The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Volume 40, Issue 2
Displaying 1-21 of 21 articles from this issue
  • Kazuaki KAWASHIMA, Hiroaki ARAKI, Hironaka AIHARA
    1986 Volume 40 Issue 2 Pages 199-204
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Chronic administration of imipramine and desipramine significantly reduced the duration of immobility in rats forced to swim in comparison with acute administration. However, amitriptyline did not potentiate the reductive effect of chronic administration. Chlorimipramine, a selective serotonin uptake inhibitor, did not affect the duration of immobility in both the acute and chronic administration. On the other hand, the chronic administration of chlorpromazine, haloperidol and diazepam enhanced the duration of immobility, whereas their acute administration had no effect on it. Sulpiride reduced and enhanced the duration of immobility by the acute and chronic administration, respectively. The present results suggest that the chronic administration of drugs to rats in a forced swimming test can clarify the characteristics of the psychotropic drugs.
    Download PDF (444K)
  • Yoshiko MORITA
    1986 Volume 40 Issue 2 Pages 205-214
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    A serum extract possessing ACTH-potentiating activity was partially purified by Sephadex G-100 gel filtration. Fractions from 9, 000 to 40, 000 in molecular weight (APS-Fr) potentiated the corticosterone production induced by synthetic adrenocorticotropic hormone (ACTH1-24). Approximately 5μg (as protein) of APS-Fr in 0.5 ml medium showed the maximum activity to potentiate the response of isolated rat adrenal cells to ACTH1-24 Puromycin, cycloheximide and actinomycin D did not abolish the potentiation by APS-Fr of ACTH1-24-induced steroidogenesis. The log-dose response curve for ACTH1-24 was shifted toward the side representing lower doses of ACTH1-24 by APS-Fr, but the maximum response was not changed. In a typical experiment, the median effective dose (ED50) for ACTH1-24 was decreased from 5.2×10-11 M to 3.0×10-12 M. ACTH1-24-induced production of cyclic AMP was also increased by APS-Fr. Time courses of both corticosterone and cyclic AMP production induced by ACTH1-24 did not differ qualitatively in either the presence or absence of APS-Fr, although they showed a marked difference quantitatively. When dibutyryl cyclic AMP was used in place of ACTH1-24, APS-Fr did not potentiate steroidogenesis. These results suggest that APS-Fr acts at a step between the binding of ACTH to its receptor and the formation of cyclic AMP. ACTH1-24-induced steroidogenesis which was increased by increasing concentration of calcium in the medium, was further increased by addition of APS-Fr. The calcium requirement for the same degree of response was decreased by addition of APS-Fr, in a similar way to when a higher concentration of ACTH1-24 was used.
    Download PDF (705K)
  • Yoshiko MORITA
    1986 Volume 40 Issue 2 Pages 215-230
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Peptides that potentiate the response of adrenal cells to ACTH1-24 were isolated from rat serum. ACTH-potentiating activity was found in fractions of 9, 000-40, 000 in molecular weight (APS-Fr) and of smaller molecular weight (SM-Fr) on Sephadex G-100 gel filtration of the serum extract. The peptides were isolated from APS-Fr by preparative acid polyacrylamide gel electrophoresis and named d1, d, d2, e, f and g. Their molecular weights, estimated by Sephadex G-75 gel filtration, were 41, 000, 33, 000, 24, 000, 17, 500, 17, 500 and 16, 000, respectively. All of these peptides were glycopeptides. The isoelectric point of peptide d was 8.45 and some of the others, such as f and g, were more basic. Sodium dodecyl sulfate (SDS) polyacrylamide gel electrophoresis revealed that these peptides were decomposed into various fragments. ACTH-potentiating activity was highest in peptide d1 and lowest in peptide e. The maximum activity of peptide d was observed at 3×10-8 M when steroidogenesis was induced by 9×10-12 M ACTH1-24. While these peptides did not show any ACTH-like activity at any stage of isolation, the fractions of these peptides eluted from a Sephadex G-75 column showed more or less ACTH-like activity. These peptides therefore seemed to possess latent ACTH-like activity. The molecular weight of SM-Fr was smaller than ACTH1-24. The ACTH-potentiating activity of SM-Fr was low, and SM-Fr did not show any ACTH-like activity. SM-Fr therefore seems to be the smallest structure which has ACTH-potentiating activity. The similarity of these peptides to proopiomelanocortin-related substances was discussed.
    Download PDF (1382K)
  • Yukinobu GOTOH, Shinji SHIBANOKI, Koichi ISHIKAWA
    1986 Volume 40 Issue 2 Pages 231-237
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    The direct correlation analyses between the distribution of chlorpromazine (pharmacokinetics) and the biochemical effects of the drug on monoamine metabolisms (pharmacodynamics) are reported. Both samples for quantitative determination of CPZ and of monoamine transmitters and metabolites were obtained by organic extraction procedures from the same sample. The determinations were carried out by high performance liquid chromatography with electrochemical detection. CPZ affected the concentrations of metabolites of noradrenaline, dopamine and 5-hydroxytryptamine, but not those of the monoamine transmitters themselves. However, simultaneous assay demonstrated differences in effects of the drug on the transmitter systems. The concentrations of HVA and DOPAC were increased over a wide range of intracerebral concentrations of the drug, but those of MOPEG, in the range of higher concentrations. On the other hand, CPZ did not reveal any correlations between the intracerebral concentrations of the drug and 5-HIAA. These results suggest that CPZ affected primarily the dopaminergic system rather than the serotonergic one in the early stage of its biochemical actions. The proposed procedure is demonstrated to be simple and useful as a new approach in biochemical pharmacology. The same procedure can be applicable for other centrally acting drugs.
    Download PDF (593K)
  • Susumu OKABE, Eiko HIGAKI, Tomoko HIGUCHI, Masaru SATO, Kaoru HARA
    1986 Volume 40 Issue 2 Pages 239-249
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Biochemical and pharmacological properties of a newly synthesized compound, 2-[(2-dimethylaminobenzyl)sulfinyl] benzimidazole (NC-1300), were studied. NC-1300, at pH 6.0, potently inhibited the activity of H+K+ATPase in the rabbit gastric mucosa, thereby classifying it as a proton pump inhibitor. The inhibitory efficacy of NC-1300 on the pump was much the same as that seen with omeprazole. NC-1300 had no effect on acetylcholine-stimulated ileum contraction in guinea pigs at 10-5 M, but it non-competitively inhibited the contraction at 10-4 M. NC-1300 had no effect on histamine-stimulated atrial beating frequency in guinea pigs at 10-4 or 10-5 M. NC-1300, given either intraduodenally or orally, had a potent and long-lasting (more than 24 hr) inhibitory effect on gastric secretion in pylorus-ligated rats. Pretreatment with NC-1300 dose-dependently protected the gastric mucosa from damage induced by pylorus ligation, water-immersion stress, aspirin, and indomethacin, and the duodenal mucosa from damage induced by mepirizole in rats. We conclude that the antisecretory activity of NC-1300 appears to be mainly related to an inhibition of H+K+ATPase, while its anti-gastric and antiduodenal lesion activities are primarily related to an antisecretory effect.
    Download PDF (785K)
  • Masayasu KIMURA, Ikuko KIMURA, Hiroshi NOJIMA, Masashi MUROI
    1986 Volume 40 Issue 2 Pages 251-256
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    The myopathy in skeletal muscles of genetically diabetic male KK-CAy mice or alloxan-induced diabetic mice was investigated. In these diabetic mice, nerve-stimulated twitch tensions of in situ sciatic nerve-gastrocnemius muscle preparations were inhibited by intraarterially administered succinylcholine (SuCh) to a greater extent than in normal (non-diabetic) ones. Despite the high blood glucose level, at one week after alloxan administration, no hypersensitivity to SuCh was induced in mice, but mice at 2 weeks and 4 weeks after alloxan showed greater sensitivities. In isolated diaphragm muscles of diabetic KK-CAy mice, the acetylcholine (ACh, iontophoretically applied) potential amplitude was greater than in KK-CAy prediabetic muscles. SuCh in diabetic KK-CAy muscles inhibited ACh potentials to a greater extent than in normal ddY muscles. Hill coefficients obtained from the inhibition curve by SuCh of the nerve-stimulation response were decreased by the diabetic state. The sensitivities to d-tubocurarine and α-bungarotoxin were the same in both kinds of muscles. Both extrajunctional ACh receptors in denervated muscles of normal ddY and diabetic KK-CAy mice revealed the lower sensitivity to SuCh than junctional receptors in non-denervated normal muscles. In conclusion, diabetic muscles showed the hypersensitivity restricted to SuCh. These phenomena are neither due to glycosylation nor to denervation supersensitivity.
    Download PDF (483K)
  • Ikuko SHIMIZU, Noboru TODA
    1986 Volume 40 Issue 2 Pages 257-263
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Contractile responses to ouabain in helical strips of dog and monkey coronary arteries were investigated. Ouabain (5×10-8 to 5×10-6 M) caused a dose-related contraction in dog and monkey arteries; the response of monkey coronary arteries was significantly greater. In dog coronary arteries, contractile responses to high concentrations of ouabain were potentiated by treatment with propranolol. In the arteries contracted with ouabain, the addition of phentolamine caused a relaxation. Contractile responses of dog coronary arteries to ouabain were markedly suppressed by exposure to Ca2+-free media or by treatment with verapamil. Reduction of external concentration of K+ or lowering the temperature of bathing media did not selectively influence the ouabain-induced contraction. These results suggest that ouabain-induced contractions of dog coronary arteries are associated mainly with an increase in the Ca2+-influx, which does not result from an inhibition of the Na+ K+-activated ATPase nor from an activation of α adrenoceptors by noradrenaline released from adrenergic nerves. Ouabain in high concentrations seems to liberate noradrenaline from adrenergic nerves, which preferentially activates β adrenoceptors in dog coronary artery.
    Download PDF (502K)
  • Katsuya MORITA, Toshihiro DOHI, Akira TSUJIMOTO
    1986 Volume 40 Issue 2 Pages 265-271
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Nicotine and muscarine caused the transient increase in cAMP and cGMP efflux from dog adrenal glands followed by a small but lasting increase in the nucleotide efflux. The initial increase preceded catecholamine (CA) release and the latter slowly developed. Nicotine and muscarine caused the maximal increase of cAMP and cGMP levels in adrenal medulla 15 sec after the treatment, and these effects were antagonized by hexamethonium and atropine, respectively. Hexamethonium in combination with atropine, verapamil and an omission of Ca2+ in the medium prevented ACh from producing the increase in cyclic nucleotide efflux and CA release. Reintroduction of Ca2+ (1.3 mM) in fluid after perfusion with Ca2+ and Mg2+-free fluid caused the transient increase in cyclic nucleotide efflux and CA release. Adenylate cyclase activity in adrenal medulla was activated by Ca2+. These results may suggest that cAMP formation was increased by activation of adenylate cyclase as a result of increased influx of Ca2+ when adrenal medulla were stimulated.
    Download PDF (529K)
  • Hiromichi TSURU, Toshihiko UEMATSU
    1986 Volume 40 Issue 2 Pages 273-282
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Changes in the sensitivity of the rabbit ear artery to exogenous norepinephrine and potassium and to sympathetic nerve electrical stimulation were examined in vitro following decentralization which was performed by removing the unilateral preganglionic nerve proximal to the superior cervical ganglion. The contralateral side was left intact as a control. The postjunctional supersensitivity to exogenous norepinephrine and potassium had fully developed one week after the decentralization and was sustained for at least 8 weeks; the arteries decentralized for 1-8 weeks were about 2.1- and 1.3-fold supersensitive to norepinephrine and potassium, respectively, as compared with the contralateral control arteries. The frequency-response curve of the electrically stimulated decentralized artery shifted gradually to the left of the control within weeks after decentralization. Since the response to electrical stimulation was attributed to endogenous norepinephrine released from the sympathetic nerve terminals within the adventitial-medial junction, the leftward shift of the frequency-response curve in the decentralized artery probably reflects a gradual increase in the released norepinephrine per pulse by electrical stimulation, i.e., the prejunctional supersensitivity to electrical stimulation. It is concluded that the prejunctional sympathetic supersensitivity to electrical stimulation develops slower than the postjunctional nonspecific supersensitivity in the rabbit ear artery. The change in the sensitivity of the denervated postganglionic neuron, including the superior cervical ganglion is also discussed with regard to the "law of denervation supersensitivity".
    Download PDF (805K)
  • Seiji NOMA, Masashi SASA, Yukihiro OHNO, Izuru MATSUOKA, Shuji TAKAORI
    1986 Volume 40 Issue 2 Pages 283-290
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    ElectrophysiologicaI studies were performed to elucidate the mechanism underlying the antivertigo action of eperisone, an antispastic drug, using cats anesthetized with α-chloralose. lontophoretic application of eperisone up to 100 nA produced a dose-dependent inhibition of spike generation upon vestibular nerve stimulation in monosynaptic and polysynaptic neurons of the medial vestibular nucleus (MVN). The inhibition of neurons in the MVN was more prominent than that in the lateral vestibular nucleus. In addition, iontophoretically applied eperisone in doses of 50-100 nA inhibited the orthodromic spike elicited by vestibular nerve stimulation in the MVN monosynaptic neurons projecting to the abducens nucleus (ascending neuron), without affecting that in the MVN neurons projecting to the spinal cord (descending neuron). An inhibition of antidromic spike elicited by abducens nucleus stimulation in the MVN monosynaptic ascending neurons was observed in some cases during application of eperisone. These results suggest that eperisone predominantly inhibits synaptic transmission of the MVN ascending neurons.
    Download PDF (514K)
  • Rie MIYOSHI, Shozo KITO, Kumiko MIZUNO, Hiroaki MATSUBAYASHI
    1986 Volume 40 Issue 2 Pages 291-296
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    The authors noticed effects of somatostatin on muscarinic acetylcholine receptors (mAchR) in the rat hippocampus from binding experiments. Saturation experiments of 3H-oxotremorine-M-acetate (3H-oxo-M) buffered with Krebs-Henseleit solution revealed that there were two binding sites with very high and low affinities whose Kd values were 1.2 nM and 445.8 nM, respectively. Adding somatostatin in this incubation medium caused an increase in the Kd value of the high affinity binding site with no change in the Bmax value. As for the low affinity binding site, Kd and Bmax values were too large to determine the effect of somatostatin. The oxotremorine/3H-N-methyl-scopolamine competition experiments indicated the presence of two components of agonist binding sites. The inhibition curve after adding somatostatin fitted best to a single homogenous binding site whose Ki value was consistent with the dissociation constant of the oxotremorine low affinity binding site. Therefore, it seems that somatostatin accelerates conformational changes of the oxotremorine high affinity binding site to the low affinity binding state. A single binding site with a Kd value of 30.9 nM was obtained by switching the buffer to Na-K phosphate solution. The affinity of this binding site was likewise inhibited by somatostatin. The inhibitory effect of somatostatin-28 was more marked than that of [D-trp8] somatostatin. The above-mentioned effects of somatostatin was limited to mAchR agonist binding.
    Download PDF (422K)
  • Kazuko AOKI, Midori KAJIWARA, Tetsuo OKA
    1986 Volume 40 Issue 2 Pages 297-302
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    The enkephalin-hydrolyzing peptidases in mouse vas deferens were studied and compared with those in guinea pig ileum which had been characterized in the previous study. The present results showed that three distinct peptidases, bestatin-sensitive aminopeptidase, captopril-sensitive peptidyl dipeptidase A, and thiorphan-sensitive endopeptidase-24.11, played a critical role in the inactivation of enkephalin in mouse vas deferens, being consistent with the previous results obtained with guinea pig ileum. However, the data in both previous and present studies showed that the activity of the bestatin-sensitive aminopeptidase relative to that of either the captopril-sensitive peptidyl dipeptidase A or the thiorphan-sensitive endopeptidase-24.11 in guinea pig ileum was higher than that in mouse vas deferens, while the activity of either peptidyl dipeptidase A or endopeptidase-24.11 relative to that of aminopeptidase in mouse vas deferens was higher than that in guinea-pig ileum. In contrast to these three enzymes, both L-tyrosyl-L-tyrosine-sensitive dipeptidyl aminopeptidase and D-phenylalanine-sensitive carboxypeptidase were suggested not to be involved significantly in the inactivation of enkephalin in mouse vas deferens as well as guinea pig ileum.
    Download PDF (455K)
  • Hisashi KURIBARA, Sakutaro TADOKORO
    1986 Volume 40 Issue 2 Pages 303-310
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Characteristics of the acquisition processes of discrete lever-press and shuttle avoidance responses (intertrial interval=25 sec, warning duration=5 sec with an escape contingency, and 1 session=1 hr training/day) as well as those of the ambulatory activity were investigated in 6 strains of mice (dd, ICR, BALB/c, C57BL/6, C3H/He and DBA/2). In the lever-press avoidance situation, the dd, BALB/c and DBA/2 strains demonstrated a good avoidance response, showing average avoidance rates of higher than 80% within 10-15 sessions of the training. The C3H/He also demonstrated a good avoidance response, though 20 sessions or more of the training were required to attain to the level. The ICR and C57BL/6 strains demonstrated a poorer avoidance response than the other 4 strains, and achieved average avoidance rates of 30-40%. The dd, BALB/c, C3H/He and DBA/2 strains also demonstrated a good shuttle avoidance response when they were trained in an experimental box of 50 cm in width. In contrast, the ICR and C57BL/6 strains demonstrated an extremely poor avoidance response in this situation, showing an average avoidance rate of less than 10%. However, when the dd, ICR and C57BL/6 strains were trained in a shuttle box of 30 cm in width, they rapidly acquired the avoidance response, and the average avoidance rates finally achieved were much higher than those of the mice trained in the shuttle box of 50 cm in width. In particular, the C57BL/6 strain exhibited the best avoidance response among the 3 strains. The ambulatory activity of the C57BL/6 strain was less than those of the other 5 strains.
    Download PDF (654K)
  • Mayumi MORI, Hiromi TSUSHIMA, Tomohiro MATSUDA
    1986 Volume 40 Issue 2 Pages 311-318
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Effects of dibutyryl-cyclic AMP (db-cAMP) and cyclic AMP (cAMP) when microinjected into the hypothalamic paraventricular nucleus (PVN) in a water-loaded and ethanol-anesthetized rat on the rate of urine outflow, urine osmotic pressure and other visceral functions were investigated. The microinjection of db-cAMP decreased the rate of urine outflow with concomitant increase in the urine osmotic pressure, but did not change mean blood pressure, heart rate, respiration rate and rectal temperature. The antidiuretic effect of db-cAMP was more potent than the effect of cAMP, the median effective doses (ED50) being approx. 40 nmol for db-cAMP and more than 300 nmol for cAMP, respectively. The time-courses for the antidiuretic effects and for the increase in the urine osmotic pressure showed a similar pattern, with the maximal effect at approx. 30 to 40 min and the duration of approx. one hour or longer. The effect of db-cAMP was potentiated by pretreatment with methylxanthines and inhibited by pretreatment with atropine. A second microinjection of db-cAMP induced a less potent anti-diuretic effect than the first microinjection (tachyphylaxis). The results indicated the antidiuretic effects of microinjection of db-cAMP and cAMP into the PVN, and a possible mechanism for this was discussed.
    Download PDF (603K)
  • Hiromi TSUSHIMA, Mayumi MORI, Tomohiro MATSUDA
    1986 Volume 40 Issue 2 Pages 319-328
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Effects of catecholamines microinjected into the paraventricular nucleus in the hypothalamus on urine outflow in a rat which was loaded with water and anesthetized with ethanol were studied. L-Norepinephrine, L-epinephrine and L-isoproterenol induced potent antidiureses with similar time courses to each other. The ED50 values for L-norepinephrine, L-epinephrine and L-isoproterenol were approximately 5, 10 and 5 nmol, respectively. The D-isomer of isoproterenol demonstrated no significant antidiuretic activity. The effect of L-norepinephrine was inhibited strongly by premicroinjection of alpha- and beta-adrenoceptor antagonists. The effect of DL-isoproterenol was inhibited strongly by beta-adrenoceptor antagonists, but not affected by alpha-adrenoceptor antagonist. Premicroinjection of a muscarinic antagonist, atropine, partially inhibited anti-diuretic effects induced by L-norepinephrine and DL-isoproterenol. Visceral functions other than urine outflow such as mean blood pressure, respiration rate, heart rate and rectal temperature were not significantly altered when the urine outflow decreased down to 20-30% of the control by microinjection of L-norepinephrine and DL-isoproterenol. The results demonstrated that stimulation of alpha- and beta-adrenoceptor in the paraventricular nucleus induced potent antidiuretic effects, partial inhibition of which by atropine suggested a possible presynaptic facilitation of the release of ACh by the stimulation of the adrenoceptors.
    Download PDF (731K)
  • Susumu OKABE, Hiroshi JINO, Akito NISHIDA
    1986 Volume 40 Issue 2 Pages 329-337
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    We studied the effects of 15(R)-15-methyl prostaglandin E2 (arbaprostil) on gastric secretion and various acute and chronic gastric lesions produced in rats. Arbaprostil significantly inhibited gastric secretion in 4 hr-pylorus-ligated preparations when given intraduodenally in a dose of 30 or 100 μg/kg. The agent, however, significantly stimulated gastric secretion of rats with either a ligated or intact pylorus when given orally in doses of 3-100 μg/kg. Orally administered arbaprostil dose-dependently prevented the development of HCl-ethanol-, histamine-, water-immersion stress-, or indomethacin-induced gastric erosions. Intraduodenally administered arbaprostil also dose-dependently prevented the development of aspirin-induced gastric erosions in pylorus-ligated rats. Arbaprostil, given orally in doses of 1-100 μg/kg twice daily for 2 weeks, had little or no effect on the healing of acetic acid-induced gastric ulcers. However, oral administration of the agent in a dose of 3 or 10 μg/kg twice daily for 4 weeks significantly accelerated the healing of acetic acid-induced gastric ulcers. The increase in doses up to 100 μg/kg twice daily for 4 weeks had no effect on ulcer healing. These results indicate that arbaprostil, at either antisecretory or even acid stimulating doses, is effective in preventing the development of acute gastric erosions and in accelerating the healing of chronic gastric ulcers.
    Download PDF (664K)
  • Satoshi YUASA, Atsuko SUDOH, Kohei UMEZU
    1986 Volume 40 Issue 2 Pages 339-341
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    The effects of tritoqualine (TRQ) on established cell lines of fibroblasts, Balb/3T3 and 3T6, were investigated with respect to growth and collagen secretion. TRQ suppressed growth rate in the log phase and inhibited collagen secretion in the stationary phase of both cell lines. However, TRQ was not cytotoxic because of lack of influence on cell maintenance in the stationary phase. These effects of TRQ are thought to be very important as a mechanism of inhibitory action against liver fibrosis in chronic liver injury in rats.
    Download PDF (240K)
  • Keita KAMIKUBO, Hiroshi MURASE, Masanori MURAYAMA, Kiyoshi MIURA
    1986 Volume 40 Issue 2 Pages 342-346
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Akaike's information criterion (AIC) (Akaike, H., IEEE Trans. Automat. Contr. AC-19, 716-723 (1974)) was applied to estimate statistically the number of classes of binding sites from ligand-binding data. Several sets of data were analyzed by both the AIC method and the F-test method. Good agreement was obtained between results from both methods. The present results suggest that the AIC method can be a good alternative to the F-test to estimate the number of classes of sites.
    Download PDF (431K)
  • Mitsukazu KITADA, Naoko YAMAGUCHI, Tadaaki RIKIHISA, Yoshio KANAKUBO, ...
    1986 Volume 40 Issue 2 Pages 347-349
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Cytochrome b5 did not exert any effect on NADPH-dependent aniline hydroxylation in the absence of acetone or 2, 2'-bipyridine, whereas cytochrome b5 exhibited a stimulatory effect on the reaction in the presence of acetone or 2, 2'-bipyridine. In addition, cytochrome b5 did not have any significant effect on the cumerie hydroperoxide-dependent reaction in the presence of acetone or 2, 2'-bipyridine.
    Download PDF (251K)
  • Kenichi MIYAMOTO, Takayuki MATSUNAGA, Yoshihiro WAKI, Ryozo KOSHIURA
    1986 Volume 40 Issue 2 Pages 350-352
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    Among several sympathomimetic drugs, isoproterenol, epinephrine and norepinephrine significantly potentiated the cytotoxic effect and the uptake of MMC into rat ascites hepatoma AH1 30 cells in in vitro experiments, but salbutamol, tulobuterol and phenylephrine did not. The enhancement of MMC uptake into AH130 cells by isoproterenol and norepinephrine was diminished by propranolol but not by phentolamine. These results indicate that the cytotoxic effect and the uptake of MMC is potentiated by the stimulation of β-adrenoceptors, but not by stimulation Of β2- and α-receptors.
    Download PDF (213K)
  • Kumi SUGIHARA, Munekazu GEMBA
    1986 Volume 40 Issue 2 Pages 353-355
    Published: 1986
    Released on J-STAGE: September 15, 2006
    JOURNAL FREE ACCESS
    -cis-Diamminedichloroplatinum II (cisplatin) is a potent anticancer chemotherapeutic agent. The major limitation in its use is nephrotoxicity, caused by an unknown mechanism. Injection of cisplatin into rats caused a decrease in body weight and an increase in blood urea nitrogen (BUN). These effects were modified by giving a radical scavenger, α-tocopherol, before the cisplatin injection. N-N'-diphenyl-p-phenylenediamine, another powerful radical scavenger, also attenuated the increase in BUN induced by cisplatin. These results suggest that the toxic effects of cisplatin may be related to free radical induced damage.
    Download PDF (184K)
feedback
Top