All issues
Successor
Volume 27 (1977)
- Issue 6 Pages 755-
- Issue 5 Pages 601-
- Issue 4 Pages 481-
- Issue 3 Pages 333-
- Issue 2 Pages 183-
- Issue 1 Pages 1-
Volume 27, Issue 6
Displaying 1-21 of 21 articles from this issue
- |<
- <
- 1
- >
- >|
-
Ryoichi ISHITANI, Takio IWAMOTO1977 Volume 27 Issue 6 Pages 755-762
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSAfter administration of H3-imipramine, H3-dimetacrine and S35-chlorpromazine by the direct lateral intraventricular injection, synaptosomes-rich fraction (F-B) was isolated from rat cerebral cortex by differential and 3-stepwise density gradient centrifugation. The isolated F-B fraction was treated by hyposmotic-lysis followed by freezing and thawing once or 15 times and, furthermore, fractionated into the subsynaptosomal fractions by 5-stepwise density gradient centrifugation. The subsynaptosomal distribution of these drugs showed the same distribution patterns, i.e., the larger portion of radioactivity was recovered in the synaptic ghost membranes-rich fractions. On the other hand, synaptic vesicles-rich fractions contained less radioactivity. On the disrupting process of F-B fraction, when the F-B fraction was treated by hyposmotic-lysis followed by freezing and thawing 15 times, only pellet (FD-6) fraction was obtained as compared with freezing and thawing once (4 interphase layers were obtained). Morphological examination revealed that the synaptic ghost membranes were located in the FD-6 fraction, but morphological damages were not observed. Under these conditions, H3-imipramine showed a 74.1% of release from the synaptosomes, while release with H3-dimetacrine and S35-chlorpromazine was 3.9 and 11.3% respectively.View full abstractDownload PDF (388K) -
Takahiro FUTAMI1977 Volume 27 Issue 6 Pages 763-767
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSAlkyldimethylbenzylammonium chloride (alkyl-DBAC), a cationic surfactant, produces acute exudative inflammation accompanied by an enhancement of energy metabolism. The mechanism of metabolic changes, consequently the cyclic AMP level and the effects of certain drugs were determined in the gastrocnemius muscles of rats in which acute exudative inflammation had been induced by intramuscular injections of alkyl-DBAC. A transient increase in the cyclic AMP level was noted at 15 to 30 minutes after the injection of alkyl-DBAC, and this elevation was antagonized by chlorpromazine, diphenhydramine, promethazine, aspirin and indomethacin. The time course of increasing tendency in the cyclic AMP level after the injection of histamine closely paralleled that of alkyl-DBAC. These results suggest that cyclic AMP may be involved in the metabolic changes with inflammation induced by alkyl-DBAC.View full abstractDownload PDF (217K) -
Lester ZITOWITZ, John STIMSON, Arnold J. WOHL, Stewart J. EHRREICH1977 Volume 27 Issue 6 Pages 769-779
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSAntianginal drugs were evaluated on the basis of their ability to protect against subepicardial electrogram changes induced by local ventricular ischemia in anesthetized dogs. Sch 11973 [N-(2-phenylisopropyl)-N-p-toluene sulfonyl urea], a potential new antianginal agent, was also effective against local ventricular ischemia with its maximum effect appearing at 1 mg/kg, i.v. or i.d. and with a duration of at least 2 hours. Nitroglycerin, at a dose of 0.04 mg/kg given bucally, exerted less protection, lasting on the average less than 15 minutes. Protection by propranolol at 1 mg/kg, i.v., was not better than nitroglycerin, but lasted up to one hour, while dipyridamole was ineffective when given in a dose range of 0.1-10 mg/kg, i.v. Sch 11973 differed from standard antianginal agents which may act via beta-adrenergic blocking activity or alteration of cardiac or circulatory dynamics since no acute pharmacological changes were observed after Sch 11973 was administered.View full abstractDownload PDF (468K) -
Masaatsu UCHIDA1977 Volume 27 Issue 6 Pages 781-789
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSStudies were done on the specific labeling of the histaminergic H1-receptor of the longitudinal smooth muscle of cat small intestine. A procedure involving ‘double protection’ combined with the double labeling technique was developed. The first protection was the usual with a protective antihistamine, promethazine, and the second was cross protection of non-specific sites with non-hitaminergic drugs, thioriazine and atropine. Muscle tissue protected with promethazine against non-radioactive dibenamine was treated with 3H-dibenamine in the presence of these second protectors. The second protectors covered non-receptor sites which had been protected from non-radioactive dibenamine with promethazine. The dose-response curves were carefully checked in each experiment to confirm that the second protectors did not interfere with the specific coverage provided by the first protector. Finally 14C-dibenamine was applied to measure non-specific binding after which the labeled muscles were fractionated and the radioactivity was counted. The specificity of labeling achieved in the receptor-rich fraction by this method is discussed.View full abstractDownload PDF (457K) -
Yoshikazu YAMATAKE, Sumiko SASAGAWA, Saizo YANAURA, Noboru KOBAYASHI1977 Volume 27 Issue 6 Pages 791-797
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSParticipation of histamine H1- and H2-receptors in both asthmas, i.e. experimentally induced bronchoconstriction and bronchosecretion, with ascaris suum and histamine in anesthetized dogs was investigated. Dogs given 0.2% histamine solution or ascaris antigen (3 mg protein) by inhalation showed increases in respiratory resistance (Rrs) and respiratory rate to 2.5-5.0 fold. Airway secretion volume was also significantly increased 3-4 fold. The increase in Rrs by histamine inhalation was effectively inhibited or abolished by a histamine H1-receptor antagonist, chlorpheniramine (0.3-1 mg/kg i.v.), but not by a H2-receptor antagonist, cimetidine (1-3 mg/kg i.v.). The increase in Rrs by antigen inhalation was reduced by relatively high doses of chlorpheniramine (1-3 mg/kg i.v.), and not by cimetidine. In contrast, hypersecretion of tracheobronchial fluid in both asthmas was significantly prevented by either chlorpheniramine or cimetidine. Combinations of both antagonists abolished the hypersecretion. Atropine (2 mg/kg i.v.) significantly inhibited the occurrence of responses in both asthmas. The results suggest that histamine is involved in the allergic asthma produced by ascaris suum and that histamine directly evokes airway constriction through H1-receptors and hypersecretion of tracheobronchial fluid through H1 and H2-receptors, and, in a part, indirectly activates the cholinergic pathway.View full abstractDownload PDF (293K) -
Hiromichi TSURU, Naohisa ISHIKAWA, Tatsuro SHIGEI, Takako ANJYO, Masas ...1977 Volume 27 Issue 6 Pages 799-805
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSCardiotonic activities of six newly synthesized ring A-modified cardenolides, four 3, 5-seco-4-nor-cardenolides and two 4-oxa-cardenolides, were studied in isolated frog hearts and guinea pig atria. These compounds were 14-hydroxy-3, 5-seco-4-nor-5-oxo-l4β-card-20(22)-enolid-3-oic acid (IIa), and its methyl ester (IIb); 5β, 14 and 5α, 14-dihydroxy-3, 5-seco-4-nor-14β, -card-20(22)-enolid-3-ols (IIIa and IIIb); 3-dehydro-4-oxa-uzarigenin (IVa) and 3-dehydro-4-oxa-digitoxigenin (1Vb). In the frog heart (Straub's preparation), positive inotropic effects were demonstrated with all compounds except IIa. The pattern of response was the same as that to digitoxigenin (I). The relative potencies obtained on the basis of the concentration of each compound in which a contracture was brought about, the potency of I being taken as standard, were as follows: I (1.0), IIa (-), IIb (0.03-0.1), IIIa (0.01), IIIb (<0.01), IVa (<0.01), and IVb (0.03-0.1). The positive isotropic effect of IIb was also confirmed in guinea pig atria. IIb and IVb potentiated dose-dependently the K-contracture of the frog ventricular muscle just as was seen with I, indicating that the cardiotonic activity of the compounds is the same in nature as that of digitoxigenin. It was clearly demonstrated that the perhydrocyclopentanophenanthrene nucleus is not an indispensable requirement for cardiotonic activity.View full abstractDownload PDF (288K) -
Makoto OKA, Chiaki KAMEI, Masanao SHIMIZU1977 Volume 27 Issue 6 Pages 807-815
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSEffects of psychotropic drugs on the conditioned behavior after pretreatment with α-methyltyrosine(α-MT) or p-chlorophenylalanine(PCPA) were studied using operant conditioning technique in rodents. The operant conditioning procedure used was composed of a concurrent milk-reinforced and avoidance schedule in an operant conditioning chamber with two levers where lever pressing by rats was maintained by milk (VR 6) and electric shock (intertrial interval 1 min). Chlorpromazine (1 mg/kg i.p.), perphenazine (0.1 mg/kg i.p.), haloperidol (0.05 mg/kg i.p.) and oxypertine (0.25 mg/kg i.p.), at half of the maximum ineffective dose, respectively, caused a significant decrease in both lever pressings after pretreatment with α-MT (20 mg/kg i.p.). Such potentiating effect by α-MT was not observed with diazepam and nortriptyline. PCPA pretreatment (300 mg/kg i.p.) did not influence suppressive effects on responding under both schedules by any drug used. The one-way active avoidance procedure in mice was also employed in this study. On the avoidance response, chlorpromazine, perphenazine, haloperidol, trifluperidol, clozapine and oxypertine showed a suppressive effect, ED50 values of which were considerably lowered by pretreatment with α-MT (25 mg/kg i.p.). No influence was seen with PCPA (200 mg/kg i.p. × 2). Diazepam, phenoxybenzamine, phentolarnine, arecoline, physostigmine and clonidine also had a suppressive effect on the avoidance response, which was not influenced by pretreatment with α-MT. These results suggest that the suppressive effect of neuroleptics on the conditioned behavior is selectively potentiated by α-MT, and not influenced by PCPA.View full abstractDownload PDF (394K) -
Akira KIZU, Taizo NAKAMURA, Syuji KATO, Katsunori SAWADA, Hamao IJICHI ...1977 Volume 27 Issue 6 Pages 817-821
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe major part of orally administered β-pyridylcarbinol was converted to nicotinic acid in the gastrointestinal tract, whereas that administered intraperitoneally was partially converted to nicotinic acid in the liver. The conversion of this compound to nicotinic acid in both the gastrointestinal tract and liver involved enzymatic processes. The converted nicotinic acid from β-pyridylcarbinol may play a dominant role in the biological actions of β-pyridylcarbinol and possibly involves in the synthesis of NAD via Preiss-Handler's pathway.View full abstractDownload PDF (193K) -
Tsugutaka ITO, Misako HORI, Kouichi YOSHIDA, Masanao SHIMIZU1977 Volume 27 Issue 6 Pages 823-831
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSEffects of anticonvulsants were determined on thalamic afterdischarge in gallamine-immobilized cats and d-tubocurarine-immobilized rats in order to clarify the participation of anticonvulsants in the thalamus. Thalamic afterdischarge was induced by electrical stimulation of cat nucleus centralis lateralis and rat nucleus reticularis at 50 Hz, 1 msec for 4 sec. In cats, diphenylhydantoin, carbamazepine, phenobarbital, and diazepam raised afterdischarge threshold, and shortened its duration induced at twice the threshold voltage. Trimethadione and dipropylacetate raised the threshold, but did not change the duration. In rats, diphenylhydantoin, phenobarbital, and diazepam raised the threshold, and shortened the duration with comparable dose ranges used for cats. Dipropylacetate and acetazolamide raised the threshold, although did not change the duration except for shortening action with a higher dose of dipropylacetate. Trimethadione was without effect. These results suggest that the depressive effect of anticonvulsants on the thalamus is, at least in part, associated with control of the epilepsies.View full abstractDownload PDF (370K) -
Shoji TSUDA, Norimoto URAKAWA, Yukio SAITO1977 Volume 27 Issue 6 Pages 833-843
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSPapaverine (Pap) inhibited a tonic tension development in guinea pig taenia coli induced by an elevation of the potassium concentration of the medium to 40 mM (40-K). The ID50 of Pap was 4.5 × 10-6 M. Inhibition of the 40-K induced tonic tension by Pap was dependent on the calculated concentration of non-ionized form, but not the ionized form. Inhibition of the tonic tension by Pap and various metabolic inhibitors was not antagonized by raising the Ca++ concentration in the medium. Results obtained from simultaneous measurement of the 40-K induced O2 consumption and tension illustrated that the inhibition of O2 consumption rapidly induced the inhibition of the tension. Furthermore, glucose removal, amytal or Pap resulted in a progressive relationship between the inhibition of O2 consumption and the inhibition of tension. The inhibition of Pap as determined by O2 consumption was not reversed by application of 10-4 M 2, 4-dinitrophenol (DNP). These results plus graphical analysis of the mechanical response suggest that Pap may penetrate the cell membrane and inhibit mitochondrial respiration, thereby inhibiting this very respiration-dependent contracture.View full abstractDownload PDF (464K) -
Shuji TSUDA, Norimoto URAKAWA, Jun-ich FUKAMI1977 Volume 27 Issue 6 Pages 845-853
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSTo elucidate the inhibitory action of papaverine (Pap) on the highly respiration-dependent contracture of guinea pig taenia coli in 40 mM potassium (40-K) medium, the effects of Pap and rotenone (Rot) on the respiration of mitochondria (Mt) were examined using guinea pig taenia coli, rat liver and pigeon heart. The addition of Pap to taenia coli Mt at a concentration which inhibits the muscle contracture rapidly inhibited the aerobic oxidation of glutamate but not succinate. A peak of cytochrome (cyt) bγ was not observed in the Mt which were treated with Pap and contained glutamate. These results were confirmed and extended to rat liver Mt. Both the taenia coli kit and the heart Mt oxidized NADH when added as a substrate. Pap (10-5-10-4 M) inhibited the oxidation of NADH by both Mt to almost the same degree as it inhibited the respiration of the muscle strip in 40-K medium. Raising the NADH concentration did not antagonize inhibition by Pap. NADH-ferricyanide reaction in both Mt occurred essentially as reported in the electron transport particle of heart. Mt. The reduction of ferricyanide was scarcely inhibited by Pap. The effects of Pap and Rot were identical throughout the experiment. It is suggested that Pap inhibits the electron transport of the mitochondrial respiratory chain between NADH dehydrogenase and coenzyme Q10 (CoQ) on the O2 side of the dehydrogenase, thereby inhibiting the contracture.View full abstractDownload PDF (412K) -
Shuji TSUDA, Norimoto URAKAWA, Jun-ichi FUKAMI1977 Volume 27 Issue 6 Pages 855-863
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe differential effects of papaverine (Pap) and rotenone (Rot) were studied on the highly respiration-dependent contracture of guinea pig taenia coli in 40 mM potassium (40-K) medium, on isolated DT diaphorase activity and on mitochondrial respiration. The inhibition of guinea pig taenia coli to the 40-K induced tension by Rot (5 × 10-7 M) was fully reversed by the addition of a water soluble vitamin K3 (VK3) derivative or menadione sodium bisulfite (MSB). A low concentration (10-7-10-6 M) of Pap which had no effect on the 40-K induced tension inhibited the VK3 restored tension from the Rot suppression, corresponding to a Pap inhibition of the isolated DT diaphorase. Inhibition of the effective concentration of Pap to the 40-K induced tension development was never reversed by addition of VK3 or MSB. In taenia coli, both MSB and VK3 established a bypass of the Rot sensitive site on the mitochondrial respiratory chain by means of the DT diaphorase system. The difference in washoutefficacy between Pap and Rot on the inhibition of 40-K induced tension was ascribed to a difference in their mitochondrial binding properties.View full abstractDownload PDF (334K) -
Takashi BAN1977 Volume 27 Issue 6 Pages 865-880
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIn isolated guinea pig papillary muscles driven at 1 Hz, propranolol in the concentrations of 10-6, 2 × l0-6 and 5 × 10-6 g/ml and N-propylajmaline (NAP) in the concentrations of 2 × 10-7, 5 × 10-7 and 10-6 g/ml both depressed dose-dependently the maximum rate of rise of action potential (Vmax) without affecting resting potential. With a rise in driving frequency from 0.25 to 5 Hz, Vmax was reduced progressively both in propranolol and NPA-treated preparations but such was slight in the control. Comparison of effects of both drugs in a concentration which exerted a similar extent of depression of Vmax at 1 Hz revealed that propranolol usually exerted less depression at lower frequencies and a greater depression at higher frequencies than NPA. Vmax depressed under the influence of propranolol was recovered toward the pre-drug level in the first response after a pause in stimulation with rate constants of 0.081 to 0.116 sec-1. A kinetic model was constructed on the basis of assumption that drug molecules were taken up to the site where they affect the sodium carrying system at the very beginining of excitation and were released during diastolic intervals with the rate constant of the recovery. Two modifications of the model are presented to elucidate the effects of both drugs.View full abstractDownload PDF (687K) -
Yukio YONEDA, Sumie TAKASHIMA, Kazuo HIRAI, Etsuo KURIHARA, Yoshinao Y ...1977 Volume 27 Issue 6 Pages 881-888
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSMicroassay methods for taurine (2-aminoethanesulfonic acid) and cysteine sulfinate decarboxylase (CSD : EC 4.1.1.29) have been developed. Cation exchange resin (Dowex 50W × 8. 200-400 mesh) was used for the separation of taurine from other fluorescamine reactive substances. The “taurine fraction” in this column chromatographic procedure was collected and fluorescence development was carried out. The maximal sensitivity obtained for taurine was 25 pmoles. The specificity, reproducibility, sensitivity and recovery for taurine obtained by this method were satisfactory enough to be used for biological applications. The activity of CSD was determined by measuring the formation of 14C02 from DL-[l-14C]-cysteine sulfinic acid using a specially designed micro-vessel. The activity in cerebral tissues containing 5 μg of protein was accurately detected by this microradiometrical method. Using above microassay methods for taurine and CSD activity, it was found that in the rat spinal cord, taurine is distributed rather evenly, whereas the distribution of CSD activities is uneven and the highest activity is localized at the dorsal part of the dorsal horn.View full abstractDownload PDF (345K) -
Takaharu ONO, Minoru OHTSUKA, Shigeru SAKAI, Syuzo OHNO, Shigenobu KUM ...1977 Volume 27 Issue 6 Pages 889-898
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe interrelation of the inhibitory effect of aspirin-like drugs on the resting tones of tracheal chain in guinea pigs, arachidonic acid-induced contraction in rat stomach fundus strips and bradykinin-induced broncheconstriction in guinea pigs in vivo was investigated. Alt the drugs tested produced a dose-related inhibitory action on the resting tonus of the tracheal chain in comparatively low doses. Diclofenac was the most potent of all the drugs and was equal in activity to isoproterenol, followed in descending order by flufenamic acid, mefenamic acid, indomethacin, ibuprofen, phenylbutazone, oxyphenbutazone and aspirin. These aspirin-like drugs also inhibited arachidonic acid-induced contraction in rat stomach fundus strips. A highly significant correlation was observed between the potency of inhibition of the arachidonic acidinduced contraction and the relaxant effect on the tracheal chain. Moreover, the drugs antagonized bradykinin-induced bronchoconstriction in guinea pigs in vivo and the order of potency roughly paralleled that of the tracheal chain. These results suggest that the aspirin-like drugs produce a reduction in resting tones of the isolated guinea pig tracheal chain by inhibition of intramural biosynthesis of prostaglandin endoperoxides.View full abstractDownload PDF (422K) -
Soichi YOSHIDA, Tetsuro KUGA1977 Volume 27 Issue 6 Pages 899-902
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (182K) -
Katsuya IWATSUBO1977 Volume 27 Issue 6 Pages 903-905
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (144K) -
Mitsutaka NAKAMURA, Hideaki FUKUSHIMA1977 Volume 27 Issue 6 Pages 905-908
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (196K) -
Kazushige SAKAI, Michitaka AKIMA1977 Volume 27 Issue 6 Pages 908-910
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (127K) -
Hiromichi NAKAJIMA, Kunio NOSAKA, Masao HOSHIYAMA1977 Volume 27 Issue 6 Pages 910-914
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (239K) -
Tadashi FUJITA1977 Volume 27 Issue 6 Pages 914-916
Published: 1977
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (143K)
- |<
- <
- 1
- >
- >|