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Volume 26 (1976)
- Issue 6 Pages 639-
- Issue 5 Pages 519-
- Issue 4 Pages 395-
- Issue 3 Pages 281-
- Issue 2 Pages 133-
- Issue 1 Pages 1-
Volume 26, Issue 5
Displaying 1-17 of 17 articles from this issue
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Masashi SASA, Katsunori MUNEKIYO, Seishi IGARASHI, Shuji TAKAORI1976 Volume 26 Issue 5 Pages 519-525
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSEffects of α- and β-adrenergic blocking agents applied into the lateral ventricle were studied on the relay neuron in the rostral part of spinal trigeminal nucleus (STN) of cats. Conditioning stimulation of the locus coeruleus (LC) and sensory cortex (SC) inhibited the orthodromic spike generation in STN relay neuron without affecting the antidromic spike, as already reported, and re-confirmed herein. The LC-induced inhibition of orthodromic spike was significantly reduced by intraventricular administration of β-blockers, MJ 1999 (5 mg) and propranolol (0.5 mg), while the SC-induced inhibition of orthodromic one was not modified by the β-blockers. The antidromic spike in STN relay neuron per se remained unaffected by these treatments. Intraventricular administration of α-blockers such as phentolamine and phenoxybenzamine produced no alterations of the LC- and SC-induced inhibition of orthodromic spike. As the β-blockers produced a selective antagonism, noradrenaline originating in LC probably acts as an inhibitory transmitter on the STN relay neuron and is mediated by β-receptor.View full abstractDownload PDF (265K) -
Tsugutaka ITO, Masanao SHIMIZU1976 Volume 26 Issue 5 Pages 527-534
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSTo ascertain whether neuroleptics act on the caudate nucleus itself, the effects of these compounds as well as other centrally acting drugs were examined in relation to caudate spindle and EEG arousal responses (sciatic nerve stimulation) in gallamine-immobilized cats. Haloperidol and chlorpromazine enhanced the caudate spindle at a dose which had no effect on the EEG arousal response. On the other hand, clozapine and a higher dose of chlorpromazine enhanced the caudate spindle, but depressed the arousal response. High frequency stimulation of the sciatic nerve suppressed the caudate spindle. Pentobarbital, biperiden and diazepam, while depressing the arousal response, caused an enhancement of the caudate spindle. Imipramine at a low dose had no effect on either response, whereas at a high dose this drug enhanced the caudate spindle with concomitant depression of the arousal response. From these results, it may be concluded that the enhancing action on the caudate spindle induced by haloperidol and a low dose of chlorpromazine is due to an increase in susceptibility of the caudate nucleus itself. In addition, it is suggested that depression of the activating system is involved in an appearance of the caudate spindle.View full abstractDownload PDF (376K) -
Yasumichi HAGINO, Tatsuro SHIGEI1976 Volume 26 Issue 5 Pages 535-542
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSIn order to clarify the mechanism of the different sensitivity of the adrenoceptors between normal and hypothyroid rats, cyclic AMP levels in the liver and heart were measured after the administration of phenylephrine, isoproterenol, epinephrine and methoxamine. Cyclic AMP increased in all cases, but the extent of its increment in the heart was much less than that in the liver. Phentolamine and propranolol showed only a partial inhibition of cyclic AMP elevation by the agonists in the liver from normal and hypothyroid rat. On the other hand, propranolol blocked completely the effect of the agonists on the heart from both groups. It was also observed that cyclic AMP increased in adrenalectomized rats after the injection of the adrenergic agonists. The basal activity of protein kinase in hypothyroid status was slightly lower than that in the normal, but this enzyme was stimulated in the presence of cyclic AMP in vitro. These results suggest that the function of β-adrenoceptor remained normal even in hypothyroidism and responded well to isoproterenol and epinephrine. It is also indicated that the increased sensitivity of α-adrenoceptor to phenylephrine in the hypothyroid atria previously observed is probably in part independent of the mechanism mediated by cyclic AMP.View full abstractDownload PDF (288K) -
Yasuhiko FURUTA, Akira YOSHIKAWA1976 Volume 26 Issue 5 Pages 543-550
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe vascular action of 2, 4'-dimethyl-3-piperidino-propiophenone hydrochloride (tolperisone hydrochloride), a centrally acting muscle relaxant, was investigated in pentobarbital anesthetized dogs. Tolperisone given intravenously produced a transient hypotension, tachycardia, and hyperventilation. The drug increased the femoral arterial flow, and decreased the superior mesenteric arterial flow following an initial transient increase. When injected directly into femoral and mesenteric arteries, tolperisone caused a rapid increase in both arterial flows (vasodilatation). However, femoral vessels were about 90 times as sensitive as mesenteric vessels to tolperisone. These results indicate that tolperisone shifts the blood volume from mesenteric (visceral) vessels to femoral (skeltal) ones. The femoral vasodilatation produced by i.a. tolperisone was not depressed by the pretreatment with i.a. propranolol, atropine or chlorphenylamine. Tolperisone decreased the contractile force in an isolated and cross-circulated papillary muscle. Tolperisone produced adrenaline reversal and antagonized the pressor response to noradrenaline. Moreover, femoral vasoconstriction caused by i.a. adrenaline was converted to vasodilatation and that caused by i.a. noradrenaline was depressed during an i.a. infusion of tolperisone. These results indicate that tolperisone blocks adrenergic α-receptors. The blocking action was rapid in onset, short-lived, and in addition, competitive.View full abstractDownload PDF (294K) -
Seiji ICHIDA, Che-Hui KUO, Shuji UCHIDA, Kazuo NAGAI, Hiroshi YOSHIDA1976 Volume 26 Issue 5 Pages 551-558
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSTemperature dependent Ca-binding by the synaptic plasma membrane was increased in the presence of ATP and Mg++. Apparent Km for ATP was about 2.8 × 10-5 M and optimal concentration of Mg++ was 2 mM in the presence of 2 mM ATP. After preincubation with nonradioactive Ca++, ATP and Mg++ to attain a steady state, addition of 45Ca resulted in remarkable labelling of the membrane, indicating rapid turnover of most of the membrane bound Ca. The presence of oxalate (60 mM) greatly increased Ca up-take on prolonged incubation. The Ca uptake in presence and absence of oxalate had similar substrate specificity and was similarly influenced by various monovalent cations. Furthermore, activities for Ca-uptake in the presence and absence of oxalate could not be separated by sucrose density gradient centrifugation of the synaptic plasma membrane fraction. Accordingly, it was considered that Ca++ in the medium was taken up by surface of the membrane, ATP- and temperature-dependently and then transferred into a cavity where the Ca-oxalate complex is formed.View full abstractDownload PDF (351K) -
Akihiro TOBE, Toshikatsu KOBAYASHI1976 Volume 26 Issue 5 Pages 559-570
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSPharmacological properties of 2-amino-4-[4-(2-hydroxyethyl)-piperazin-1-yl]-6-trifluoromethyl-s-triazine (TR-10) were investigated in mice and rats. Chlorpromazine served as a reference compound. TR-10 expressed in general the pharmacological profiles as neuroleptics ascertained by anti-methamphetamine activity, supression of conditioned avoidance response, taming effects, decrease in exploratory behavior and cataleptogenic activity. Among these effects, anti-methamphetamine action was most potent. Different from chlorpromazine, TR-10 showed a similar pharmacological activity pattern in the intraperitoneal and oral routes of adminisstration as depicted from ED50/LD50 values. Although the effects relevant to neuroleptics were less potent than chlorpromazine, such were seen with TR-10 at lower doses than those causing muscle relaxation. TR-10 significantly depressed the spontaneous motor activity but showed no anti-convulsant action in mice. Hypothermic action, potentiating effects of hypnotics and α-adrenergic blocking action, characteristic to chlorpromazine, were very weak for TR-10. TR-10 also showed low toxicity in mice (LD50=820 mg/kg p.o., 465 mg/kg i.p.) compared with that of chlorpromazine (LD50 =370 mg, kg p.o., 228 mg/kg i.p.).View full abstractDownload PDF (498K) -
Hiromichi NAKAJIMA, Masao HOSHIYAMA, Keiko YAMASHITA, Akio KIYOMOTO1976 Volume 26 Issue 5 Pages 571-580
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSEffects of diltiazem on the electrical and mechanical activities of guinea pig papillary muscle were investigated in K-rich Tyrode's solution (KCl 12.7 mM). The electrical properties of cell membrane in K-rich solution were also examined in the ventricular muscle fibers. It was found that the overshoot as well as the maximum rate of rise (Vmax) of the action potential were highly sensitive to the extracellular concentration of CaCl2 in K-rich solution. Vmax was also affected by NaCl. Diltiazem at a lower concentration (1.1 × 10-7 M) caused a reduction in the contractile force of K-depolarized papillary muscle without producing significant changes in the resting and action potentials. In the presence of a higher concentration of diltiazem (1.1 × 10-5 M), the contractile force decreased concurrently with the change in the action potential. Addition of CaCl2 restored the original strength of contraction in parallel to the recovery of the action potential, especially in its overshoot and Vmax. From these results, it is inferred that diltiazem may decrease the contractile force of guinea pig papillary muscle either by interfering with the transmembrane calcium influx or by intracellularly reducing the free calcium ion concentration in the myoplasm.View full abstractDownload PDF (432K) -
Hikaru OZAWA, Tohru KOIDE1976 Volume 26 Issue 5 Pages 581-592
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe pharmacodynamic actions of (S)-2-[4, 5-dihydro-5-propyl-2(3H)-furylidene]-l, 3-cyclopentanedione (oudenone) were studied in both anesthetized animals and isolated organs. Oudenone (10-40 mg/kg i.v.) induced an initial rise in blood pressure followed by a prolonged hypotension in the anesthetized rats. In unanesthetized spontaneously hypertensive rats (SHR), oudenone (5-200 mg/kg p.o.) caused a doserelated decrease in the systolic blood pressure. The initial pressor effect was diminished by pretreatments with phentolamine, guanethidine, hexamethonium and was abolished in the pithed rats. In addition, intracisternal administrations of oudenone (100-600 μg/kg) showed a marked increase in blood pressure in the anesthetized rats, suggesting that the pressor effect may be due to centrally mediated actions. Oudenone, given intra-arterially into the femoral artery (400-800 μg/kg), caused a long-lasting vasodilation in anesthetized dogs. At a relatively high dose (40 mg/kg i.v.), oudenone antagonized all pressor responses to autonomic agents and central vagus nerve stimulation in anesthetized rats and dogs, however, oudenone showed no anti-cholinergic, -histaminergic, beta-adrenergic and adrenergic neuron blocking properties.View full abstractDownload PDF (506K) -
Masako MORIKAWA, Michiko INOUE, Shigeko YOSHIDA, Minoru TSUBOI1976 Volume 26 Issue 5 Pages 593-598
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSEffect of 1-(m-chlorophenyl)-3-N, N-dimethylcarbamoyl-5-methoxypyrazole (PZ-177) (62.5 and 250 mg/kg) on rat liver was investigated by measuring liver weight and drug-metabolizing enzyme activity. The effects of PZ-177 were compared with those of phenobarbital, phenylbutazone, and tiaramide hydrochloride. Increase of liver weight and liver/body weight ratio was observed in the rats treated with PZ-177 or phenobarbital, however, normal values were reverted to 1-2 weeks after treatment. PZ-177 similar to phenobarbital, significantly enhanced the activity of aminopyrine demethylase and aniline hydroxylase after 1, 2, and 4 weeks of treatment. In contrast, tiaramide hydrochloride decreased the activity of aminopyrine demethylase and aniline hydroxylase after 1 week of treatment, and significantly enhanced the activity of these enzymes after 4 weeks. The content of cytochrome P-450 and the activity of NADPH cytochrome C reductase were also increased by treatment with PZ-177. The sleeping time by hexobarbital was shortened significantly by the administration of PZ-177. Vmax for both aminopyrine demethylase and aniline hydroxylase increased by treatment with PZ-177. However, only the Km for aniline hydroxylase was increased by treatment with PZ-177. From the results of these experiments, PZ-177 may be classified as a phenobarbital-type inducer.View full abstractDownload PDF (237K) -
Aiko SAWA, Tetsuo OKA1976 Volume 26 Issue 5 Pages 599-605
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe effects of narcotic analgesics on the brain 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) levels of rats and mice were investigated in relation to our preceding data on the effect of humoral modulators on morphineinduced changes in locomotor activity and body temperature of rodents. The results suggest that morphine accelerates the release of brain 5-HT both in rats and mice, and that neither methadone nor pethidine alters the brain 5-HT and 5-HIAA levels in rats. The morphine-induced increase in brain 5-HT turnover is likely to be involved in the morphine-induced decrease in locomotor activity and hypothermia in rats. The activity-decreasing effects of methadone or pethidine, on the other hand, are mediated by mechanisms different from those which mediate the effects of morphine. In contrast, an increase in brain 5-HT turnover in mice apparently does not play an important role on activity-increasing effects of morphine but rather participates in other pharmacological effects of morphine.View full abstractDownload PDF (293K) -
Yukio ISHIDA, Kouzo WATANABE, Shigeru KOBAYASHI, Masaru KIHARA1976 Volume 26 Issue 5 Pages 607-614
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSA new compound, 6-(2-bromoethyl)-10, 11-methylenedioxy-5, 6, 7, 8-tetrahydrodibenz [c, e] azocine (DA-VIII-MBr) was found to have a more selective α-adrenergic blocking action than dibenamine or phenoxybenzamine. From dose-response curves for adrenaline and 5-hydroxytryptamine (5-HT) obtained in strips of rat aorta before and after incubation with each of the three blocking agents, the fractions of receptors remaining active for adrenaline and 5-HT, respectively, were estimated. After blockade with DA-VIII-MBr the receptors for adrenaline were blocked considerably, but those for 5-HT were little affected. Dibenamine blocked the receptors to adrenaline and 5-HT almost equally. The effective dose of phenoxybenzamine for adrenaline receptors was less than one hundredth that of dibenamine or DA-VIII-MBr, but specificity for these receptors was intermediate between those of dibenamine and DA-VIII-MBr. The structure of DA-VIII-MBr is an analog of apogalanthamine and its nitrogen atom bears the 2-halogenoethylamine group in part of an eight membered ring.View full abstractDownload PDF (328K) -
Tetsuo OKA, Eikichi HOSOYA1976 Volume 26 Issue 5 Pages 615-619
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSThe effect of humoral modulators on the morphine-induced increase in locomotor activity of mice was studied. The subcutaneous administration of 10 mg/kg of morphine-HC1 produced a marked increase in locomotor activity in mice. The morphine-induced hyperactivity was potentiated by scopolamine and attenuated by physostigmine. In contrast, both methscopolamine and neostigmine, which do not penetrate the blood-brain barrier, had no effect on the hyperactivity produced by morphine. Pretreatment of mice with α-methyltyrosine (20 mg/kg i.p., one hour), an inhibitor of tyrosine hydroxylase, significantly decreased the activity-increasing effects of morphine. On the other hand, pretreatment with p-chlorophenylalamine (3×320 mg/kg i.p., 24 hr), a serotonin depletor, caused no significant change in the hyperactivity. The study suggests that the activity-increasing effects of morphine are mediated by the release of catecholamines from adrenergic neurons in the brain. And the results are consistent with the hypothesis that morphine acts by retarding the release of acetylcholine at some central cholinergic synapses. It is also suggested from collected evidence that the activity-increasing effects of morphine in mice are mediated by mechanisms different from those which mediate the activity-increasing effects of morphine in rats.View full abstractDownload PDF (251K) -
Kyoichi OHASHI, Sakutaro TADOKORO1976 Volume 26 Issue 5 Pages 621-624
Published: 1976
Released on J-STAGE: December 19, 2006
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Kyuzo AOKI, Kanae YAMASHITA, Ken HOTTA1976 Volume 26 Issue 5 Pages 624-627
Published: 1976
Released on J-STAGE: December 19, 2006
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Yasuko HAYASHI, Tsutomu NOHNO, Yoshimichi MURAYAMA1976 Volume 26 Issue 5 Pages 627-631
Published: 1976
Released on J-STAGE: December 19, 2006
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Mitsuhiro NAGATA, Ken KADOTA1976 Volume 26 Issue 5 Pages 631-634
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (187K) -
Takayuki DOI, Akinori AKAIKE, Masami OHASHI, Masamichi SATOH, Hiroshi ...1976 Volume 26 Issue 5 Pages 634-637
Published: 1976
Released on J-STAGE: December 19, 2006
JOURNAL FREE ACCESSDownload PDF (153K)
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