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Volume 22, Issue 1
Displaying 1-16 of 16 articles from this issue
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II. VASODILATOR ACTIONSTaku NAGAO, Masanori SATO, Hiromichi NAKAJIMA, Akio KIYOMOTO1972 Volume 22 Issue 1 Pages 1-10
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIn a previous report (1), it was shown that a new 1, 5-benzothiazepine derivative, 3-acetoxy-2, 3-dihydro-5-[2-(diethylamino) ethyl]-2-(p-methoxyphenyl)-1, 5-benzothiazepine-4 (5H)-one hydrochloride, produced a potent coronary vasodilator effect in anesthetized dogs. Among four stereoisomers of the compound, d- and l-isomers of cis- and transforms, the d-cis-isomer (CRD-401) exhibited the most powerful effect when injected into the femoral vein. Without increase in myocardial oxygen consumption, a significant increase in coronary blood flow resulted.
The present report deals with the vasodilator action of d-cis-isomer of the new benzothiazepine derivative under the influence of various pharmacological blockers. The results are considered in relation to the mechanism of the compound. Effects of dl- and l-cis-isomers and dl-trans-isomer were also investigated and compared with the action of d-cis-isomer. Experiments were performed on the coronary and femoral arteries in anesthetized dogs and on the coronary vessels in isolated hearts of the guinea pig.View full abstractDownload PDF (329K) -
S.K. KULKARNI, P.C. DANDIYA, N.L. VARANDANI1972 Volume 22 Issue 1 Pages 11-16
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe alkaloid, berberine, isolated from Berberis aristata Linn has been used in the Indian system of medicine as a stomachic, bitter tonic and also in the treatment of oriental sores. The root bark and its decoctions were thought be an excellent remedy against malaria and were used as a diaphoretic and antipyretic in the past (1). It was reported to possess bacteriostatic activity especially against V. Cholera and was found to be useful in the treatment of cholera and diarrhoea (2). Recently, it has been claimed that berberine and its salts have a place in the chemotherapy of amoebiasis (3-4). The present work is devoted to the study of the antiamoebic properties of this drug on experimentally induced amoebiasis in rats, the minimum inhibitory concentration and other relevent pharmacological effects on experimental animals and animal tissues.View full abstractDownload PDF (235K) -
Keijiro TAKAGI, Hiroshi SAITO, Chi-Ho LEE, Tomiko HAYASHI1972 Volume 22 Issue 1 Pages 17-26
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSConsiderable investigation has been done as to whether or not a particular drug is effective for recovery of an animal after it has become exhausted. Experiments have included screening antifatigue effect on animals, but applications have not been generally established. Effects of drugs on psychological fatigue as seen in man can hardly be inferred from tests on animals. Even physiological effects of some stimulants differ, depending on the cause of exhaustion (1). There is reason to believe that enforced exercise involves stress not present in spontaneous exercise (2). As psychological and physiological factors as yet remain obscure, fatigue itself is hard to define. The present paper reports attempts to determine simple pharmacological methods for screening effects of drugs on exhausted states of animals.View full abstractDownload PDF (339K) -
Kiyomi SAEKI, Koiti ENDO, Hidemasa YAMASAKI1972 Volume 22 Issue 1 Pages 27-32
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSMost of the histamine in mast cells is known to be stored in specific granules (1-3), but as for the mode by which histamine is bound within the granules, opinions are not in harmony. Thus, a hypothesis has been proposed that histamine is bound electrostatically to anionic sites of the heparin-protein complex of the granule constituents from which histamine is easily released by ionic exchange when the isolated granules are exposed to cations in the medium (4-7). However, many classical experiments have indicated that histamine in mast cell granules is not so susceptible to the releasing action of inorganic cations of the outer milieus (8-12). A possible reason for the discrepancy may be changes in the properties of mast cell granules during the isolation procedures. In the present paper, this assumption has been supported by the observation that there are considerable differences in the histamine release by inorganic cations from mast cell granules depending on the method of granule isolation.View full abstractDownload PDF (233K) -
Keijiro TAKAGI, Issei TAKAYANAGI1972 Volume 22 Issue 1 Pages 33-36
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSRecently, 3', 5'-cyclic adenosine monophosphate (3', 5'-cyclic AMP) is being discussed as the second messenger in the beta-adrenergic action (1) and adenosine triphosphate (ATP) as the inhibitory transmitter of the unknown nerves in the stomach (2). To date, these actions on the cholinergic nerves in the ileum are not yet clear. The objective of this paper is to examine the actions of 3', 5'-cyclic AMP, its dibutyryl derivative or N6, 2'-O-dibutyryl-3', 5'-cyclic adenosine monophosphate (dibutyryl cyclic AMP) and ATP on the cholinergic nerves in the guinea pig ileum.View full abstractDownload PDF (156K) -
I. PRESENCE OF 5-HYDROXYTRYPTAMINE RELEASING FACTOR IN RABBIT PLASMA AND ITS INTERACTION WITH HEPARIN AND ENDOTOXINYasuyuki NOMURA, Hiroshi TAKAGI1972 Volume 22 Issue 1 Pages 37-42
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIt has been well established that the 5-hydroxytryptamine (5HT) release from blood platelets by bacterial endotoxin (lipopolysaccharide; LPS) requires the presence of calcium ion and plasma protein in the medium, and that heparin inhibits this release (1-5). The chemical natune of the plasma factor has not yet, however, been elucidated, hence it is the objective of this study.View full abstractDownload PDF (218K) -
Norio KURIHARA, Sakutaro TADOKORO, Haruyoshi OGAWA1972 Volume 22 Issue 1 Pages 43-58
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSRecent global trends of population increase has turned attention to hormonal control of ovulation as an effective contraceptive. Consequently, oral contraceptives have been studied and are generally utilized in the North America and Europe. These are used in a combination of progestogens and estrogens, in either a combination or sequential method. A near perfect contraceptive result is effected, however, carelessness or misuse often results in failure (1).
It has been reported that acetophenone derivatives of 16α, 17α-dihydroxyprogesterone show long-lasting potent progestational activity (2-4). In view of this, attempts have been made to produce a contraceptive effect via a monthly intramuscular injection of the steroid which has been dissolved in vegetable oil. In this administration a certain prolonged concentration of the steroid is maintained in the blood, subsequently, the question is raised as to endocrinological side effects of the steroid or toxicities. The objective of the present work is to determine in rats, hormonal action of a mixture of dihydroxyprogesterone acetophenide and estradiol enanthate, one of the test preparations of parental contraceptive, developed by Squibb Institute for Medical Research.View full abstractDownload PDF (826K) -
Noboru TODA, Hachiro USUI, Jyo MORI1972 Volume 22 Issue 1 Pages 59-69
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSTransmural electrical stimulation with repetitive pulses of short duration causes contraction of isolated vascular smooth muscles, which is suggested to correlate with excitation of adrenergic nerve terminals innervating the vascular wall (1, 2). This is supported by findings which indicated that field stimulation causes contraction and an increased efflux of 3H-noradrenaline from rabbit main pulmonary arteries (3) and that a biologically active (gutrelaxing) substance is released from stimulated rabbit ear arteries (4). Tyramine releases noradrenaline from the stored site that is not accessible to nerve impulses (5). Excitatory responses of the vascular smooth muscle to electrical and chemical stimulation are thought to relate directly to functional noradrenaline involved in the different pools of nerve terminals.
The aim of the present study was to examine contractile responses of ascending and thoracic aortae and the main pulmonary and superior mesenteric arteries to transmural stimulation, tyramine and dopamine, in comparison with noradrenaline. Since arterial strips have a capacity to accumulate and retain noradrenaline when applied exogenously at high concentrations (6, 7), the contractile response to the electrical and chemical stimulation was also investigated in arterial strips after exposure to noradrenaline or dopamine.View full abstractDownload PDF (441K) -
II. PURIFICATION OF 5-HYDROXYTRYPTAMINE RELEASING FACTOR FROM RABBIT PLASMAYasuyuki NOMURA, Hiroshi TAKAGI1972 Volume 22 Issue 1 Pages 71-77
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSPrevious studies have demonstrated that 5-hydroxytryptamine (5HT) released from blood platelets by bacterial endotoxin (lipopolysaccharide; LPS) requires the presence of calcium ion and plasma factor and that heparin inhibits its release (1-5). Recently, Nomura and Takagi (6) have separated the 5HT releasing factor from rabbit plasma by gel filtration on a Sephadex G-150 column. They have suggested that the plasma factor with 5HT releasing activity is a protein with a molecular wt. of approx. 110, 000 and that 5HT release induced by LPS could be mediated through antagonism by LPS to the inhibitory effect of heparin on the 5HT releasing plasma factor, and also that activity of the 5HT releasing factor in plasma could be regulated by heparin and the anti-5HT releasing factor existing in the albumin fraction.
The present report describes studies on the further purification of the 5HT releasing factor in rabbit plasma and its properties.View full abstractDownload PDF (259K) -
III. MECHANISM OF ACTION OF 5-HYDROXYTRYPTAMINE RELEASING FACTORYasuyuki NOMURA, Toshikazu OKADA, Hiroshi TAKAGI1972 Volume 22 Issue 1 Pages 79-87
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIt has been well established that 5-hydroxytryptamine (5HT) release from blood platelets by bacterial endotoxin (lipopolysaccharide, LPS) requires the presence of plasma factor and calcium ion (1-4). Recently, separation and purification of plasma factor with 5HT releasing activity has been reported by Nomura and Takagi (5, 6). They estimated that this factor could be mainly prothrombin-like protein, however, the mechanism of 5HT release by this factor is unknown. Thrombin has been considered an enzyme with 5HT releasing activity from the blood platelets and mechanism of its action was studied by Gainter et al. (7), Pletscher et al. (8) and Markwardt et al. (9-11).
The purpose of the present experiment is to investigate the mechanism of action of 5HT releasing factor purified using a previous method (6), as well as making a comparison with thrombin.View full abstractDownload PDF (482K) -
Kenji TASAKA, Koiti ENDO, Hidemasa YAMASAKI1972 Volume 22 Issue 1 Pages 89-95
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSSeveral observations (1-5) have suggested that an antigen-antibody combination takes place on the mast cell surface this triggering the cellular processes leading to histamine release and morphological changes in the mast cells. It is as yet unknown whether or not intracellular antigen-antibody-induced histamine release can be precluded, in any type of immunologic reaction in mast cells. Even though an antigen-antibody combination takes place on the mast cell surface, a question arises as to whether the reaction occurs over the whole cell membrane in all-or-none fashion or at a limited portion where antigen is applied locally. Recent findings (6-9) indicate that both degranulation and histamine release from a single rat mast cell can be provoked locally on the cell surface at the site of topical application of chemical histamine releasers by means of microelectrophoresis, while these reactions are not induced by their intracellular applications (6, 7, 9).
The present experiments were undertaken to see whether antigen-antibody reaction in mast cell is a local reaction or a kind of integral reaction spreading over the whole cell, and also to determine whether the site of the reaction is inside or outside of the mast cell, using two types of antigen-antibody reaction: 1) applying antigen to the mast cell of an actively sensitized rat, or to the mast cell sensitized passively in vitro with homologous antibody, and 2) applying a rabbit anti-rat serum to the non-sensitized mast cell. Antigen and antiserum were applied by means of microelectrophoresis, topically or diffusely on the cell surface or intracellularly, to a single rat mesentery mast cell.View full abstractDownload PDF (604K) -
Hideya SAITO, Isami SHUDO1972 Volume 22 Issue 1 Pages 97-102
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSProtokylol, a sympathomimetic drug has been utilized in general clinical practice as a bronchodilator in recent years. To date no reports concerning the actual drug metabolism are available. As a result of our present research, it was found that protokylol in a manner similar to catecholamine, changes into a substance with a high fluorescence intensity by trihydroxyindole reaction. Using this method it has become possible to measure minute amounts of protokylol (1-3).
The present paper outlines a time course observation on protokylol distribution in rats following an intravenous injection of protokylol.View full abstractDownload PDF (223K) -
Katsuya IWATSUBO, Iwao YAMAMOTO, Takeshi ODANAKA1972 Volume 22 Issue 1 Pages 103-113
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIt has been shown that there was a marked increase in the incorporation of 32P into the phospholipid fraction when secretion of amines from the adrenal medulla (1, 2), enzyme from pancreas (3, 4) or the salivary gland (5, 6) and other substances from respective glands (7) were stimulated with cholinergic agents. From these striking phospholipid effects, it has been considered that phospholipids may play a role in the active secretion of proteins by exocrine glands and of amines by the adrenal medulla (7).
However, as to the time courses of acetylcholine-stimulated 32P incorporation into phospholipids of the adrenal medulla, and of acetylcholine-evoked amine release, it was observed that amine release reached a maximum after 10 min; in contrast 32P incorporation into phospholipids became apparent only after this interval of time (2). Furthermore, calcium ion had little influence on stimulating phospholipid effects of acetylcholine in the adrenal medulla (8) or pancreas slices (4), while their secretions in response to acetylcholine were completely inhibited by omission of calcium. Another possible role of the increased phospholipid metabolism might be involved in a post-process of chromafiin cells after the stimulated secretion.
The present work represents efforts to trace the role of phospholipid metabolism of the adrenal medulla in reference to the possible “recovery process” of the tissue after the stimulated secretion.View full abstractDownload PDF (489K) -
Masahiro MIZUTANI, Toshio IHARA, Kyo KAZIWARA1972 Volume 22 Issue 1 Pages 115-124
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIn vitro studies with thiamine tetrahydrofurfuryl disulfide (TTFD) revealed that treatment of the fertilized sea urchin ova produced arrest of cellular division at the metaphase stage (1). It was postulated that this was probably due to interference with interconversion of thiol disulfide responsible for the mitotic mechanism (1, 2). The depressant effect of TTFD on cellular proliferation has also been demonstrated in primary monolayer culture of chick heart cells, hamster and monkey kidney cells (3) and amnion (4) and kidney cells of the human embryo (5).
It has also been shown that in experimental animals (rats and rabbits) there is a more marked accumulation of TTFD in circulating erythrocytes and tissue cells than thiamine (6) and that, in pregnant mice, TTFD•HCl crosses the placental barrier into the foetus (7).
Despite the possible implications of these findings to embryonic development, daily oral administration of TTFD•HCl at 30 and 300 mg/kg (equivalent to 5 to 10 and 50 to 100 times the maximum human therapeutic dosage) to pregnant CF-1 mice and SD rats during the critical stages of organ differentiation failed to produce any significant developmental abnormality (8).
The present report deals with subsequent teratological studies of TTFD•HCl, performed in the rabbit and in the cynomolgus monkey.View full abstractDownload PDF (389K) -
Noboru TODA, Hachiro USUI, Kiro SHIMAMOTO1972 Volume 22 Issue 1 Pages 125-135
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSA new antihypertensive drug (1), 1-cyclohexyl-3-guanidinoazetidine sulfate (AZ-55), structurally resembles guanethidine. It is widely known that guanethidine depresses peripheral adrenergic nerve function by preventing release of adrenergic nerve transmitters (reviewed by Boura and Green, 2). Bretylium also possesses the adrenergic neuron blocking action, but accumulated data point to the fact that bretylium and guanethidine fail to share all mechanisms of the blocking action (2).
The present study was aimed to investigate the effects of AZ-55 on responses of S-A nodes of the heart and of aortic smooth muscles to transmural neural stimulation, tyramine and noradrenaline. Effects were then compared with those of guanethidine and bretylium.View full abstractDownload PDF (402K) -
Mitsuo SAKATO, Yasuo SHIMO, Takeo BANDO1972 Volume 22 Issue 1 Pages 137-138
Published: 1972
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (91K)
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