The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
40 巻, 1 号
選択された号の論文の25件中1~25を表示しています
  • Seiichi KOMORI, Konomi MATSUO, Yoshihiro KANAMARU, Hidenori OHASHI
    1986 年 40 巻 1 号 p. 1-11
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Active substances extracted from the Remak nerve of the chicken were subjected to chromatographic and electrophoretic separation followed by bioassay of contracting activities on the longitudinal muscle of the guinea-pig ileum (LMGPI) and on the isolated whole chick rectum (WCR). Gel filtration profiles on a Sephadex G-50 column showed two peaks of LMGPI-contracting activity and of WCR-contracting activity. No difference was seen in the enzymatic destruction between the LMGPI-contracting activity and substance P. Their similarities were also indicated by the parallelism of their elution curves in the gel chromatography on Sephadex G-25, their equal stability in acid solutions, and comparable antagonism and inhibition of the contractile effects on LMGPI by substance P antagonists and after desensitization of substance P receptors. Ion exchange chromatography revealed the existence of two main substances responsible for the LMGPI-contracting activity. One of them eluted at the same position as that for substance P, but differed in immunoreactivity and electrophoretic mobility from substance P. The WCR-contracting activity differed from the LMGPI-contracting activity in that it was pepsin-resistant and carboxypeptidase A-susceptible, and it eluted at a different position during ion exchange chromatography. It seems likely that the LMGPI-contracting activity in the extracts is attributed to a substance P-family of peptides, but the WCR-contracting activity is due to another substance of a peptide nature.
  • Hideyuki TAKENAGA, Tetsuo MAGARIBUCHI, Hajime TAMAKI
    1986 年 40 巻 1 号 p. 13-20
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effects of trimebutine maleate (TM-906) on the spontaneous contraction of isolated duodenum and ileum were studied in both guinea pigs and rabbits. In the duodenum and ileum of both guinea pigs and rabbits, TM-906 (10-6 g/ml, 10-5 g/ml) produced a potentiation of the spontaneous contraction in preparations with low contractile activity (low tone or small contraction), while it caused an inhibition of the spontaneous contraction in preparations with high contractile activity (high tone or large contraction). The potentiation of spontaneous contraction by TM-906 was more pronounced in the ileum than in the duodenum of both guinea pigs and rabbits. When the spontaneous contraction of duodenum and ileum was decreased by atropine, the potentiation of spontaneous contraction by TM-906 was further augmented and was more pronounced in the ileum than in the duodenum. When the spontaneous contraction was remarkably potentiated by physostigmine or acetylcholine, TM-906 markedly inhibited the potentiated spontaneous contraction, and the potentiation by TM-906 seen in preparations with low contractile activity disappeared. From these results, it is concluded that TM-906 produces, depending on the contractile activity of the preparations, a potentiation or an inhibition of the spontaneous contraction of duodenum and ileum in both guinea pigs and rabbits and that the potentiation by TM-906 is more pronounced in the ileum than in the duodenum. It is suggested that the endogeneous acetylcholine partly modifies the effects of TM-906, but that it does not relate to the more pronounced potentiation by TM-906 in the ileum than in the duodenum.
  • Takeshi SHIBUYA, Yasuo WATANABE, Harlan F. HILL, B. SALAFSKY
    1986 年 40 巻 1 号 p. 21-29
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The post treatment effects of early prenatal, late prenatal, early postnatal or combined prenatal and neonatal treatment with diazepam on the development of pain sensitivity, acoustic startle responsiveness, and benzodiazepine receptors in the cerebral cortex were investigated in rats between 14 and 90 days of age. Tail-flick latency was significantly decreased by combined prenatal and neonatal and by early prenatal diazepam treatment, but not by diazepam during the last half of gestation or during the neonatal period alone. Acoustic startle response was decreased by either late prenatal or neonatal diazepam treatment, but not by early prenatal treatment alone. Density of benzodiazepine receptors in the cortex was increased from postnatal day 1 to 21 by either early or late prenatal diazepam treatment. Neonatal diazepam treatment suppressed cortical benzodiazepine receptor or development until postnatal day 21; thereafter, receptor density increased to significantly higher values than in controls at 90 days of age. The results demonstrate that diazepam can alter development of pain sensitivity by actions during early gestation, startle responsiveness by actions late in pregnancy, and cortical benzodiazepine receptors by actions throughout gestation and the early postnatal period.
  • Buichi FUJITANI, Masako WATANABE, Junji KUWASHIMA, Toshimichi TSUBOI, ...
    1986 年 40 巻 1 号 p. 31-35
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The antithrombotic effect of a prostaglandin E1 derivative, OP-1206 (17S-20-dimethyl-trans-Δ2-PGE1)·α-cyclodextrin clathrate (OP-1206·α-CD), was compared with that of acetylsalicylic acid (ASA) in a electrically induced thrombosis model of guinea-pig mesenteric arteries using intact animals and animals subjected to the superfusion of tranylcypromine (TC, 15 mM) over their mesentery. The drug-effect was assessed by the change of the threshold voltage for the thrombus formation. 1) TC (1.5-15 mM) lowered the threshold voltage, and the effect was comparable to its inhibitory effect on PGI2 formation in vitro, suggesting that PGI2 generated in mesenteric arteries acts to prevent thrombus formation. 2) In intact animals, OP-1206·α-CD at doses of 0.01-0.3 mg/kg, p.o. (as OP-1206), significantly and dose-dependently elevated the threshold voltage. ASA (30-1000 mg/kg, p.o.) significantly elevated the threshold voltage, but the effect reached to its maximum at 100 mg/kg and lessened with further increase of ASA. 3) In TC-treated animals, OP-1206·α-CD elevated the threshold voltage dose-dependently, but the elevation of threshold voltage by ASA reached to its plateau level which was significantly lower than that obtained with OP-1206·α-CD at 0.3 mg/kg, indicating that the antithrombotic effect of ASA is incomplete in this model. 4) Threshold voltages in TC-treated animals given OP-1206·α-CD was significantly lower than those in intact animals at all doses tested, but threshold voltages in TC-treated and intact animals given ASA at 300-1000 mg/kg were not different, suggesting that high doses of ASA inhibits PGI2 formation in vivo. Thus, the antithrombotic effect of ASA was restricted by its inhibitory effect on PGI2 formation and its incomplete inhibition on thrombus formation, while such differences were not observed in OP-1206·α-CD.
  • Kei TSUZURAHARA, Takashi MURATA, Setsuko ISHIKAWA, Tadamasa DATE, Shig ...
    1986 年 40 巻 1 号 p. 37-46
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effects of TA-5707F [6-methyl-N-(1H-tetrazol-5-yl)-2-pyridinecarboxamide] and its sodium salt (TA-5707) on IgE-induced homologous PCA in rats were investigated. 1. Both TA-5707 and TA-5707F were found to be orally effective inhibitors of rat PCA. Maximum activity by oral administration was obtained when they were administered 5 min before the challenge. Their ID50's under these conditions were both approximately 1 mg/kg. Administration 5 min after the challenge was no longer effective. 2. TA-5707 was also effective by intravenous administration, and its I D50, ca. 0.1 mg/kg, was less than that of disodium cromoglycate (DSCG). 3. The PCA-inhibitory activity of TA-5707 was not affected by adrenalectomy and adrenomedullectomy. 4. Daily administration of TA-5707 or TA-5707F for 8 days did not induce drug tolerance. 5. Tachyphylaxis and cross -tachyphylaxis were observed when the PCA-inhibitory activities of TA-5707 and DSCG were tested after intravenous pretreatment with a large dose (ca. 30 times the ID50) of either drug, but not after oral pretreatment with a therapeutic dose of TA-5707 or TA-5707F.
  • Naoki INAGAKI, Akihide KODA, Akira YAGI, Yasushi HARAGUCHI, Hiroichi N ...
    1986 年 40 巻 1 号 p. 47-56
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effect of n-pentyl glycosides and alkyl α-L-sorbopyranosides on IgE antibody formation in rats and mice were investigated. When n-pentyl α-L-sorbopyranoside was given subcutaneously or orally, the IgE antibody formation in rats and mice was suppressed, while no suppression of hemagglutinin formation was observed. The study on timing of administration indicated that n-pentyl α-L-sorbopyranoside significantly suppressed the secondary IgE antibody response when administered before the secondary immunization.
  • Shozo KITO, Masanori SHIMOYAMA, Rumiko ARAKAWA
    1986 年 40 巻 1 号 p. 57-67
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The effects of neurotransmitters or drugs on the release of endogenous dopamine (DA) and extracellular levels of its metabolites, 3, 4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA), were examined in vivo by intracerebral dialysis. A dialysis tube was implanted stereotaxically through bilateral caudate nuclei of rats and perfused with the Ringer solution. Amounts of DA, DOPAC and HVA in the perfusates were measured by high performance liquid chromatography (HPLC) with electrochemical detection. The basal level of DA was 2.76±0.64 pg/min, whereas the levels of DOPAC and HVA were 218.7±20.7 and 142.4±10.6 pg/min, respectively. Apomorphine (4 mg/kg, i.v.) reduced the efflux of DA and its metabolites. Haloperidol (0.4 mg/kg, i.v.) did not change DA release and produced only a minor increase of its metabolites. This increase of metabolites was inhibited by pargyline. Met-enkephalin (10-4 M), substance P (10-4 M) and acetylcholine chloride (10-4 M) added to the perfusing medium increased the release of DA. Met-enkephalin also increased the release of DOPAC. γ-Amino-n-butyric acid (GABA, 10-4 M) reduced the release of DOPAC and HVA when added to the perfusing medium. Thyrotropin releasing hormone (TRH, 5 mg/kg, i.v.) increased the release of HVA. These findings indicated that different mechanisms mediated effects of neurotransmitters or drugs on the release and metabolism of DA in the rat striatum.
  • Tetsuhiro HISAYAMA, Issei TAKAYANAGI
    1986 年 40 巻 1 号 p. 69-82
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The properties and mechanisms of Ca release induced by thymol from the intracellular Ca-store in the guinea-pig taenia caecum were investigated and compared with those by carbachol, using an intact muscle and a microsomal fraction. In Ca, Na-free, EGTA-containing K-solution, a transient contraction was evoked by each drug, and carbachol produced the contraction following treatment with thymol; however, a reversed sequence did not. The efflux of preloaded 45Ca in the presence and absence of ATP from taenia microsomes was accerelated by increasing concentrations of Ca ions outside. The minimal concentration to stimulate 45Ca-efflux was below 0.2 μM in both cases, and the Km values for Ca ions in the presence and absence of ATP were estimated to be 0.65 μM and 2.0 μM Ca ions, respectively. Thymol, which has been reported to be one of the most potent stimulators of the Ca-induced Ca release in the sarcoplasmic reticulum of skeletal muscle, enhanced the 45Ca-efflux from the taenia microsomes in the presence of ATP dose-dependently, and its mode of action seemed bimodal. That is, at 0.5 mM, thymol lowered the concentration of Ca ions which are needed to induce stimulation of 45Ca-efflux, whereas, at 1 mM, the stimulative effect of thymol on 45Ca-efflux was to augment the maximum rate of 45Ca-efflux, independent of concentrations of Ca ions. Carbachol (1 mM) did not have an effect on 45Ca-efflux with or without 0.1 mM GTP. In conclusion, the possibility has been suggested that in the guinea-pig taenia caecum, carbachol might release stored Ca ions via unknown pathway(s), whereas thymol directly releases Ca ions in a ATP-regulated fashion. Further, carbachol would be more efficaceous for releasing stored Ca ions. Notwithstanding, the Ca-stores and/or the Ca-releasing mechanisms, which are utilized by both thymol and carbachol, seemed to share a common part(s) to some degree.
  • Hiroyasu SATOH, Keitaro HASHIMOTO
    1986 年 40 巻 1 号 p. 83-93
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effects of procaine (50-500 μg/ml) on membrane potential and currents were investigated using a two microelectrode-voltage clamp technique. Procaine reduced the action potential amplitude (APA), the maximum diastolic potential and the maximum rate of depolarization (Vmax) in a dose-dependent manner. At the same time, the action potential duration and the cycle length were prolonged. In voltage clamp experiments, procaine (50 μg/ml) did not affect the slow inward current (Isi), but reduced the time-dependent outward current (Ik). At concentrations higher than 100 μg/ml, procaine reduced both currents and the inward current activated by hyperpolarization in a dose-dependent manner. In 7 of 20 specimens, a low concentration of procaine (50 or 100 μg/ml) increased Isi which enhanced the Vmax and APA, but did not increase Ik. Procaine did not affect the steady-state inactivation of Isi (f) and the activation of Ik (p). The results suggest that the depressions of currents induced by procaine are due to a reduction in conductances of the current systems.
  • Midori KAJIWARA, Kazuko AOKI, Kaori ISHII, Hiroaki NUMATA, Teruhiko MA ...
    1986 年 40 巻 1 号 p. 95-101
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Both agonist and antagonist actions of buprenorphine on isolated preparations were studied. The Ke (equilibrium dissociation constant) values of both naloxone and Mr 2266 [(-)-2-(3-furylmethyl)-5, 9-diethyl-2'-hydroxy-6, 7-henzomorphan] against buprenorphine and the ratio of IC50 (concentration of the drug to produce 50% inhibition of the twitch) value of buprenorphine after to before exposure of mouse vas deferens to β-FNA (β-fumaramate methyl ester derivatives of naltrexone), an irreversible mu antagonist, suggest that buprenorphine acts as both a mu and kappa agonist on mouse vas deferens. The agonist effect of buprenorphine at relatively high doses on guinea-pig ileum and mouse vas deferens and the negative agonist effect on both rat and rabbit vas deferens indicate that buprenorphine acts as a partial agonist on isolated preparations. The Ke values of buprenorphine show that buprenorphine has about equal antagonist effectiveness against a mu and kappa agonist with approximately five-fold lower effectiveness against a delta agonist. The possible mechanisms for the several characteristic actions of buprenorphine on guinea-pig ileum such as the slow onset of action, the increased magnitude of inhibition after washing the tissue, the negative elimination of the inhibition by either washing the tissue or the naloxone administration, and the negative elimination of the antagonist action by washing the tissue were discussed.
  • Seiichi KOMORI, Atsushi MIZUTANI, Yukinori AMANO, Yoshihiro KANAMARU, ...
    1986 年 40 巻 1 号 p. 103-113
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Acid-acetone extracts of the chicken rectum were subjected to chromatographic and electrophoretic separation, and two new smooth muscle-contracting substances close to purity were obtained. One of them showed chemical and biological characteristics similar to those of substance P, but it was clearly different from substance P on the basis of chromatographic and electrophoretic criteria. Thus, one could be a peptide belonging to the substance P-family. The other substance was also shown to be of peptide nature since its biological activity was destroyed by chymotrypsin and carboxypeptidase A. Parallel bioassay on the two tissues of the longitudinal muscle of the guinea-pig ileum and the isolated whole chick rectum revealed that none of the peptides such as substance P, physalaemin, kassinin, eledoisin, bradykinin and angiotensin II could be a candidate for the active substance. The biological activity was not antagonized by naloxone, suggesting that the substance was a peptide other than the opioid compounds. The molecular sizes estimated by gel filtration are 1300 for the substance P-like peptide and 1600 for the other substance. The possible physiological roles of the two substances as an excitatory non-adrenergic, non-cholinergic transmitter were discussed.
  • Kiyohisa UCHIDA, Yasuharu NOMURA, Haruto TAKASE, Toshio HARAUCHI, Tosh ...
    1986 年 40 巻 1 号 p. 115-122
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Feeding of vitamin K-deficient diets or fasting produced vitamin K deficient syndromes in both conventional and germ-free male rats in 3 days, increasing prothrombin time (PT), activated partial thromboplastin time (APTT), plasma and liver descarboxyprothrombin (PIVKA) levels and liver gamma-glutamylcarboxylase activities, but decreasing plasma clotting factor VII and prothrombin levels. These changes were not found when daily 30 μg/rat of vitamin K1 was injected during this period. The changes caused by fasting were comparable with those caused by a diet containing 20-30 ng/g of vitamin K1, while a diet containing less than 5 ng/g caused greater changes in both conventional and germ-free rats. Germ-free rats on a diet containing sufficient amounts of vitamin K1 showed PT and APTT values similar to those in conventional rats, but lower plasma clotting factor levels and higher PIVKA and microsomal gamma-glutamylcarboxylase activities. The values for PT, APTT, factor VII, prothrombin and PIVKA in the fasted germ-free rats were almost the same as those in the fasted conventional rats. These findings suggest that menaquinones synthesized in the large intestine are not utilized sufficiently to prevent vitamin K deficiency in rats.
  • Katsuhiko TAWARA, Munehiro TOMIKAWA, Yasushi ABIKO
    1986 年 40 巻 1 号 p. 123-133
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The mode of action of probucol in reducing serum cholesterol was studied in normal and cholesterol-fed mice. Probucol did not affect intestinal absorption of radioactive cholesterol in normal and cholesterol-fed mice. In normal mice, probucol treatment resulted in inhibition of incorporation of [14C]-acetate into cholesterol in the liver, while it stimulated the incorporation in the small intestines. Incorporation of [14C]-mevalonate into cholesterol was not affected by the treatment. These results were consistent with the finding that the HMG-CoA reductase activity was decreased in the liver, but increased in the intestinal tissues of the treated mice. In cholesterol-fed mice, probucol treatment had no effect on cholesterol synthesis in the liver, while it increased the intestinal cholesterol synthesis. The over-all effect of this drug on cholesterol synthesis was not significant, although it tended to be inhibitory in normal mice and stimulatory in cholesterol-fed mice. On the other hand, probucol treatment resulted in acceleration of the clearance of [14C]-cholesterol-derived radioactivity from the circulation and resulted also in a significant increase in fecal excretion of the radioactivity, cholesterol and bile acids without changes in lipid composition of the bile. Cholesterol content in and radioactivity distribution among the tissues were not affected by probucol. Hepatic cholesterol 7α-hydroxylase activity was increased by probucol. These findings indicate that probucol lowers serum cholesterol mainly by increasing catabolic excretion of cholesterol into bile.
  • Michihiko TSUJITANI, Eiichiro OKABE, Haruo ITO
    1986 年 40 巻 1 号 p. 135-141
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effect of potassium gluconate (K-GL) on K+ uptake of rat erythrocytes was investigated. K-GL produced a significant increase in active K+ transport of Na+-rich erythrocytes, while Na+, K+-ATPase activity of hemoglobin-free ghosts without a glycolytic system was unaffected. When the experiment was carried out in intact erythrocytes, K-GL increased the lactate production and ATP content, and it promoted the methemoglobin reduction rate. In Na+-rich erythrocytes, the glycolysis inhibitors which produced a marked reduction in lactate content abolished the K-GL-induced increase in K+ and ATP content without affecting the KCl-induced increase. These results suggest that K-GL enhances K+ transport of erythrocytes through acceleration of glycolytic process.
  • Yoshito KOTANI, Yasuaki HIROTA, Kazuna SUGIYAMA, Shigeharu JOH, Tohru ...
    1986 年 40 巻 1 号 p. 143-147
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effects of noxious electrical tooth stimulations and intraarterial administration of bradykinin or inhalation of volatile anesthetics on substance P content in the diencephalon-mesencephalon, pons-medulla and the spinal cord were examined in the rat. Noxious stimulation by electrical long duration stimulation (type 2) of tooth pulp caused an increase of substance P content in the ponsmedulla. Inhalation of volatile anesthetics such as methoxyflurane and diethylether produced an increase of substance P content in the spinal cord; and in addition, methoxyflurane produced a decrease of substance P content in ponsmedulla. However, halothane did not produce any changes in substance P content in any parts of the central nervous system (CNS). These results suggest that volatile anesthetics such as diethyl-ether and methoxyflurane act on the substance P neuron and may modulate pain transmission through the action of substance P in the pons-medulla or the spinal cord.
  • Akihide KODA
    1986 年 40 巻 1 号 p. 149-159
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    An experimental neurogenic bladder was induced in rats by an intraspinal injection of 10% phenol-glycerin solution. The functional and biochemical changes in the bladder were studied in vivo and ex vivo, and the effect of Robaveron, a biological prepared from swine prostate, on these changes were examined. The forced voiding pressure in the control rats which had been caused by the neurogenic bladder was reduced to 1/4-1/5 that of the intact animals. Robaveron recovered a decrease in the pressure, and the effect of 150-250 mg/kg, p.o., corresponded nearly to that of 40 mg/kg, i.m. In the ex vivo study with the strips of isolated neurogenic bladder muscle, the time required to cause 50% of the maximum contraction by transmural electric stimulation prolonged to about four times that of the intact one. Such a prolongation was recovered by Robaveron in a dose-dependent fashion, and the effect of Robaveron given p.o. corresponded to about 1/6 that of the drug given i.m. No change in Ca2+-influx, was found, although Ca2+-efflux was inhibited in the strip of neurogenic bladder muscle. Such an inhibition was significantly relieved in that of animals treated with Robaveron. In the neurogenic bladder rat, the ratio of bladder weight to body weight increased, and the activities of total ChE and AChE in the bladder muscle decreased, on which Robaveron did not show any influence. Phasic and tonic contractions in the strips of intact rat bladder and guinea pig ileum were inhibited by La3+, particularly phasic response in both the strips. Robaveron recovered the inhibition in a dose-dependent fashion. The present study suggests that the urinary dysfunction in neurogenic bladder may be caused not only by nervous disorders but also by changes in the bladder muscle itself. Robaveron was found to be effective for most of such changes. These findings may support the clinical efficacy of Robaveron for improving the attenuated bladder function.
  • Aiko TSUJIMOTO, Gozoh TSUJIMOTO, Kiyohiko KATO, Keitaro HASHIMOTO
    1986 年 40 巻 1 号 p. 161-168
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The effects of development upon adrenergic regulation of glycogenolysis were characterized using isolated hepatocytes from 3 different age groups of male rats (6 week-old, 8 week-old and 30 week-old). The phosphorylase a response in isolated hepatocytes to alpha-adrenergic stimulation decreased moderately with advancing age; whereas, that to beta-adrenergic stimulation declined more rapidly and almost disappeared at the age of 30 weeks. This developmental alteration in relative contribution of alpha- and beta-adrenergic regulation of phosphorylase was further confirmed by the experiments with specific antagonists. Also, the dramatic decrease of beta-adrenergic response on glycogen phosphorylase activity was found to be closely associated with a similar change of cAMP generation. In addition, the glucagon effect on cAMP production was found to be declined with advancing animal age. These results demonstrate that the glycogenolytic response of isolated rat hepatocytes to catecholamines can be mediated by different pathways according to the age of the animal; thus, juvenile male rats exhibit both the alpha- and beta-adrenergic mechanism for activation of phosphorylase and the maturation is associated with a modest decline of alpha receptor-mediated effect and a dramatic attenuation of a beta-adrenergic/cAMP response.
  • Den'etsu SUTOO, Kayo AKIYAMA, Naoyuki FUJII, Kazuhiro MATSUSHITA
    1986 年 40 巻 1 号 p. 169-173
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The effects of the Ca2+, Mg2+, Zn2+, Cd2+, Hg2+ and Mn2+ on the conformation of calmodulin (CaM) have been tested by using 400 MHz 1H NMR. In the aromatic region of the spectrum of CaM with a one molar ratio of cation per CaM, Zn2+, Cd2+, Hg2+ and Mn2+ induced spectral changes which were very similar to those seen for Ca2+. However, the Mg2+-induced change was different. These results are consistent with our pharmacological findings on divalent cations.
  • Tomitaro KITA, Taeko HATA, Takashi HIGASHIGUCHI, Eiji ITOH, Atsufumi K ...
    1986 年 40 巻 1 号 p. 174-177
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    In SART-stressed rats regarded as pathologically diseased model animals with vagotonic-type autonomic imbalance, a decrease of total acetylcholine (T-ACh) content and enhancements of choline acetyltransferase (CAT) and acetylcholinesterase (AChE) activities were recognized in the basal ganglia and hypothalamus. In contrast, in the duodenum, an increase in T-ACh content and a decrease in AChE activity were found, while CAT activity showed no change. These findings suggest that in both brain areas of basal ganglia and hypothalamus in SART-stressed rats, ACh neurons may be activated.
  • Minoru HARADA, Akira WATANABE, Mitsuo TAKEUCHI, Yasuko NIINOMI
    1986 年 40 巻 1 号 p. 178-181
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    PCA-eliciting activities of cephalothin and penicillin G-polymers were examined in rats sensitized with homologous IgE antibodies of mouse origin. Cephalothin-polymers elicited PCA regardless of the source of antibodies and the methods to raise them, the minimal effective dose being 2 to 20 μg/animal. Penicillin G-polymers provoked PCA only when anti-benzylpenicilloyl IgE antibody of C57BL/6J mouse raised early after immunization was used. The minimal effective dose in this case was 5 μg/animal, being comparable to that of cephalothin polymers.
  • Minoru HARADA, Akira WATANABE, Mitsuo TAKEUCHI
    1986 年 40 巻 1 号 p. 182-184
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The cross-reactivity of mouse anti-benzylpenicilloyl antibodies against cephalothin-haptens and cephalothin-polymers was divergent depending on the source and isotype of antibodies and the methods to raise them. High cross-reactivity nearly equal to the reactivity to homologous haptens and polymers was obtained only with the IgE antibody of C57BL/6J mouse raised shortly after an immunizing injection of the emulsion containing Freund's complete adjuvant and benzylpenicilloyl-bovine γ-globulin conjugate. With the other antibody preparations, cross-reactivity was moderate to negligible.
  • Hiroshi WATANABE, Michi-e TANIGUCHI
    1986 年 40 巻 1 号 p. 185-187
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Subchronic treatment with methamphetamine (3 mg/kg, s.c., twice daily for 14 days) attenuated hypomotility produced by a low dose of apomorphine (0.1 mg/kg, s.c.) and enhanced hypermotility induced by a high dose of apomorphine (3 mg/kg, s.c.) in mice. The treatment did not affect apomorphine-induced decrease in striatal DOPA accumulation following γ-butyrolactone plus m-hydroxybenzylhydrazine, an L-amino acid decarboxylase inhibitor, administration. These results suggest that drug sensitivity of presynaptic dopamine receptors in the striatum may not be altered after subchronic methamphetamine treatment.
  • Hiroshi MAEHASHI, Yuriko MURATA
    1986 年 40 巻 1 号 p. 188-190
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    The effects of 2, 3-dimercaptosuccinic acid (DMSA) and 2, 3-dimercaptopropane-1-sulfonic acid, Na salt (DMPS) on arsenic excretion in arsenic poisoning were studied using ICR mice. One group of mice was given arsenic trioxide (5 mg As/kg, s.c.) and another two groups were given DMSA or DMPS (100 mg/kg, i.p.) immediately after administration of the arsenic (5 mg/kg, s.c.). Arsenic excretion in urine and feces was determined by atomic absorption spectrophotometry. Results obtained showed a marked arsenic excretion in the urine collected at the first 12 hr in the group treated with DMSA. Further remarkable arsenic excretion in the feces was seen in the group treated with DMPS, suggesting that arsenic might have been excreted in the bile.
  • Toshimi HATTORI, Hiroshi MAEHASHI
    1986 年 40 巻 1 号 p. 191-193
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effects of 5 kinds of fluorides on the twitch of the sartorius muscle of the bull frog were investigated. All of the fluorides (0.1-2.0 mM) enhanced the twitch evoked by nerve stimulation. The extents of enhancement at 2.0 mM were in the order: stannous fluoride >> potassium fluoride > sodium silico fluoride > sodium fluoride > diammine silver fluoride. The extent of each enhacement was larger than that in the case of direct stimulation of the muscle. These findings show that fluorides commonly enhance the twitch of skeletal muscle and that the extent of enhancement is related to the properties of cations included in the fluoride.
  • Keiji YOKOYAMA, Mitsuru SHIMIZU, Osamu YAGASAKI
    1986 年 40 巻 1 号 p. 194-198
    発行日: 1986年
    公開日: 2006/09/15
    ジャーナル フリー
    Effect of external Ca2+ concentration ([Ca2+]o) on spontaneous and various types of stimuli-induced acetylcholine (ACh) release from guinea-pig ileum myenteric plexus was studied. Electrical field stimulation- or high-K+-induced ACh release increased with the increment of [Ca2+]o. On the other hand, the spontaneous and the nicotine-induced ACh release increased up to 0.45 mM [Ca2+]o and then declined progressively as [Ca2+]o was raised. Qualitatively similar results were obtained with dimethylphenylpirerazinium-, 5-hydroxytryptamine- and substance P-induced ACh release. These results were discussed in terms of the stabilizing effect of Ca2+.
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