巻号一覧
40 巻 (1986)
- 4 号 p. 481-
- 3 号 p. 357-
- 2 号 p. 199-
- 1 号 p. 1-
40 巻, 3 号
選択された号の論文の16件中1～16を表示しています
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Charles WAMBEBE1986 年 40 巻 3 号 p. 357-365
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーThe influence of apomorphine, levodopa and haloperidol was studied on nitrazepam sleep using young chicks and rats. In addition, the influence of dopamine and ADTN was studied in young chicks. Nitrazepam dose-dependently (0.4-51.2 mg/kg, i.p.) induced behavioural sleep in chicks. However, higher doses of nitrazepam (12.8-51.2 mg/kg, i.p.) were required to induce behavioural sleep in rats. Dopamine (12.5-100 mg/kg, i.p.) and ADTN (2.5-80 mg/kg, i.p.) delayed the onset but prolonged nitrazepam sleep in chicks: these effects were statistically significant. Levodopa (12.5-100 mg/kg, s.c.) and apomorphine (0.2-0.8 mg/kg, s.c.) profoundly delayed the onset and shortened the duration of nitrazepam sleep in both chicks and rats. Noradrenaline (20-80 mg/kg, i.p.) shortened the onset and prolonged nitrazepam sleep in chicks. Pimozide (1-8 mg/kg, i.p.) potentiated nitrazepam sleep and antagonized the effects of dopamine, levodopa and ADTN on nitrazepam sleep in chicks. Similarly, haloperidol (0.5-1.0 mg/kg, i.p.) potentiated nitrazepam sleep and antagonized the effects of levodopa and apomorphine on nitrazepam sleep in rats. The EEG synchronization and decreased EMG induced by nitrazepam (1.6 mg/kg, i.p., and 12.8 mg/kg, i.p., for chicks and rats, respectively) were antagonized by levodopa (12.5 mg/kg, s.c.). The behavioural and electroencephalographical results suggest that enhancement of dopaminergic neurotransmission may be involved in the mechanisms of wakefulness in both chicks and rats.抄録全体を表示PDF形式でダウンロード (659K) -
Katsuhiko NAKATA, Terumichi IWATANI, Masato HORIUCHI, Hirokazu KITO, H ...1986 年 40 巻 3 号 p. 367-372
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーA marked species difference was observed both in vitro and in vivo in the activity of SA446, an orally active inhibitor of angiotensin converting enzyme (ACE), as compared with that of captopril in five different animal species. The activity of SA446 in vitro in inhibiting plasma ACE correlated with the activity in vivo as determined by inhibition of the pressor response to angiotensin I (Al). SA446 was more potent as an inhibitor of Al response in dogs, cats and rabbits than in guinea pigs and rats. Furthermore, ACE activity in whole blood in vivo was inhibited by SA446, and the activity of SA446 was also more potent in dogs than in rats. The concentration of SA446 in the ultrafiltrate of blood (free form) was significantly higher in dogs than in rats, while no difference was observed in level of SA446 in the whole blood (free and protein-bound form) between these two species after intravenous injection. The binding rate of SA446 to plasma protein of rats in vitro was more than twice as high as that of dogs. These results suggest that the difference in the protein binding rate of SA446 is reflected in ultrafiltrate level and is one of the important components in defining the species difference in SA446 action.抄録全体を表示PDF形式でダウンロード (410K) -
Katsuhiko NOGUCHI, Takayuki KATO, Ryuji SUNAGAWA, Yoshimasa MIYAMOTO, ...1986 年 40 巻 3 号 p. 373-380
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーEffects of a new angiotensin-converting enzyme inhibitor, N-[3-(N-cyclohexanecarbonyl-D-alanylthio)-2-methylpropanoyl]-L-proline calcium (MC-838), on the systemic and coronary circulation were evaluated in anesthetized dogs, and the effects were compared with those of captopril. Administration of MC-838 (0.1, 0.3, 1.0 and 3.0 mg/kg, i.v.) produced a gradual and dose-dependent decline in aortic pressure associated with no marked changes in coronary blood flow, heart rate and LVdP/dt. Captopril (0.01, 0.03, 0.1 and 0.3 mg/kg, i.v.) also caused a dose-related decrease in aortic pressure, but the significant hypotension appeared more rapidly than that of MC-838. Both MC-838 and captopril inhibited selectively the pressor response to angiotensin I in a dose-related manner. The doses of MC-838 and captopril to lower mean aortic pressure by 10 mmHg from the pre-drug value were 2.8 mg/kg and 0.03 mg/kg, respectively; those of these drugs to cause 50% inhibition of angiotensin I-pressor response were 1.0 mg/kg and 0.04 mg/kg, respectively. When administration of MC-838 (3.0 mg/kg) was repeated three times at a 30 min-interval, the second and third injections caused no additional hypotension, while each of the repeated injections of captopril (0.3 mg/kg) produced significant hypotension. These results indicate that MC-838 inhibits angiotensin I-conversion and decreases systemic blood pressure more slowly and persistently than captopril in anesthetized dogs.抄録全体を表示PDF形式でダウンロード (553K) -
Keisuke TAKEDA, Kazuki MATSUI, Mikio NAKAZAWA, Hajime NAKAHARA, Hirohi ...1986 年 40 巻 3 号 p. 381-388
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーAnalysis of the relative magnitude of the positive inotropic and chronotropic effects and the coronary vasodilating effects of amrinone conducted in the canine heart-lung preparation with a support dog in comparison with those of dobutamine demonstrated that amrinone was a preferential coronary vasodilator rather than a selective positive inotropic agent. An in vitro experiment in the canine papillary muscle suggested the initiation of the slow response action potential as a mechanism of the positive inotropic effect of amrinone.抄録全体を表示PDF形式でダウンロード (476K) -
Takashi MATSUBARA, Noriko YAMADA, Toshio MITOMI, Seishichi YOKOYAMA, Y ...1986 年 40 巻 3 号 p. 389-398
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーHuman liver samples from 17 embryos, 5 fetuses, 5 infants and 4 adults were used to investigate human liver cytochrome P-450-dependent 7-alkoxycoumarin O-dealkylase activities, and their drug-metabolizing activities were compared to those of rat livers. The O-dealkylase activities in human embryos and fetuses were very low, although detectable, similar to those in fetal rats. Both male and female rats showed a postnatal increase of hepatic O-dealkylase activities with a maximum at about 30-40 days after birth and then a decline in the activities which was marked in female rats. Adult female rats showed a marked decrease in the hepatic enzyme activity observed in the O-depropylation reaction rather than the O-demethylation and O-deethylation reactions. During the developmental period of human infants, the O-demethylase activity, but not O-depropylase activity, increased gradually. Enzymes in adult human livers metabolize the O-methyl derivative of 7-hydroxycoumarin in preference to the O-ethyl and O-propyl derivatives. The metabolic activities of human adult enzymes for 7-alkoxycoumarin resembled those in adult female rats and were quite different from those in male rats. The study demonstrated that caution must be exercised in extrapolating pharmacological results from animal to man in the field of drug metabolism.抄録全体を表示PDF形式でダウンロード (757K) -
Jun NAGURA, Bunsei MURAYAMA, Nobuo HARADA, Kunio SUZUKI, Tetsuji MIYAN ...1986 年 40 巻 3 号 p. 399-409
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーThe cardiovascular effect of NPK-1886 (NPK), a novel photostable dihydropyridine compound, was studied by comparing it with that of nifedipine (Nif). In normal Wistar rats (NWR), systolic blood pressure was only slightly depressed by NPK or Nif, while in three types of hypertensive rats (i.e., spontaneously hypertensive rats (SHR), renal hypertensive rats (RHR) and DOCA-saline-induced hypertensive rats (DOC-Na-R)), the hypotensive potency of NPK was more than or equal to that of Nif. The effectiveness of NPK on the normal and hypertensive models was in the following order: DOC-Na-R, RHR, SHR, NWR. Coronary perfusion flow in Langendorff's heart was increased almost the same extent by NPK and Nif. On isolated rabbit aortic strips, the antagonistic potencies of NPK, like those of Nif, were greater for calcium than for norepinephrine, serotonin and angiotensin II. The negative ino and chronotropic potency of NPK in isolated guinea-pig right atria was less than that of Nif. The slow membrane action potentials of guinea-pig papillary muscle were suppressed by NPK, but less than by Nif, with manifestations of a reduction of Vmax and AP-duration. These results indicate that NPK has a potent hypotensive effect on hypertensive models and a weaker cardiac inhibition. The general toxicity of NPK was lower than that of Nif.抄録全体を表示PDF形式でダウンロード (740K) -
Yoshimi NIWANO, Minoru KATOH, Matazaemon UCHIDA, Tatsuyoshi SUGIMOTO1986 年 40 巻 3 号 p. 411-415
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーThe effect of malotilate (diisopropyl 1, 3-dithiol-2-ylidenemalonate) on liver regeneration was studied by using partially hepatectomized rats. Malotilate administration (100 mg/kg/day, p.o.) facilitated the weight gain of the liver after partial hepatectomy. Protein, RNA and DNA contents of the regenerating liver correlated well with the weight gain. The weight gain, RNA and DNA contents, and mitotic index were significantly suppressed in the alloxan-diabetic rats 24 hr after partial hepatectomy. However, malotilate administration significantly improved the delayed recovery of RNA content. Other parameters were not significantly improved by malotilate, but tended to increase to a level comparable to those of partially hepatectomized control rats. These results show that malotilate accelerates cell proliferation, resulting in facilitated liver regeneration in rats (as well as in alloxan-diabetic rats).抄録全体を表示PDF形式でダウンロード (376K) -
Katsuaki MATSUBARA, Akira MATSUSHITA1986 年 40 巻 3 号 p. 417-422
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーCaerulein has been shown to possess a long-lasting antagonistic effect on amphetamine hyperactivity in rats when given in combination with haloperidol. We found that this effect of caerulein involved β-endorphin. Naloxone pretreatment and hypophysectomy abolished the caerulein effect, while intracerebroventricular or intra-nucleus accumbens injection of β-endorphin together with haloperidol administration produced an effect similar to that of caerulein. The results suggest that the long-term antagonism of the amphetamine effect of caerulein is mediated by the endogenous opioid β-endorphin.抄録全体を表示PDF形式でダウンロード (464K) -
Shigeo ITO, Toshio OHTA, Yoshikazu NAKAZATO, Akira OHGA, Noboru YANAIH ...1986 年 40 巻 3 号 p. 423-434
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーExperiments were carried out to investigate whether avian pancreatic peptide (APP) antagonized relaxations of vascular and gastrointestinal smooth muscles induced by vasoactive intestinal peptide (VIP) and non-adrenergic, non-cholinergic inhibitory nerve stimulation using the cat submandibular gland, cat colon and dog stomach in vivo and several isolated smooth muscles in vitro. APP caused a dose-dependent inhibition of an atropine-resistant vasodilatation induced by chorda-lingual and pelvic nerve stimulation and by VIP. APP did not reduce VIP output induced by pelvic nerve stimulation. APP shifted the dose-response curve for VIP and the frequency-response curve for pelvic nerve stimulation to the right. The vasodilatation induced by isoproterenol or bradykinin was inhibited by somewhat higher doses of APP. APP failed to inhibit the vago-vagal reflex relaxation of the dog stomach. In guinea pig and rat fundic strips and in isolated chick rectum, APP did not exert any significant effects on relaxation caused by VIP or transmural stimulation in the presence of atropine and guanethidine. The result indicates that APP inhibits VIP-mediated relaxation of the vascular smooth muscle, but not that of the gastrointestinal smooth muscle. The inhibitory effect of APP on VIP-mediated vasodilatation is suggested to be due to the physiological competition.抄録全体を表示PDF形式でダウンロード (943K) -
Hitoshi ITO1986 年 40 巻 3 号 p. 435-443
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーCorrelation between antitumor activity and effects on some biological properties, such as phagocytic activity of the reticuloendothelial system, the third component of complement (C3) activation, hepatic drug-metabolizing activities and pentobarbital-induced narcosis, of antitumor agents from various natural sources such as B B (Broncasma Berna), GU-P (Grifora umbellata polysaccharide), OK-432, PS-K (Polysaccharide Kureha), and RA-P (Rumex acetosa polysaccharide) were studied with female ICR mice implanted with Sarcoma 180 solid tumor. All of these agents depressed aniline hydroxylase and aminopyrine demethylase activities, prolonged the duration of pentobarbital-induced narcosis, and significantly enhanced the phagocytic activity and C3 activity. Especially, RA-P which has the strongest antitumor activity was the most effective in changing these activities. The biological activities of GU-P at a dose of 10 mg/kg reached the same level as that found with PS-K at a dose of 100 mg/kg. A possible mechanism of inhibition of Sarcoma 180 solid tumor growth by the treatment with the antitumor agents could be interpreted as due to the C3 activation, the stimulation of phagocytic activity and depression of the hepatic microsomal drug-metabolizing system in tumor-bearing mice.抄録全体を表示PDF形式でダウンロード (882K) -
Kyoji MORITA, Hitoshi HOUCHI, Atsushi NAKANISHI, Kazuo MINAKUCHI, Moto ...1986 年 40 巻 3 号 p. 445-453
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーThe direct effect of hydralazine on catecholamine-synthesizing enzymes was investigated. Hydralazine caused a concentration-dependent inhibition of tyrosine hydroxylase (TH) prepared from bovine adrenal medulla, and a more pronounced effect was obtained by incubating the enzyme with the drug prior to the enzyme assay. Kinetic studies showed that hydralazine increased the apparent Km value of the enzyme for tyrosine and cofactor, 6, 7-dimethyl-5, 6, 7, 8-tetrahydropterin (DMPH4), without any change in the Vmax. The inhibitory effect of the drug was irreversible, and an excess amount of FeSO4 failed to restore the enzyme activity inhibited by this drug. Furthermore, hydralazine also inhibited the dopamine β-hydroxylase (DBH) in chromaffin granule membranes. Hydralazine increased the apparent Km value of DBH for ascorbic acid without any change in the Vmax, and it decreased the Vmax of the enzyme for tyramine with no change in the apparent Km value. The observations described here suggest the possibility that hydralazine presumably causes the inhibition of catecholamine-synthesizing enzymes as a result of allosteric alterations in the molecular structures of these enzymes. It thus seems unlikely that the inhibitory action of hydralazine on these enzymes may totally be based on its metal-chelating activity.抄録全体を表示PDF形式でダウンロード (692K) -
Nagao SUZUKI, Osamu INAGAKI, Yutaka KASUYA1986 年 40 巻 3 号 p. 455-462
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーInhibitory effects of propranolol on the contractions to various treatments were investigated in the epididymal half of the rat vas deferens. Reportedly, 10-5 ?? 3×10-4 M propranolol inhibited 150 mM K-induced contractions dose-dependently; 3×10-4 M propranolol abolished the contractions. The present results showed that propranolol at concentrations up to 10-4 M did not inhibit the maximal contractions to 10-3 M norepinephrine (NE) or 10-2 M methacholine (MCh). Propranolol at 3×10-4 M slightly inhibited contractions to NE and MCh by 11% and 12%, respectively. In contrast, propranolol inhibited twitch components of the contractions induced by nerve stimulations at similar doses to those reported for high K contractions. Propranolol also inhibited contractions to Ca in high K-containing solution and shifted the dose-response curve to the right. Propranolol did not affect the depolarizations by high K measured by microelectrodes. Propranolol at concentrations of 10-5 ?? 3×10-5 M diminished the magnitude of spikes dose-dependently. Spikes were rarely observed in the presence of 10-4 M propranolol in spite of generation of e.j.p.s with amplitudes that would be sufficient to induce spikes in the absence of propranolol. These results suggest that propranolol inhibits contractions by decreasing Ca-influx through the potential-operated Ca-channels in the smooth muscle cells of rat vas deferens.抄録全体を表示PDF形式でダウンロード (623K) -
Masako MORIKAWA, Takashi KOJIMA, Michiko INOUE, Minoru TSUBOI1986 年 40 巻 3 号 p. 463-468
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーThe intracellular Ca2+ mobilization in thrombin-stimulated platelets was greater in male rats than in female rats. Thromboxane (TX) B2 production in male platelets was greater than that in female platelets. Aspirin suppressed Ca2+ mobilization in rat platelets, but the inhibitory effect of aspirin was more efficient in males than that in females. Aspirin inhibited TXB2 production, and this inhibitory effect of aspirin was stronger in male platelets than in female platelets. Castration decreased Ca2+ mobilization and TXB2 production and weakened the effect of aspirin on them. It is suggested that the sex difference in the antiplatelet effect of aspirin results from the difference in the inhibition of Ca2+ mobilization via the inhibition of TXA2 production in thrombin-stimulated rat platelets.抄録全体を表示PDF形式でダウンロード (431K) -
Seiji ICHIDA1986 年 40 巻 3 号 p. 469-471
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーThe contractile responses of isolated uterine smooth muscle from estradiol-treated ovariectomized rats to acetylcholine and high KCl in Ca-depleted modified Locke-Ringer (without CaCl2 and with 0.1 mM EGTA) solution on addition of CaCl2 (final concentration, 5 mM) are used as an indicator of Ca influx through the Ca channel. L-Methionine significantly enhanced these responses in the absence and presence of 3-deazaadenosine plus homocysteine thiolactone, blockers of methylation. These findings suggest that methylations of some components in isolated uterine smooth muscle seem to be important in stimulation-contraction coupling in the muscle.抄録全体を表示PDF形式でダウンロード (241K) -
Katsuo KAMATA, Akira SUGIMOTO, Tsutomu KAMEYAMA1986 年 40 巻 3 号 p. 472-477
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーEffect of microinjection of apomorphine into the substantia nigra zona reticulata (SNP, ) on the dopamine (DA) release in the ipsilateral striatum was examined in the present study. To measure the DA release, we determined DA and/or DOPAC levels in the striatum by using in vivo voltammetry. The microinjection of apomorphine (10 μg/2 μl) into the SNR produced a rapid and prolonged increase in the DA and/or DOPAC peak in the ipsilateral striatum. These results suggest that release of DA from dendrites of DA cells normally plays a physiological role in the SNR neurons.抄録全体を表示PDF形式でダウンロード (449K) -
Midori MASUDA, Kazuyoshi HORISAKA, Takemi KOEDA1986 年 40 巻 3 号 p. 478-480
発行日: 1986年
公開日: 2006/09/15
ジャーナル フリーIn dietary hyperlipidemic rats, an increase in serum lipid level may cause an increase in membrane lipid level of the neutrophils, and phagocytosis and bactericidal capacity may be thereby lowered. Treatment with taurine (470 mg/kg/day, p.o.) strengthened the bactericidal capacity of neutrophils which was decreased by cholesterol diet feeding, as the capacity was stronger on the 40th day than that in animals fed laboratory chow. The results suggest that taurine may play an important role in the mechanism of host defense through the neutrophil function.抄録全体を表示PDF形式でダウンロード (224K)
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