著者

Shinichiro Haze Keiko Sakai Yoko Gozu

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.90, no.3, pp.247-253, 2002 (Released:2002-11-23)

参考文献数

18

被引用文献数

77 112

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We investigated the effects of fragrance inhalation on sympathetic activity in normal adult subjects using both power spectral analysis of blood pressure fluctuations and measurement of plasma catecholamine levels. Fragrance inhalation of essential oils, such as pepper oil, estragon oil, fennel oil or grapefruit oil, resulted in 1.5- to 2.5-fold increase in relative sympathetic activity, representing low frequency amplitude of systolic blood pressure (SBP-LF amplitude), compared with inhalation of an odorless solvent, triethyl citrate (P<0.05, each). In contrast, fragrance inhalation of rose oil or patchouli oil caused a 40% decrease in relative sympathetic activity (P<0.01, each). Fragrance inhalation of pepper oil induced a 1.7-fold increase in plasma adrenaline concentration compared with the resting state (P = 0.06), while fragrance inhalation of rose oil caused a 30% decrease in adrenaline concentration (P<0.01). Our results indicate that fragrance inhalation of essential oils may modulate sympathetic activity in normal adults.

著者

Toshio KASAMA Yoshinori IWATA Takashi OKUBO Yutaka SAKAGUCHI Mamoru SUGIURA

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.30, no.3, pp.293-300, 1980 (Released:2006-12-19)

参考文献数

10

被引用文献数

2

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Prolonged administration of insulin leads to the formation of insulin-binding antibodies due to contaminant peptides and the animal source of the insulin. It follows that quantitation and identification of these factors are of significant importance in pharmaceutical insulin preparations. The assay and test procedures stipulated in the current pharmacopoeia of various countries, nevertheless, cannot determine either of these effects. In the present study, the content of impurities in insulin preparations was measured by polyacrylamide gel disc electrophoresis and the animal source of insulin identified by amino acid analysis. Assays of 17 commercial insulin preparations by these techniques revealed diversity in purity and animal sources of insulin. The present results suggest potential usefulness of these assay methods and advisability of their adoption not only by the manufacturers but also by the official pharmacopoeia as well.

著者

Kumatoshi Ishihara Masashi Sasa

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.80, no.3, pp.185-189, 1999 (Released:2001-03-31)

参考文献数

40

被引用文献数

40 47

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Electroconvulsive therapy (ECT) is used to treat drug-resistant depressive disorders. The results of studies on the mechanism underlying the effectiveness of ECT on depression are still controversial. ECT stimulus is usually larger than the threshold of induction of seizures and activation of whole-brain is believed to be necessary to produce therapeutic effects. A single ECT session induces alterations of the electroencephalogram (EEG) including initial epileptic discharges, then slow waves, and finally flattened EEG. Repeated ECT results in an increasing number of slower waves in the EEG for as long as a month. ECT-induced changes in various neurotransmitter systems have also been reported. Serotonin (5-hydroxytryptamine, 5-HT) is one of the most important neurotransmitters involved in depressive illness, and ECT alters several 5-HT-receptor subtypes in the central nervous system. 5-HT1A receptors in post-synaptic neurons are sensitized by repeated ECT, but those in pre-synaptic neurons (auto-receptors) are not changed. In addition, our electrophysiological studies have shown that ECT increases sensitivity to 5-HT of 5-HT3 receptors in the hippocampus, resulting in an increase in release of neurotransmitters such as glutamate and γ-aminobutyric acid. In contrast, ECT decreases the auto-receptor functions in noradrenergic and dopaminergic neurons in the locus coeruleus and substantia nigra, respectively, resulting in an increase in release of noradrenaline and dopamine. In conclusion, 5-HT1A-receptor sensitization may be important for explaining the effectiveness of ECT, as this change induces a decrease in the number of 5-HT2A receptors that are elevated in depressive patients. Facilitation of neurotransmitter releases due to 5-HT3-receptor sensitization by ECT may also play an important role in effective treatment of depressive patients refractory to therapeutic drugs.

著者

Masakatsu Takahashi Hiroko Fukunaga Hiroshi Kaneto Shin-ichi Fukudome Masaaki Yoshikawa

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.84, no.3, pp.259-265, 2000 (Released:2001-05-31)

参考文献数

36

被引用文献数

38 57

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Central effects of gluten exorphin A5 (Gly-Tyr-Tyr-Pro-Thr), a fragment from wheat gluten, were studied on the pain-inhibitory system, emotionality and learning/memory processes in mice. Orally administered gluten exorphin A5 produced neither an antinociceptive effect nor an effect on morphine analgesia. Intracerebroventricularly (i.c.v.) administered gluten exorphin A5 produced mild but significant antinociception in a dose-dependent manner, while not affecting the morphine analgesia. On the other hand, oral gluten exorphin A5 suppressed the endogenous pain-inhibitory system, i.e., antinociception induced by socio-psychological- (PSY-) stress (SIA) using a communication box; intraperitoneal gluten exorphin A5 abolished both footshock- (FS-) stress-induced antinociception (SIA) and PSY-SIA; and i.c.v. gluten exorphin A5 suppressed FS-SIA, but rather potentiated PSY-SIA. This peptide given by these routes was withuot effect on forced swim-SIA. In addition, oral gluten exorphin A5 tended to prolong the retention time on open arms in the elevated plus-maze test. Finally, oral gluten exorphin A5 when given during the post-training period of learning/memory processes significantly increased the latency into the dark compartment in the one-trail step-though type passive avoidance test, indicating that the peptide also facilitates the acquire/consolidation process of learning/memory. Thus, gluten exorphin A5 has been found to produce various effects no only in the peripheral nervous systems but also in the central nervous system.

著者

J.N. SINHA B.P. JAJU R.C. SRIMAL

出版者

(社)日本薬理学会

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.16, no.3, pp.250-256, 1966-09-01 (Released:2007-02-02)

参考文献数

12

被引用文献数

1 1

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Hafliger (1) synthesized a series of iminodibenzyl compounds which were found to possess antihistaminic, anticholinergic, sedative and analgesic properties. It was only after a clinical trial by Kuhn (2) that G 22355 (imipramine) “emerged as an antidepressant”. The exact mechanism of the antidepressant action of imipramine (IMI), its derivative desmethylimipramine (DMI) and its analogue amitriptyline (AMI) is not yet established. These agents have been shown to antagonise reserpine induced muscular rigidity and this effect has been attributed to their central cholinolytic activity (3, 4). Another structurally related antidepressant, orphenadrine, has been reported to possess both central (5) and peripheral (6) muscle relaxant properties. We have, earlier, reported the inhibition of myoneural transmissson by IMI, DMI and AMI (7). Prolonged inhibition of linguomandibular reflex by low doses of these agents as compared to short lived action of mephenesin (8) prompted us to find out if these agents fulfill all the criteria essential for a central muscle relaxant. Accordingly, these drugs were subjected to various test procedures like effect on behaviour, effect on polysynaptic linguomandibular reflex, effect on facilitatory influence of reticular formation on patellar reflex and the effect on decerebrate muscular rigidity in cat.

著者

Seitaro Ohkuma Shi-Hu Chen Masashi Katsura Da-Zhi Chen Kinya Kuriyama

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.64, no.2, pp.125-128, 1994 (Released:2006-04-10)

参考文献数

19

被引用文献数

32 33

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The effect of muscimol on N-methyl-D-aspartate (NMDA)-induced injury of primary cultured cerebral cortical neurons was examined. NMDA induced a dose-dependent leakage of LDH activity, which was significantly inhibited by (±)-5-methyl-10, 11-dihydro-5H-dibenzo-[a, d]cyclopentan-5, 10-imine (MK-801). Muscimol significantly reduced the NMDA-induced increase of lactic dehydrogenase (LDH) leakage, and bicuculline abolished this protective effect of muscimol. Similarly, muscimol reduced the NMDA-induced increase in trypan blue staining of the cells, and bicuculline suppressed this inhibitory action of muscimol. These results suggest that GABAA-receptor stimulation exerts a protective action against the neuronal injury induced by NMDA-receptor activation.

著者

Alain Schotte Pascal Bonaventure Paul F.M. Janssen Josee E. Leysen

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.69, no.4, pp.399-412, 1995 (Released:2006-04-07)

参考文献数

73

被引用文献数

65 68

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Risperidone was compared with antipsychotics hitherto used for in vitro receptor binding using animal brain or cloned (human) receptors and in vivo receptor occupancy in rat and guinea pig brain following acute treatment. Both in vitro and in vivo, risperidone, 9-OH-risperidone, SM-9018, clozapine and clocapramine showed higher affinity for 5-HT2A- than for D2-receptors, whereas mosapramine, haloperidol, bromperidol and nemonapride had a slight to strong preference for D2- compared to 5-HT2A-receptors. In vivo, risperidone showed the highest potency for 5-HT2A-receptor occupancy; To obtain the same extent of D2-receptor occupancy, a 19-times higher dosage was required. 9-OH-Risperidone, the principal active metabolite of risperidone, showed a receptor occupancy profile comparable to that of risperidone. No regional selectivity for D2-receptor occupancy in mesolimbic vs nigrostriatal areas was detected for any of the compounds. Risperidone differed from the other compounds by the remarkably shallow slope of its D2-receptor dose-occupancy curve. A greater predominance of 5-HT2A-receptor vs D2-receptor occupancy and a more gradual occupancy of D2A-receptors differentiate risperidone from the other compounds. Both properties probably assist in preventing an extensive blockade of D2-receptors, the cause for extrapyramidal symptoms (EPS). The predominant 5-HT2A-receptor occupancy most likely underlies risperidone''s beneficial effects on the negative symptoms of schizophrenia and an adequately low D2-receptor occupancy adds to the treatment of positive symptoms with a low liability of EPS.

著者

Masayoshi Furushiro Satoru Suzuki Yoshiyuki Shishido Masashi Sakai Hideyuki Yamatoya Satoshi Kudo Shusuke Hashimoto Teruo Yokokura

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.75, no.4, pp.447-450, 1997 (Released:2006-03-27)

参考文献数

15

被引用文献数

20 21

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Soybean lecithin transphosphatidylated phosphatidylserine (SB-tPS) was investigated for its effect on the impaired learning of a passive avoidance task by mice induced by scopolamine or cycloheximide. SB-tPS (240, 360, 480 mg/kg) administered orally significantly prolonged the step-through latency shortened by scopolamine. SB-tPS (240 mg/kg) administered orally also prolonged the step-through latency shortened by cycloheximide. These results suggest that the effect of SB-tPS on the impaired learning behavior may be related not only to the cholinergic system but also the serotonergic system.

著者

Hiroshi MIKASHIMA Shuzo TAKEHARA Yoshito MURAMOTO Takako KHOMARU Michio TERASAWA Tetsuya TAHARA Yutaka MARUYAMA

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.44, no.4, pp.387-391, 1987 (Released:2006-09-15)

参考文献数

13

被引用文献数

10 9

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The antagonistic effect of etizolam, an anti-anxiety drug, on platelet-activating factor (PAF) was investigated in rabbit platelets in vitro. Etizolam inhibited PAF-induced aggregation in a dose-dependent manner, with an IC50 of 3.8 μM, about one tenth that of triazolam (IC50=30 μM). At 300 μM, it inhibited both ADP and arachidonic acid-induced aggregation only slightly, while the other anti-anxiety drugs tested had no effect on PAF-induced aggregation even at this concentration. Etizolam and triazolam inhibited the specific binding of 3H-PAF to PAF receptor sites on washed rabbit platelets with IC50 values of 22 nM and 320 nM, respectively. Diazepam and estazolam were inactive even at 1 μM. These results indicate that etizolam is a specific antagonist of PAF.

著者

Makoto Tominaga David Julius

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.83, no.1, pp.20-24, 2000 (Released:2001-01-31)

参考文献数

29

被引用文献数

58 68

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Capsaicin, the main pungent ingredient in ‘hot’ chili peppers, elicits burning pain by activating specific(vanilloid)receptors on sensory nerve endings.The cloned capsaicin receptor(VR1)is a nonselective cation channel with six transmembrane domains that is structurally related to a member of the TRP(transient receptor potential)channel family.VR1 is activated not only by capsaicin but also by increases in temperature that reach the noxious range(>43°C).Protons potentiate the effects of capsaicin or heat on VR1 activity by markedly decreasing the capsaicin concentration or temperature at which the channel is activated.Furthermore, a significant increase in proton concentration(pH<5.9)can evoke channel activity at room temperature.The analysis of single−channel currents in excised membrane patches suggests that capsaicin, heat or protons gate VR1 directly.VR1 can therefore be viewed as a molecular integrator of chemical and physical stimuli that elicit pain.VRL−1, a VR1 homologue, is not activated by vanilloids or protons, but can be activated by elevation in ambient temperature exceeding 52°C.These findings indicate that related ion channels may account for thermal responsiveness over a range of noxious temperature.

著者

Masaaki Tagawa Michiko Kano Nobuyuki Okamura Masatoshi Itoh Eiko Sakurai Takehiko Watanabe Kazuhiko Yanai

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.83, no.3, pp.253-260, 2000 (Released:2001-01-31)

参考文献数

46

被引用文献数

16 16

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Ethanol is a social drug and has been generally known to be a CNS depressant.A large fluctuation of blood alcohol concentration(BAC)is well−known to occur due to main factors such as the genetic polymorphism of the main alcohol metabolizing enzymes and the effect of blood.Few studies have substantially discussed the relationship between impaired CNS activities and BAC.In this study, focusing on the correlation of BAC, we investigated the acute effects of alcohol intake on cognitive performance in humans by objective evaluation methods consisting of the attention−demanding cognitive tasks.Tasks were administered to ten healthy male volunteers before and after ingesting established amounts of alcohol.With increased BAC, we observed prolongation of reaction time performances and lowering of a coordination performance.From the results, we concluded that cognitive performance deteriorates with an increase of BAC.Additionally, the BAC threshold that causes significant impairment of cognitive performance was estimated to be approximately 50 mg/dl(ca.10 mM).

著者

Nobuo KUBO Osamu SHIRAKAWA Takayoshi KUNO Chikako TANAKA

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.43, no.3, pp.277-282, 1987 (Released:2006-09-15)

参考文献数

17

被引用文献数

98 105

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Quantitative evaluation of antimuscarinic effects of antihistamines (H1and H2-receptor antagonists) was carried out using a receptor-binding assay. The inhibition constants (K1 values) of twenty seven H1-receptor antagonists, one related antidepressant and three H2-receptor antagonists at H1-receptors and muscarinic receptors in the bovine cerebral cortex were determined. All the H2receptor antagonists examined showed very low affinity for the muscarinic receptors. On the other hand, some H1-receptor antagonists (mequitazine, cyproheptazine, clemastine, diphenylpyraline, promethazine, homochlorcyclizine and alimemazine) had high affinity for the muscarinic receptors (K1=5.0-38 nM). Another group of H1 -receptor antagonists (mepyramine, terfenadine, metapyrilen, azelastine, hydroxyzine and meclizine) had low affinity for the muscarinic receptors (K1=3, 600-30, 000 nM). Thus, a broad range of antimuscarinic potencies among the antihistamines was demonstrated. These results should provide helpful information with regard to the clinical and experimental use of antihistamines.

著者

SHIGERU TSUNOO TSUNEO KAWAI TARO MORI

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.2, no.2, pp.149-153, 1953 (Released:2007-02-16)

参考文献数

8

被引用文献数

2 4

著者

Sato Yoji Kurose Hitoshi Nagao Taku

出版者

公益社団法人 日本薬理学会

雑誌

The Japanese journal of pharmacology (ISSN:00215198)

巻号頁・発行日

vol.73, no.4, pp.325-332, 1997-04-01

参考文献数

22

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To examine the contribution of &beta;-adrenoceptor (&beta;AR) downregulation to desensitization of &beta;ARs by chronic administration of a &beta;AR agonist, we compared the adenylyl cyclase (AC) activities in two kinds of cardiac ventricular membranes with decreased available &beta;ARs: one was derived from rats infused with a selective &beta;<SUB>1</SUB>AR agonist, T-0509 [(&minus;)-(<I>R</I>)-1-(3, 4-dihydroxyphenyl)-2-[(3, 4-dimethoxyphenethyl)amino]ethanol hydrochloride], in vivo (40 &mu;g/kg/hr, s.c. for 6 days); and the other was obtained from treatment of control membranes with an irreversible &beta;AR antagonist, bromoacetyl alprenolol methane (BAAM). T-0509 infusion decreased the densities of &beta;<SUB>1</SUB>ARs and, &beta;<SUB>2</SUB>ARs by 26% and 32%, respectively, and reduced the maximal isoproterenol-stimulated AC activity by 53%. The amount of G<SUB>s&alpha;</SUB> and G</SUB>i&alpha;</SUB> proteins in the membranes was not significantly changed by T-0509 infusion. To make preparations that mimic the T0509-induced downregulation, we treated the control membranes with 100 nM BAAM in vitro. The BAAM treatment decreased the B<SUB>max</SUB>, value of [<SUP>125</SUP>I] iodocyanopindolol for &beta;1ARs and &beta;2ARs by 29070 and 36070, respectively, whereas it reduced the maximal effect of isoproterenol on AC activity only by 37%. These results suggest that downregulation of &beta;ARs cannot fully account for the desensitization by chronic treatment of T-0509 and that other mechanism(s) can play a significant role in the loss of responsiveness.

著者

Naohiko ONO Yasundo YAMASAKI Noriyuki YAMAMOTO Akihiko SUNAMI Hidekazu MIYAKE

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.42, no.3, pp.431-439, 1986 (Released:2006-09-15)

参考文献数

23

被引用文献数

4 5

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The possible mechanism of the anti-inflammatory activity of proglumetacin maleate (PGM), a new indomethacin (IND) derivative interacting with arachidonic acid (AA) metabolism, was investigated to elucidate the contributions of PGM itself and its two major metabolites, desproglumideproglumetacin maleate (DPP) and IND. PGM caused much less inhibition of PGE2 formation by sheep seminal vesicle microsomes (IC50=310 μM) and TXB2 formation by a washed rabbit platelet suspension (IC50=6.3 μM) than IND. DPP also caused less inhibition of cyclooxygenase than IND. Moreover, PGM had less effect on sodium arachidonate (SAA)-induced rat platelet aggregation ex vivo and AA-induced sudden death in rabbits than IND. These results show that PGM has anti-inflammatory activity after its conversion to the active metabolite IND. However, the inhibitory effects of PGM and DPP were as strong as that of IND on SAA- or collageninduced rabbit platelet aggregation in vitro. These activities are considered to be associated with platelet membrane interaction. Moreover, unlike IND, PGM (IC50=1.5 μM) and DPP (IC50=16.3 μM) strongly inhibited 5-HETE formation by the cytosol of guinea pig polymorphonuclear leukocytes. This unique activity of PGM on 5-lipoxygenase may contribute to its anti-inflammatory activity.

著者

Remmers John E. Schultz Stanley A. Wallace Jacqueline TAKEDA Ryuji HAJI Akira

出版者

公益社団法人 日本薬理学会

雑誌

The Japanese journal of pharmacology (ISSN:00215198)

巻号頁・発行日

vol.75, no.2, pp.161-169, 1997-10-01

参考文献数

19

被引用文献数

4

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Investigation of the identity and modes of action of neurotransmitters in the mammalian central nervous system can be facilitated by simultaneous intracellular recording of membrane potential and extracellular iontophoresis of agonists and antagonists. We describe here techniques for conveniently constructing a compound microelectrode, originally described by Sonnhof (Pflugers Arch 341, 351-358, 1973), suitable for such studies. The Sonnhof electrode consists of two components, a centraxial micropipette for recording membrane potential surrounded by a cylindrical array of 6 pipettes for iontophoresis. The cylindrical array tapers coaxially and terminates in 6 contiguous, crescent-shaped orifices surrounding the terminal portion of the central pipette, 25-50 &mu;m from the tip. Pipettes were constructed from borosilicate glass tubing of 1-mm wall thickness having a 10-mm or 16-mm outer diameter. The resistances, flux and transport numbers for iontophoresis of glycine were measured for pipettes constructed from both sizes of glass. Flux increased with increasing levels of current, and transport number decreased with increasing micropipette resistance. A spherical diffusion model points out the steep dependence of steady state concentration on diffusional distance, stressing the importance of diminishing the distance between the iontophoresis source and the recording site. This is particularly true when brief pulses of current are used.

著者

Yuji Ikegaya Norio Matsuki

出版者

The Japanese Pharmacological Society

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.89, no.3, pp.324-326, 2002 (Released:2002-07-22)

参考文献数

10

被引用文献数

8 12

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This paper reports that vasopressin is emetogenic in the house musk shrew Suncus murinus. Either intravenous or intracerebroventricular administration of vasopressin caused vomiting within a few minutes. The ED50 of intravenous vasopressin was as high as 4.67 μg/kg, whereas intracerebroventricularly injected vasopressin was effective at a low dose of 20 ng/brain. The emetogenic target of vasopressin may therefore be present in the central nervous system. We propose the Suncus as a useful animal for investigation of vasopressin-mediated emesis, including motion sickness.

著者

Seiji INOUE Ka BIAN Tomio OKAMURA Hideki OKUNISHI Noboru TODA

出版者

(社)日本薬理学会

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.50, no.3, pp.271-282, 1989 (Released:2006-08-25)

参考文献数

24

被引用文献数

7 9

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Effects of eperisone, an antispasmodic in skeletal muscle, were investigated in helical strips of dog saphenous artery and vein. Eperisone relaxed saphenous arteries and veins previously contracted with norepinephrine, serotonin, acetylcholine, K+, or Ba2+; but in contrast, it produced contractions in the blood vessels contracted with prostaglandin (PG) F2α. Treatment with eperisone attenuated the contractions induced by norepinephrine and serotonin in the arteries and those by clonidine and phenylephrine in the veins. Eperisone inhibited angiotensin II-induced relaxations, mediated possibly by endogenous PGI2, but did not alter relaxations caused by exogenous PGI2. Treatment with eperisone (10-5 M) potentiated the contractile response to electrical stimulation of adrenergic nerves; the potentiating effect was suppressed by yohimbine. The eperisone-induced contraction in PGF2α-contracted arteries was inhibited by treatment with indomethacin or aspirin, although cyclooxygenase activity was not inhibited by eperisone. These results may indicate that eperisone blocks postjunctional α1- and α2-adrenergic, muscarinic, serotonergic receptors and prejunctional α2 adrenoceptors and reduces PGI2 synthesis via a mechanism other than cyclooxygenase inhibition.

著者

Kiyoshi OIZUMI Hiroshi NISHINO Hiroyuki KOIKE Toshio SADA Masaaki MIYAMOTO Tomio KIMURA

出版者

(社)日本薬理学会

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.51, no.1, pp.57-64, 1989 (Released:2006-08-25)

参考文献数

14

被引用文献数

36 45

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CS-905 is a novel dihydropyridine calcium blocker. A single oral administration of CS-905 or nicardipine at doses of 0.3-3.0 mg/kg produced a dosedependent reduction of blood pressure in conscious SHR. CS-905, when administered orally in conscious SHR, was more than 3 times as potent as nicardipine. Unlike the hypotensive effect of nicardipine, that of CS-905 has a gradual onset and is long-lasting, with little increase in heart rate. An intravenous administration of CS-905 also produced a hypotension with a slow onset and long duration in SHR, but CS-905 was 3 times less potent than nicardipine by intravenous administration. This difference may be attributed to the first pass effect, which was associated with nicardipine but not with CS-905. The blood pressure lowering effects of CS-905 was most potent in DOCA-salt hypertensive rats, followed by SHR, RHR and normotensive rats, in this order. CS-905 is expected to be an antihypertensive agent that is effective on a once a day regimen in clinical settings.

著者

Keishiro SHIMURA Hitoshi ITO Hiroshige HIBASAMI

出版者

(社)日本薬理学会

雑誌

The Japanese Journal of Pharmacology (ISSN:00215198)

巻号頁・発行日

vol.33, no.2, pp.403-408, 1983 (Released:2006-11-07)

参考文献数

25

被引用文献数

26 24

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On crossed immunoelectrophoresis, human serum C3 (the third component of complement) converted by antitumor polysaccharides (ATSO [antitumor polysaccharide oral], AB-P [Agaricaus blazei/polysaccharide], GU-P [Grifora umbellata polysaccharide], PS-K [polysaccharide Kureha] and zymosan) moved faster than native C3, appearing as the 3rd peak. The ratio of height of the 3rd peak to the α2-macroglobulin (α2-M) peak was linearly proportional to the dose of ATSO. At the dose of 500 μg/ml antitumor polysaccharides, the ratios were higher than 0.76, and the ratios for the serum treated with polysaccharide of no antitumor activity (dextran and gum arabic) were less than about 0.52. This ratio readily determined in vivo can be used as a measure for the antitumor activity of polysaccharides.