoxamine. The concentration-relaxation curve was shifted to the right by pretreatment with propranolol. 5. Orally administered celiprolol produced long lasting hypotension in conscious SHR without any heart rate change. 6. These results indicate that celiprolol is a highly cardioselective β-blocker with a significant ISA, which contributes to its vasodilatory and hypotensive effects.View full abstractDownload PDF (8133K) -
α2-Adrenoceptor blocking effects of a cardioselective β-blocker, celiprololAkira MIURA, Yojiro UKAI, Takushi MATSUZAKI, Tsuyoshi ISHIMA, Seiji HA ...1990 Volume 95 Issue 4 Pages 201-208
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSα-Adrenoceptor blocking effects of the cardioselective β-blocker celiprolol were tested. 1. Celiprolol antagonized the contractions induced by UK-14304, but not those by phenylephrine, in isolated rat tail arteries with a pA2 value of 4.95. 2. In the isolated rat vas deferens, twitch contractions elicited by the transmural electrical stimulation (TS) were almost blocked by TTX (10-7 M). Clonidine inhibited the TTX-sensitive contraction in a concentration-dependent manner. Celiprolol produced little effect on the inhibitory effects of clonidine. The concentration-inhibition curve of clonidine was shifted to the right by yohimbine (10-8M), but not by prazosin (10-8M). 3. Although celiprolol slightly increased the 3H-efflux to TS from the (3H)-norepinephrine-loaded rat vas deferens, the increment was not significant. Yohimbine (10-7 M) significantly increased the 3H-efflux. TTX (10-7M) and bretylium (3 × 10-5 M) blocked the 3H-efflux. 4. In the spinal rat treated with propranolol (3 mg/kg, i.v.) and prazosin (0.1 mg/kg, i.v.), celiprolol (30 and 100 mg/kg, i.v.) and yohimbine (0.1 ?? 1 mg/kg, i.v.) inhibited the pressor response to clonidine. 5. These results indicate that celiprolol may have a weak α2-blocking effect which was more effective on postsynaptic α2-receptors than presynaptic ones.View full abstractDownload PDF (5866K) -
Effects of celiprolol on the cardiovascular system and renal function, and its antiarrhythmic effectsSeishi OCHI, Yutaka KIMURA, Takushi MATSUZAKI, Seiji HAYASHI, Asahiko ...1990 Volume 95 Issue 4 Pages 209-227
Published: 1990
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSEffects of celiprolol on the cardiovascular system and renal function, and its antiarrhythmic effects were studied. 1. In anesthetized dogs, celiprolol (0.01 ?? 3 mg/kg, i.v.) dose-dependently depressed the maximum rate of rise of left ventricular pressure, cardiac output and cardiac work less severely than propranolol and atenolol. 2. Celiprolol (0.01 mg/kg, i.v.) decreased the myocardial oxygen consumption in anesthetized dogs as potently as propranolol. 3. Celiprolol (0.03 ?? 3 mg/kg, i.v.) tended to increase femoral blood flow. Celiprolol (1 mg/kg, i.v.) increased common carotid blood flow. 4. Celiprolol decreased urine volume and urinary excretion of Na+ and Cl- at doses of 1 and 10 mg/kg and increased the sodium reabsorption rate at a dose of 10 mg/kg in anesthetized dogs, whereas it produced no change in plasma renin activity. 5. Celiprolol inhibited both halothane-adrenaline arrhythmia in dogs and ouabain-induced arrhythmia in rabbits. Its antiarrhythmic effects were 1/10 ?? 1/3 as potent as those of propranolol. 6. Celiprolol suppressed the maximum rate of rise of action potential at a concentration of 3×10-4 M, which was 30 times as high as that of propranolol. Celiprolol (3×10-5 ?? 3×10-4 M) dose-dependently shortened the effective refractory period (ERP), but it produced no change in the ratio of ERP to action potential duration. 7. These results suggest that celiprolol may be a useful drug for the treatment of ischemic heart disease and some types of arrhythmia, and that it has only a little influence on renal function.View full abstractDownload PDF (14464K)
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