The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Volume 23 , Issue 5
Showing 1-24 articles out of 24 articles from the selected issue
  • G. BENZI, E. ARRIGONI, P. PANCERI, R. PANZARASA, F. BERTE', A. CREMA
    1973 Volume 23 Issue 5 Pages 599-607
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    The effect of certain antibiotics on the ureteral tone and motility has been studied in vitro and in situ in guinea-pigs and dogs. Tetracycline and rolitetracycline induced a constriction, while ampicillin, isoxazolyl penicillins, gentamicin, aminosidin, spiramycin and chloramphenicol induced a relaxation of the ureter. In vivo, the responses were independent of both bladder activity and systemic effects related to the antibiotic flowing into the ureter and eventually absorbed from it. The antibiotics acted directly on the ureteral smooth muscle; factors influencing the action were: (a) the free or conjugated form of the antibiotic flowing through the ureter; (b) pH of the urine; (c) time of contact; (d) time lag.
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  • T.N. BHALLA, J.N. SINHA, R.P. KOHLI, K.P. BHARGAVA
    1973 Volume 23 Issue 5 Pages 609-614
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Phenylquinone, bradykinin and aconitine induced writhing syndromes have been compared as to screening suitability for analgesic agents. It was observed that aconitine induced writhing appears more quickly, is more frequent and lasts for a longer period. Drug antagonism studies show that both phenylquinone and bradykinin induced writhing responses and are antagonised by antipyretics as well as narcotic analgesics, while aconitine induced writhing syndrome, is more selectively antagonised by the antipyretic analgesic agents.
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  • Yasuko SHINAGAWA, Yoshiya SHINAGAWA
    1973 Volume 23 Issue 5 Pages 615-626
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    The reaction indices of π-electronic structures of the diuretics, xanthine, thiazide and triazine derivatives were calculated. An attempt was made to explain the potency of the diuretic action in the light of quantum chemistry. The reaction indices of xanthine derivatives, the first frontier superdelocalizability at the substituent occupying the 7-position of the highest occupied orbital and the second frontier superdelocalizability at the 3-position of the occupied orbital show fairly good correlations with the diuretic activities. The reaction index Sr(E) is defined as: Sr″= fr11+fr22, where subscripts 1 and 2 stand for the highest occupied (or the lowest unoccupied) orbital, and the next highest occupied (or the next lowest unoccupied) orbital, fr is the electron density of the corresponding orbital and λi (i=1, 2) is the coefficient of energy in the i-th molecular orbital ε=α+λ1β, α and β being the standard Coulomb and resonance integrals. The diuretic activities of thiazide derivatives are in good parallel with the reaction indices, the π-electron densities at the 2-position, at the 4-position and at the 7-position. The potency of carbonic anhydrase inhibition of thiazide derivatives and sulphonamide derivatives however are fairly well parallel with the reaction indices, the π-electron density of the lowest unoccupied orbital and the formal charge at the position of amino group or at the position of nitrogen atom in sulphonamide. The diuretic activities of triazine derivatives show good correlation with the reaction indices, the first frontier superdelocalizability of the lowest unoccupied orbital at the 1-position (carbon atom) and the π-electron density of the unoccupied orbital at the 4-position (nitrogen atom). The positions of these diuretics, which are assumed to play the important role in diuretic action, are the positions in the group =N- ?? -N=. As the values of the Coulomb integral and the resonance integral of trill uoromethyl group (CF3) and the Coulomb integral of carbon atom adjacent to this pseudo-atom, α 2.0β, 1.0β and α-0.1β are employed.
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  • 2ND REPORT: ELEVATION OF NADH-CYTOCHROME c REDUCTASE ACTIVITY IN THE LIVER CELL MEMBRANE OF RATS FOLLOWING CCl4 ADMINISTRATION
    Yasusuke MASUDA, Masato KUCHII, Ichiro YANO, Hiroyuki YAMAMOTO, Tadash ...
    1973 Volume 23 Issue 5 Pages 627-637
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Distinct fractional zones of cell membranes in sucrose gradients were obtainable from homogenates of rat liver up to 6 hr (females) and 12 hr (males) following an i.p. injection of CCl4 (0.2 ml/kg body wt.). CCl4 administration to rats caused a marked elevation of NADH-cytochrome c reductase activity in the liver cell membrane. There was a remarkable difference between sexes with respect to time-course of the changes of the enzyme activity, viz., a. peak was reached 6 hr after administration in female rats and 12 hr in male rats with normal activity at 6 hr. Neither mitochondrial fractions nor microsomal fractions of rat liver displayed any significant alterations in NADH-cytochrome c reductase activity 6 hr after CCl4 administration.
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  • 3RD REPORT: ON THE PURITY OF LIVER CELL MEMBRANE FRACTION ISOLATED FROM CCl4-TREATED RATS
    Masato KUCHII, Yasusuke MASUDA, Nobuyuki OKADA, Hiroyuki YAMAMOTO, Tad ...
    1973 Volume 23 Issue 5 Pages 639-644
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Purity of the cell membrane fraction from CCl4-treated rats was studied using markers of other fractions; DT-diaphorase in supernatant, cytochrome c oxidase and succinate-cytochrome c reductase in mitochondria, and NADPH-cytochrome c reductase, glucose-6-phosphatase and RNA in microsomes. Cell membrane fractions were not contaminated with supernatant DT-diaphorase, but were contaminated by mitochondrial fraction in both normal and CCl4-treated rats to some extent. Glucose-6-phosphatase activity and RNA content of the normal membrane fraction were 9 % and 6 % of microsomes, respectively. Administration of CCl4 did not increase the contamination. However, NADPH-cytochrome c reductase activity was increased about 4 times as was the case with NADH-cytochrome c reductase following CCl4 treatment. Thus, it may be concluded that elevation of NADH-cytochrome c reductase activity in the cell membrane fraction 6 hr after administration of CCl4 does not result only from the contamination with other subcellular fractions during the isolation procedure.
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  • 4TH REPORT: ELECTRON MICROSCOPIC OBSERVATIONS ON CHANGES IN ULTRA-STRUCTURE OF LIVER CELL MEMBRANES IN CCl4-TREATED RATS
    Ichiro YANO, Yasusuke MASUDA, Masato KUCHII, Hiroyuki YAMAMOTO, Tadash ...
    1973 Volume 23 Issue 5 Pages 645-652
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Morphological changes of liver cell membranes in CCl4-administered rats were observed electronmicroscopically by using mainly a negative staining method. CCl4 caused not only disappearance of elementary particles attached to the surface of cell membranes, but also that of hexagonal subunit patterns (treated with 1% DOC) in the membranes of tight junction 3-6 hr after administration. Present data indicates that CCl4 primarily affects the plasma membrane rather than endoplasmic reticulum.
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  • 5TH REPORT: CHARACTERIZATION OF NADH-CYTOCHROME c REDUCTASE OF LIVER CELL MEMBRANE IN NORMAL AND CCl4-TREATED RATS
    Yasusuke MASUDA, Masato KUCHII, Hiroyuki YAMAMOTO, Tadashi MURANO
    1973 Volume 23 Issue 5 Pages 653-663
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    NADH-cytochrome c reductase activity of the cell membrane was not significantly inhibited by KCN, NaN3, Antimycin A or rotenone but was evidently inhibited by PCMB and also by NEM. Km values for NADH in NADH-cytochrome c reductase or NADH-ferricyanide dehydrogenase of the cell membrane were almost equal to those in the microsomes. These Km values were hardly affected by administration of CCl44. Cytochrome b5 and P-450 were identified in the cell membrane fraction, and the contents were normally remarkably low as compared with those in the microsomal fraction. However, they increased approx. two-fold following CCl4 administration, while those in microsomes conversely diminished by half. NADH-cytochrorne b5 reductase activity in the cell membrane fraction was approx. onethird as low as NADH-cytochrome c reductase activity. The former was virtually unaffected by administration of CCl4. It is proposed that NADH-cytochrome c reductase in the cell membrane originates from microsomes but not from mitochondria and that increase in the enzyme activity after CCl4 administration may be caused by migration of hemo- and flavo- protein from endoplasmic reticulum to plasma membranes of liver cells in vivo.
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  • Takao SATO, Issei TAKAYANAGI, Keijiro TAKAGI
    1973 Volume 23 Issue 5 Pages 665-671
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Two kinds of spikes, a single-spike unit and burst unit, were obtained by a glass suction electrode recording from neurons in Auerbach's plexus of the guinea pig ileum. Both spikes were inhibited by tetrodotoxin but not by Mn2+. Frequency of the single-spike unit was increased by nicotine and high concentrations of acetylcholine. The single-spike unit induced by nicotine was inhibited by hexamethonium, while hexamethonium was without any effect on the spontaneous single-spike unit. Morphine inhibited the spontaneous single-spike unit. The spontaneous singlespike unit was also inhibited by α-adrenergic stimulants but not by β-adrenergic stimulants. Inhibition of single-spike unit activity by the α-adrenergic stimulants was antagonized by α-adrenergic blockers. These findings indicate that the single-spike unit is concerned with cholinergic transmission in Auerbach's plexus. The singlespike unit evoked by nicotine was partly inhibited by morphine or α-adrenergic stimulants. This fact indicated the possibility that morphine and the α-adrenergic stimulants also inhibit the acetylcholine release from the cholinergic nerve at the ending of the post-ganglionic fibres. On the other hand the burst unit was little affected by the drugs utilized herein.
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  • Seth S.D.S., Mukhopadhyay A., Bagchi N., Prabhakar M.C., Arora R.B.
    1973 Volume 23 Issue 5 Pages 673-679
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Musk (Kasturi), a dried prepucial secretion from male musk deer, has a wide range of activity in antagonizing the in vitro effects of-histamine, 5-hydroxytryptamine, bradykinin, prostaglandin, acetylcholine and the Schultz-Dale reaction on the guinea-pig ileum. Musk also diminished in rats, the increased capillary permeability induced by histamine and Russell's viper venom.
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  • Heitaroh IWATA, Kimio KARIYA, Yutaka WADA
    1973 Volume 23 Issue 5 Pages 681-688
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Growth of Tetrahymena in the exponential phase was slightly accelerated by transfer of cells to a medium containing 10-3-10-5 M adrenaline or noradrenaline, while that of stationary phase cells was inhibited by 10-3-10-7 M catecholamine. In synchronized cultures of Tetrahymena, adrenaline inhibited RNA and protein syntheses in both the late G1 and the G2 phases. These inhibitory effects in the late G1 and G2 phases result in an inhibition of the introduction of the S phase and of cytokinesis, respectively. These results indicate that an adrenergic mechanism in Tetrahymena plays a role in regulating the cell cycle.
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  • Toshio YOSHIZAKI
    1973 Volume 23 Issue 5 Pages 689-694
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Study on adrenaline release from the rat adrenal was performed by means of fluorometric determination of adrenaline in adrenal-venous blood specimens. The basal rate of adrenaline secretion under ether anesthesia was about 10 times that under pentobarbital anesthesia. Splanchnicotomy and spinal-transection prevented the secretion. Increase of adrenaline output was observed at doses of 0.125 to 0.5 mg/kg i.v. of nicotine under pentobarbital anesthesia, but under ether anesthesia increase of adrenaline secretion was not detected. Ether prevented the nicotine induced adrenaline release from splanchnicotomized rat adrenal, and this action was stronger than that of pentobarbital anesthesia. Morphine caused a marked adrenaline secretion under ether anesthesia and the action was dose responsive from 30 to 120 mg/kg i.p. as the hydrochloride salt. Splanchnicotomy largely prevented the increase of adrenaline release in response to morphine. These results provide a method for the study of drug effects on adrenaline release from rat adrenals.
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  • Toshio YOSHIZAKI
    1973 Volume 23 Issue 5 Pages 695-699
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Effects of histamine, bradykinin and morphine on adrenaline secretion from rat adrenal gland were investigated by means of fluorometric determination of adrenaline in adrenal-venous blood specimens. Histamine caused marked secretion of adrenaline at doses of more than 2.5 mg/kg i.v. The histamine-induced adrenaline secretion at a dose of 2.5 mg/kg was depleted to about one half by splanchnicotomy. Hexamethonium (C6) and atropine did not prevent histamine-induced adrenaline output. However, antihistaminics antagonized the action of this compound. Bradykinin caused increase of adrenaline secretion from the adrenal gland. Splanchnicotomy scarcely prevented the action of bradykinin. C6, phenylbutazone, and pyridinolcarbamate did not block the bradykinin-induced adrenaline output. Morphine caused significant increase of adrenaline secretion from the chronically and completely denervated adrenal gland.
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  • Hiroshi KANETO, Masao KOIDA, Hitoshi NAKANISHI, Hiroshi SASANO
    1973 Volume 23 Issue 5 Pages 701-707
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Mice were made physically dependent after 10 days morphinization and subjected to natural withdrawal. The spontaneously developing signs in behavior were classified depending on type and frequency and utilizing same a scoring system was developed. The scoring system permitted an approximate appraisal of the rise and fall of abstinence state up to 10 hr after the start of withdrawal. When the single suppression technique was applied, it thus became possible to generally estimate the dependence liability of a given drug and at the same time, to determine whether or not a drug could be substituted for an opiate thereby predicting the liability of morphine-type dependence.
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  • Hitoshi KATO, Shoshi SUZUKI, Kenichiro NAKAO, Eun B. LEE, Keijiro TAKA ...
    1973 Volume 23 Issue 5 Pages 709-716
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    The effects of crude platycodin on the coronary and hindquarter vascular beds in anesthetized dogs were studied and compared with those of glyceryl trinitrate, papaverine and Saponin (E. Merck AG.). Crude platycodin in doses of 200 to 800 μg i.a. dose-dependently reduced coronary and hindquarter vascular resistances and the potency was comparable to that of papaverine. Crude platycodin, 4 mg/kg i.v., also caused an increase in coronary and hindquarter blood flows, concomitantly with a transient systemic hypotension. The vasodilating effect of crude platycodin appears to be direct and non-specific on the peripheral blood vessels as in the case of glyceryl trinitrate or papaverine.
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  • Tadashi ISO
    1973 Volume 23 Issue 5 Pages 717-721
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Not only cyclic 3'. 5'-AMP but also related compounds containing adenosine moiety potentiated the contractile response of the isolated guinea-pig vas deferens to catecholamines, especially to dl-isoproterenol. The potentiating activity of cyclic 3', 5'-AMP was one-tenth that of adenosine or 5'-AMP. From these findings, it is suggested that not only adenosine moiety but also the steric conformation of adenine mononucleotides play an important role in potentiating the contractile response to catecholamines, and that the potentiation phenomenon occurs on the cell membrane. On the other hand, theophylline reduced the contractile response especially to dlisoproterenol and counteracted the potentiation phenomenon caused by cyclic 3', 5'AMP or adenosine. Possible mechanisms of action are discussed.
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  • Hiroshi AZUMA, Motohatsu FUJIWARA
    1973 Volume 23 Issue 5 Pages 723-732
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
    Transmural stimulation applied to the isolated sphincter of Oddi from rabbit caused a transient contraction. On termination of stimulation, a rapid second contraction was superimposed, then followed by a relaxation and inhibition of automaticity. Atropine inhibited the initial component during stimulation. The late second component was, however, little affected by atropine. On the other hand, the contractile response to exogenously applied acetylcholine was antagonized by atropine. All responses to transmural stimulation were completely abolished by tetrodotoxin 1.55×10-7 M. Both initial and late components of contractile response to transmural stimulation were significantly reduced in cold stored preparations depending on the period of storage, and under N2 gas-bubbling anoxia. The contractile response to exogenous acetylcholine, however, was not reduced under such conditions. Both initial and late components were unaffected by a ganglionic blocking agent and adrenergic alpha and beta blocking agents, alone or combined. Both components were significantly inhibited by pretreatment with hemicholinium-3, or noradrenaline, however, the response to exogenous acetylcholine was little affected by pretreatment with noradrenaline. The physostigmine-potentiated late component was reduced by atropine, whereas the late component was not potentiated by physostigmine in the presence of atropine. It is clear that the initial component is mediated through the release of acetylcholine from the intramural postganglionic cholinergic neurones. These results indicate that the late component may also be related to acetylcholine released from the same neurones.
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  • S.S. GAMBHIR, P.K. DAS
    1973 Volume 23 Issue 5 Pages 733-735
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • J.S. BAPNA, P.C. DANDTYA, S.K. KULKARNI
    1973 Volume 23 Issue 5 Pages 735-737
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • Issei TAKAYANAGI, Masaatsu UCHIDA, Tsuyoshi ABE, Akira TOMIYAMA, Keiji ...
    1973 Volume 23 Issue 5 Pages 737-739
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • Yoshimi MISU, Hiroaki NISHIO
    1973 Volume 23 Issue 5 Pages 740-742
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • Seiichi NURIMOTO, Goro HAYASHI
    1973 Volume 23 Issue 5 Pages 742-745
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • Akira TAKANAKA, Kin-ichi ONODA, Eiko KAINUMA, Francois LIENARD, Yoshih ...
    1973 Volume 23 Issue 5 Pages 745-747
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • Toshihiro DOHI, Sekizo KOJIMA, Akira TSUJIMOTO
    1973 Volume 23 Issue 5 Pages 748-751
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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  • Heitaroh IWATA, Kimio KARIYA
    1973 Volume 23 Issue 5 Pages 751-752
    Published: 1973
    Released: December 19, 2006
    JOURNALS FREE ACCESS
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