巻号一覧
32 巻 (1982)
- 6 号 p. 973-
- 5 号 p. 751-
- 4 号 p. 583-
- 3 号 p. 405-
- 2 号 p. 213-
- 1 号 p. 1-
32 巻, 6 号
選択された号の論文の30件中1～30を表示しています
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Issei TAKAYANAGI, Hideko SONE, Katsuyoshi KAWASHIMA, Yukinobu SOHJI, T ...1982 年 32 巻 6 号 p. 973-979
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーA newly synthesized drug, SX-284, depressed the twitch response of the ileum from guinea pig to electrical stimulation at 0.1 Hz. SX-284 proved to be almost as active as atropine on electrically stimulated ileum. The responses of guinea pig ileum to nicotine and serotonin were also inhibited by SX-284. However, SX-284 did not influence the release of transmitters from the motor, sympathetic, nonadrenergic inhibitory, noncholinergic excitatory nerves, and responses of various smooth muscles mediated through drug receptors, and at these doses, SX-284 inhibited the release of acetylcholine from the vagus nerve. These facts indicate that SX-284 specifically inhibits the acetylcholine release from the vagus nerve. Furthermore, spontaneous movement of the guinea pig ileum was dose-dependently depressed by SX-284. The potency ratio for SX-284 relative to atropine was 1.7.抄録全体を表示PDF形式でダウンロード (301K) -
Masao KOIDA, Yoshinobu YAMAMOTO, Hiromichi NAKAMUTA, Junko MATSUO, Mas ...1982 年 32 巻 6 号 p. 981-986
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーIt was found that salmon calcitonin-I (sCT) inhibited in vitro 45Ca2+-uptake by rat brain hypothalamus blocks in a dose-dependent manner. The minimum effective concentration was estimated to be 10 nM or less. The effect appeared to be specific to the hypothalamus and was not observed with the pons plus medulla oblongata or the cerebral cortex. Two C-terminal fragments of the fish hormone, sCT (10-32) and sCT (22-32), and porcine calcitonin failed to inhibit the ion-uptake though tested in concentrations abolishing 125I-sCT binding to these brain tissues, indicating that the whole structure of sCT is essential for the inhibitory effect but not for the binding. Another finding to be noted was a possible dependency of this effect on the integrity of the cell membrane structure. A crude synaptosomal fraction subsequently prepared from sCT-exposed hypothalamus blocks exhibited a decreased uptake of 45Ca2+, while a corresponding fraction from unexposed tissue did not respond to the hormone. These characteristics of this novel in vitro effect of sCT suggest its possible relevancy to the anorectic effect which also appears to be specific to the fish hormone.抄録全体を表示PDF形式でダウンロード (309K) -
Akira SHIMADA, Tomoji YANAGITA1982 年 32 巻 6 号 p. 987-997
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe influence of single and repeated doses of morphine, pentazocine, and chlorpromazine on the latent time of cortical evoked potentials was observed in rats. The evoked potentials were induced by electrical stimulation of the sciatic nerve under the condition of curarization and artificial respiration. The evoked potential consisted of 4 phases. The latent time of the N2 component was prolonged by single dose administration of morphine at 5 mg/kg, s.c., pentazocine at 15 mg/kg, s.c., or chlorpromazine at 2 mg/kg, s.c. The effects of morphine and pentazocine were antagonized by naloxone but that of chlorpromazine was not. By repeated administration of morphine at 5 mg/kg or pentazocine at 15 mg/kg twice daily for 4 weeks, the prolongation of latent time tended to disappear gradually. Further, in these rats the latent time became shorter than that of normal rats after naloxone administration or natural withdrawal for 18 hr. Thus the development of tolerance to and physical dependence on these drugs were demonstrated by recovering and shortening of the latent time, even when withdrawal signs were not apparently observed in the rats' gross behavior. On the other hand, repeated administration of chlorpromazine at 2 mg/kg twice daily for 4 weeks did not produce such shortening of the latent time as was observed with morphine and pentazocine. These results indicate that the evoked potential can serve as a sensitive parameter for observation of the development of tolerance to and physical dependence on opioid analgesics in rats.抄録全体を表示PDF形式でダウンロード (581K) -
Takashi MATSUBARA, Akira TOUCHI, Ayako OGAWA1982 年 32 巻 6 号 p. 999-1011
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーEnzyme distribution in rat liver lobes was investigated using liver homogenate as the enzyme source. When the content or the activity was expressed on the basis of unit (gram) wet weight of liver tissue, the protein concentration was almost the same throughout the liver, but several enzymes were distributed heterogeneously within the liver. Cytochrome P-450 monooxygenase activity was higher in the median and right lobes of livers, while the left lobe contained a higher concentration of mitochondrial enzymes. Phenobarbital induced cytochrome P-450 monooxygenase, and the activity was still higher in the median and right lobes even after the pretreatment of rats with phenobarbital. On the other hand, administration of β-naphthoflavone resulted in a uniform increase of cytochrome P-450 (P-448) content throughout the liver to almost the same concentration. Increase of cytochrome P-448-dependent O-dealkylation activity of 7-alkoxycoumarin by the administration of β-naphthoflavone was much greater in the left lobe compared to that in the median and the right lobes. Heterogeneous distribution of the enzymes in various liver lobes was also determined employing liver samples obtained from various physiological states of rats (fasting, glucose refeeding after fasting and hyperthyroidism), although the cytochrome P-450 content and drug-metabolizing activity were altered markedly depending upon the physiological states of the rats.抄録全体を表示PDF形式でダウンロード (645K) -
Yoshinobu YAMAMOTO, Hiromichi NAKAMUTA, Masao KOIDA, Jay K. SEYLER, Ro ...1982 年 32 巻 6 号 p. 1013-1017
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe anorectic potency of salmon, porcine and human calcitonins (sCT, pCT and hCT, respectively) and two sCT-fragments were compared in rats. Intraventricular injections of sCT (0.062 and 0.031 nmole/animal) significantly reduced the normal feeding and body weight. The effect appeared to be dose-dependent, reversible and lasted longer than 6 hr. No anorexia ensued, however, on injections of mammalian hormones though tested in relatively high doses (pCT: up to 3.7 nmole, hCT: 3.7 nmole). The C-terminal fragments of sCT, sCT (10-32) and sCT (22-32) were also found to be devoid of anorectic activity; but when administered with sCT, the longer fragment (1.2 nmole) significantly decreased the effect of sCT and even the shorter one (18 nmole) tended to act as an antagonist. This property was not recorded with pCT and hCT in the doses examined. On the one hand, these results indicate a novel specificity of the anorectic receptor in rat brain; and on the other hand, they seem to strongly argue against the hypothesis that in mammals thyroidal calcitonin secreted postprandially might participate in the regulation of subsequent feeding, unless the presence of the sCT-like molecule can be detected in mammals. All the more because detection of such a molecule must await development of a specific assay, the antagonistic property of the sCT fragment found herein would have use for clarifying the physiological significance of the anorectic receptor which is possibly in the hypothalamus.抄録全体を表示PDF形式でダウンロード (228K) -
Kenichi MIYAMOTO, Fujiko SANAE, Masashi IWASAKI, Ryozo KOSHIURA1982 年 32 巻 6 号 p. 1019-1026
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーEffects of several autonomic agents on the cytotoxicity of mitomycin C in HeLa cells were studied. When β-adrenergic stimulants such as isoproterenol, epinephrine, terbutaline and turobuterol were added at concentrations over 1014 M 15 to 60 min before mitomycin C, the colony-forming ability of HeLa cells was significantly inhibited more than by mitomycin C alone. The action of isoproterenol and epinephrine on the colony-forming ability of the cells was abolished by propranolol. The intracellular cyclic AMP level of HeLa cells reached the peak of about twofold the basal level at 30 min after the addition of 10-8 M isoproterenol. In combination with mitomycin C, the high level of intracellular cyclic AMP induced by isoproterenol was maintained for a significantly longer period in comparison with that by isoproterenol alone, while mitomycin C alone caused essentially no change in the cyclic AMP level. The pretreatment with dibutyryl cyclic AMP also enhanced the effect of mitomycin C. From these findings, it is strongly suggested that the synergistic effect of β-adrenergic stimulants on the cytotoxicity of mitomycin C is mediated via stimulation of the β-adrenoceptors of HeLa cells which elevates the intracellular cyclic AMP for a long time in combination with mitomycin C.抄録全体を表示PDF形式でダウンロード (393K) -
Tatsuo MITA, Takayoshi KUNO, Hisao NAKAI, Chikako TANAKA1982 年 32 巻 6 号 p. 1027-1032
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe D2 receptor and two distinct affinity 5-HT2 receptors in the human prefrontal cortex were labeled with 3H-spiperone. In the Scatchard analysis of stereoselective binding defined by (+) and (-)-butaclamol, two high affinity binding sites were clearly demonstrated. Apparent KD values of these higher and lower affinity sites determined in this manner were 0.028 and 0.64 nM, respectively. However, drug displacement studies of 3H-spiperone binding at these sites, using different concentrations of 3H-spiperone (0.05 nM for higher affinity sites and 0.5 nM for lower affinity sites), indicated that 70-80% of the higher affinity sites and almost all of the lower affinity sites showed characteristics of the 5-HT2 receptor and that 20-30% of the higher affinity sites showed characteristics of the D2 dopamine receptor. An additional saturation experiment related to the specific binding of 3H-spiperone to 5-HT2 receptors confirmed the existence of two distinct populations of 5-HT2 receptors that had different affinities for spiperone. Apparent KD values for higher and lower affinity 5-HT2 receptors were 0.091 and 1.27 nM, respectively. As the D2 receptor is a possible site of antipsychotic action of neuroleptics, these receptors, especially the D2 receptor in the human prefrontal cortex, seem to play an important role in psychotic disorders.抄録全体を表示PDF形式でダウンロード (349K) -
Sakae MURATA, Taku NAGAO, Hiromichi NAKAJIMA1982 年 32 巻 6 号 p. 1033-1040
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe effects of diltiazem on the cerebral blood flow and cerebrovascular spasm were studied in pentobarbital anesthetized animals. In Rhesus monkeys, the common carotid and internal carotid blood flow were measured by an electromagnetic flowmeter. Diltiazem (10-300 μg/ kg, i.v.) dose-dependently increased both the common carotid and internal carotid blood flow, and the increase in internal carotid blood flow persisted for a longer period than that in the common carotid blood flow. In dogs, regional blood flow in the cerebral cortex (rCBF) was measured by means of the hydrogen gas clearance method. Diltiazem (20 μg/kg/min, i.v.) increased rCBF by about 20% of the control during the infusion, and the increase in rCBF was still continued 40 min after the infusion was stopped. In cats, the basilar artery was exposed by craniotomy through the transcervico-transclival approach, and vasospasm was induced by topical administration of 5-HT, PGF2α and incubated blood. Diltiazem, either applied topically to the artery (100 μg/ml) or infused continuously into the femoral vein (20 or 40 μg/kg/min), suppressed the vasoconstriction evoked by the spasmogen.抄録全体を表示PDF形式でダウンロード (464K) -
Tohru HORIE, Toshiro OHNO, Kensaku KINOSHITA1982 年 32 巻 6 号 p. 1041-1049
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe metabolic fate of a new antihypertensive agent, tripamide (N-(4-aza-endo-tricyclo [5.2.1.02, 6]-decan-4-yl)-4-chloro-3-sulfamoyl-benzamide), in rats and rabbits was studied using its 14C-labeled compound. The blood level of radioactivity in both species reached the maximum at 1 hr after oral administration, indicating the rapid absorption of the drug from the gastrointestinal tract. Following either oral or intravenous administration, a high concentration was observed in the liver of rats, but it was found in the kidney of rabbits. The major metabolite was 4-chloro-3-sulfamoylbenzoic acid in tissues, urine and feces; and in both species, the unchanged drug was only detected in the kidney. The pathway of excretion of radioactivity was via urine and feces in case of rats; but in rabbits, it was predominantly excreted via urine, although significant quantities of radioactivity were excreted with feces. The radioactivity excreted in feces was attributable to that which was excreted in bile, indicating the absorption of almost all the tripamide administered in both species. During the period of repeated dosing, though blood levels increased gradually and became about 1.5 times as high as that in the single dosing, radioactivity did not accumulate in most tissues and organs.抄録全体を表示PDF形式でダウンロード (445K) -
Akihisa MIYAKAWA, Su-Ja KIM, Tsutomu KAMEYAMA, Ryoichi ISHITANI1982 年 32 巻 6 号 p. 1051-1057
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーMyelin fragments from rat brain stems were treated with butanolwater mixtures and binding experiments of 14C-tryptamine to these extracts (i.e. proteolipids) were performed by Sephadex LH20 column chromatography. The elution peak of 14C-tryptamine appeared in a boundary between 6:1 and 4:1 chloroform-methanol, together with 19.2 and 7.3% of the total recoveries of protein and lipid phosphorus, respectively. Various compounds were studied to examine their inhibitory effects on the tryptamine binding to these extracts. The results indicated that only tryptamine and 5-methoxytryptamine inhibited the tryptamine binding, but indole analogues and other neurotransmitters had no effect. The kinetic analysis revealed that the tryptamine binding components present in the myelin butanol extracts are composed of saturable and non-saturable components, and the saturable binding components had an apparent Kd of 1.14×10-7 M. As a preliminary study, myelin butanol extracts were separated into a lipid and protein fractions with ice-cold ether treatment, and then the 14C-tryptamine binding capacities of both fractions were examined. The results indicated that only the lipid fraction possessed a tryptamine binding capacity and a chromatographic profile similar to the original butanol extracts. Moreover, the heat-treated preparation of myelin extracts also retained the tryptamine binding capacity. All these observations suggest that the myelin butanol extracts have a specific binding capacity for tryptamine, and its binding components may be lipid in nature.抄録全体を表示PDF形式でダウンロード (372K) -
Krishnaswami RAMABADRAN, Joseph J.C. JACOB1982 年 32 巻 6 号 p. 1059-1065
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーLow doses of 5-methoxy-N, N-dimethyltryptamine (5-MeODMT), quipazine and cyproheptadine produced facilitation of jumping in mice using the hot plate method. Higher doses produced severe motor disturbances which precluded the assessment of effects on nociception. The observed hyperalgesia might be a consequence of diminution of serotoninergic tone resulting either from triggering of presynaptic serotoninergic receptors in the case of 5-MeODMT and quipazine or from the blockade of postsynaptic serotoninergic receptors in the case of cyproheptadine. The 5-MeODMT-induced hyperalgesia was not attenuated by buprenorphine, which under similar conditions antagonized completely the hyperalgesic effects of naloxone; thus, the hyperalgesic effects of 5-Me-ODMT do not seemingly involve opioidergic receptors.抄録全体を表示PDF形式でダウンロード (400K) -
Hisashi KURIBARA, Sakutaro TADOKORO1982 年 32 巻 6 号 p. 1067-1074
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーEffects of gamma-1-glutamyltaurine (GT: Litoralon; Chinoin, Hungary) on rat's operant responses maintained under two types of negative reinforcement (avoidance) schedules: Sidman-type and discriminated avoidances and two types of positive reinforcement schedules and/or conflict schedules: differential water reinforcement of low rate (DRL 20 sec) and multiple fixed ratio 15/fixed ratio 15-punishment (MULT FR 15/FR 15-punishment) schedules were investigated to assess the central effects of GT. GT at 0.1-10 mg/kg i.p. induced no change in either the avoidance or DRL 20 sec responses. However, GT induced a prominent increase in the punished response (anticonflict effect) without eliciting a marked change in the non-punished response on the MULT FR 15/FR 15-punishment schedule. This behavioral change appeared not immediately, but gradually, when doses of more than 1 mg/kg were given; and a maximum level was achieved on days 3-6 and persisted for 7-14 days after the administration. The anticonflict effect of GT was synergistic with that of diazepam, a prototype antianxiety drug. No marked change in gross behavior was observed after GT. The present results suggest a possibility that GT has a central effect which correlates to the anticonflict effect.抄録全体を表示PDF形式でダウンロード (421K) -
Ryozo OISHI, Noriko SUENAGA1982 年 32 巻 6 号 p. 1075-1081
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーWhen studying the role of the locus coeruleus (LC) in the regulation of seizure susceptibility in rats, we found that bilateral LC lesion significantly lowered the electroshock seizure threshold for the tonic extension of forelegs. The pattern of maximal electroshock seizure was not affected by LC lesion, although the recovery time was slightly prolonged. In the pentylenetetrazol (PTZ) seizure threshold test, LC lesion significantly elevated the twitch threshold, but did not affect the threshold for the generalized clonic seizure or clonic convulsion. Incidence of the tonic extension in the PTZ seizure test tended toward an increase with LC lesion. Biochemical determinations revealed that LC lesion significantly decreased the norepinephrine contents in various brain regions as well as the 5-hydroxytryptamine contents of some brain regions, but not the 5-hydroxyindoleacetic acid contents. These results suggest that while the LC is involved in the regulation of seizure susceptibility, the involvement differs with various types of seizures.抄録全体を表示PDF形式でダウンロード (378K) -
Motoki KOBAYASHI, Katsuya OHATA1982 年 32 巻 6 号 p. 1083-1092
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーFour uterine-contractile substances (a, b, c and d) were extracted from procedures with acetic acid, n-butanol, distilled water, and methanol from the reaction mixture obtained by incubating rat plasma kininogen with the kininforming enzyme in the rat stomach. Gradient and equilibrium chromatography on SP-Sephadex C-25 columns were carried out with the extract containing these materials (a, b, c and d). The materials could not be separated by chromatography on SP-Sephadex C-25, but were separated by high performance liquid chromatography (HPLC) with a Zorbax ODS reversed-phase column. All the materials (a, b, c and d) contracted the rat uterus and relaxed the rat duodenum. The uterine-contractile activity of the materials was abolished by chymotrypsin, but not by trypsin treatment. The retention times of materials a, c and d on HPLC were different from that of kallidin, MLBK, bradykinin (BK) and neurotensin; but the retention time of material b was equal to that of BK. The content ratio of a: b: c: d was 4: 4: 67: 25, calculated from the uterine-contractile activity of these materials. The apparent molecular weight of the major material c, estimated by gel chromatography, was 1650. Material c contracted the rat uterus (1.2×10-10 g/ml), relaxed the rat duodenum (2×10-10 g/ml), and produced a fall in rabbit blood pressure (4.4×10-8 g/kg). Material c was classified as a biologically BK-like peptide which is distinct from kallidin, MLBK, BK and neurotensin.抄録全体を表示PDF形式でダウンロード (575K) -
Masakatsu TACHIBANA, Yasumichi HAGINO1982 年 32 巻 6 号 p. 1093-1101
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーEffects of adrenergic agents on α- and β-adrenergic receptors of parotid glands from hypothyroid rats were compared with those of euthyroid rats. The sensitivity for amylase release from parotid slices to adrenergic agents did not change even in hypothyroid status because ED50 values for amylase release in both groups were approx. the same: 7×10-8 M for isoproterenol, 4-6×10-6 M for phenylephrine and 10-5 M for methoxamine. However, the responsiveness of the tissue to those agents which was determined as the maximal amylase release was significantly higher in hypothyroid status than in the euthyroid status. The maximal increases in amylase release in euthyroid and hypothyroid rats were approx. 7.4% and 10.0% of the total in isoproterenol, 3.9% and 7.4% of the total in phenylephrine and 1.3% and 2.7% of the total in methoxamine, respectively. The effect of dibutyryl cyclic AMP mimicked that of isoproterenol, and the responsiveness of the tissue in this case was much higher in the hypothyroid rats than in the euthyroid rats. Furthermore, 10 mM tolbutamide, which completely inhibited the activity of cyclic AMP-dependent protein kinase, blocked isoproterenol-induced amylase release by 66.5% in euthyroid rats, against only 36.3% in hypothyroid rats. These results strongly suggest that the regulation mediated through β-adrenergic receptors plays a major role in amylase release from rat parotid glands even under hypothyroid status, and the step following cyclic AMP synthesis might, at least in some way, be involved in this regulation.抄録全体を表示PDF形式でダウンロード (490K) -
Yasumichi HAGINO, Masakatsu TACHIBANA1982 年 32 巻 6 号 p. 1103-1110
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe present study was undertaken to examine the phosphorylation of the parotid microsomal fraction from normal and hypothyroid rats and also to compare the effects of cyclic AMP and tolbutamide on the protein phosphorylation in the two groups. After incubation in the presence of cyclic AMP, an increased rate of phosphorylation of three protein bands was revealed by sodium dodecyl sulfate polyacrylamide gel electrophoresis and autoradiography. The apparent molecular weights of these proteins were 33, 500, 26, 000 and 19, 000. The small protein band of 17, 000 daltons decreased in 32P incorporation in the presence of cyclic AMP. Tolbutamide specifically inhibited 32P incorporation into the three proteins from normal rats, whereas the rate of phosphorylation of these proteins from hypothyroid rats remained essentially the same as that of the control, even in the presence of tolbutamide. These findings strongly suggest the possibility that stimulation of amylase release by the β-adrenergic agonist or cyclic AMP was associated with phosphorylation of the three parotid microsomal proteins and that cyclic AMP-dependent, tolbutamide-resistant phosphorylation of these proteins from hypothyroid rats plays an important role in the increased responsiveness to β-adrenergic stimulation.抄録全体を表示PDF形式でダウンロード (455K) -
Hiroyuki YOSHIMURA, Nobuya OGAWA1982 年 32 巻 6 号 p. 1111-1116
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe resident-intruder paradigm was employed in order to evoke an agonistic behavior in mice. In this situation a resident male mouse has been cohabiting with a female for 5 weeks, and an intruder male mouse is introduced into the resident's home cage. A species-specific pattern of agonistic behavior was observed in all mice. The significance of cholinergic mechanisms in the mediation of the agonistic behavior was evaluated by pharmacological manipulations. Drugs were administered to resident mice. Scopolamine hydrobromide (0.25, 0.50 and 0.75 mg/kg, i.p.) significantly suppressed the resident's aggressive episodes (offensive sideways posture, tail rattling and attack biting) in a dose-dependent manner, whereas the peripheral anticholinergic drug methylscopolamine nitrate (0.25, 0.50 and 0.75 mg/kg, i.p.) was ineffective. On the other hand, the resident's locomotor activity and rearing response were significantly increased after the administration of scopolamine hydrobromide. The evidence suggests that brain cholinoceptive mechanisms may participate in the regulation of intraspecies aggressive behavior. However, it appears that other nonspecific behavioral effects of scopolamine cannot be ruled out.抄録全体を表示PDF形式でダウンロード (336K) -
Hiroichi NAGAI, Tamotsu TAKIZAWA, Takeshi NISHIYORI, Akihide KODA1982 年 32 巻 6 号 p. 1117-1124
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe experimental glomerulonephritis was caused by the intravenous injection of a subnephrotoxic dose of nephrotoxic serum in the mice which had been previously immunized with rabbit IgG and complete Freund's adjuvant. The elevation of urinary protein excretion, serum blood urea nitrogen level and cholesterol level and the decrease of serum albumin level were demonstrated in nephritic mice. Hypercellularity in the glomerulus and hyalinosis in tubular system were observed in histopathological studies. The clinical signs in this experimental model were similar to human glomerulonephritis. In a transfer experiment, sensitized lymphocytes against rabbit IgG were necessary for the onset of disease. Clear remission of glomerulonephritis was indicated by the administration of cyclophosphamide or 6-mercaptopurine. Glucocorticoids showed moderate suppression of the development of this nephritis. These evidences suggest that this experimental model is useful for the immunopharmacological research of glomerulonephritis.抄録全体を表示PDF形式でダウンロード (399K) -
Tsugutaka ITO, Kiyoshi FURUKAWA, Tadahiko KARASAWA, Toshiaki KADOKAWA, ...1982 年 32 巻 6 号 p. 1125-1133
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーEffects of the drugs affecting monoaminergic neurotransmission were examined on the spinal polysynaptic reflex (PSR) in anesthetized spinal rats. Chlorpromazine HCl (0.5-2.0 mg/kg, i.v.) and baclofen (0.63-2.5 mg/kg) depressed and imipramine HCl (1.25-5.0 mg/kg) increased the amplitude of PSR in acute spinal animals, recorded as evoked electromyogram in the gastrocnemius muscle by electrical stimulation of the common peroneal nerve. However, chlorpromazine and imipramine showed effects neither on PSR in chronic spinal rats, nor in acute spinal rats with the intracisternal administration of 6-hydroxydopamine, which caused depletion of the spinal noradrenaline, dopamine and serotonin, and selective depletion of the spinal noradrenaline, respectively. Baclofen depressed the amplitude of PSR in both preparations with almost the same potency as that in acute spinal ones. Imipramine HCl (2.5 mg/kg, i.v.), chlorpromazine HCl (1.0 mg/kg) and baclofen (1.25 mg/kg) depressed the mono- and polysynaptic heights of the ventral root potentials in acute spinal rats. However, their depression of polysynaptic height was not so strong. These observations strongly suggest that, at the receptor sites on spinal interneurons where the descending monoaminergic neurons terminate, spinal monoamines, especially noradrenaline, are involved in PSR modification by chlorpromazine and imipramine, but not in PSR depression by baclofen.抄録全体を表示PDF形式でダウンロード (449K) -
Ken-ichi SASAKI, Shinobu FURUSAWA, Giichi TAKAYANAGI1982 年 32 巻 6 号 p. 1135-1142
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe effect of lipopolysaccharide (obtained from Escherichia coli, LPS) on the antitumor activity, acute toxicity and metabolism of tegafur was investigated in mice in comparison with 5-fluorouracil (5-FU). It was found that the intravenous administration of LPS (1.25 or 2.5 mg/kg) 24 hr prior to tegafur decreased the antitumor activity of tegafur against the solid form of Sarcoma 180. On the acute toxicity of tegafur or 5-FU, the lethality of the former was decreased and that of the latter was enhanced by the pretreatment with LPS 24 hr before. In LPS-treated mice, after the administration of tegafur, the level of tegafur in plasma was higher and the elevated level maintained longer than in untreated mice; and a small amount of 5-FU was released. A high level of 5-FU in plasma after the administration of 5-FU was also observed in LPS-treated mice. In the liver and kidneys of LPS-treated mice, the level of 5-FU after the administration of tegafur or 5-FU was higher, and its conversion of 5-FU to fluorouridine (FUR) was lower than that of control mice. On the other hand, LPS inhibited significantly the hepatic drug-metabolizing enzymes 24 hr after. It can, therefore, be presumed that the antitumor activity of tegafur was affected with LPS as a result of inhibition of conversion from tegafur to 5-FU or from 5-FU to FUR mainly according to depression in the hepatic drug-metabolism.抄録全体を表示PDF形式でダウンロード (421K) -
Fukio KONNO, Issei TAKAYANAGI1982 年 32 巻 6 号 p. 1143-1150
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーWe studied the effects of morphine, codeine and codeine-7, 8-oxide (codeine-epoxide) on the stimuli-induced 45Ca2+ uptake into the synaptosomes isolated from naive and tolerant rats and clarified the relationship between pharmacological responses of opiates and synaptosomal 45Ca2+ uptake. In vitro additions of morphine and codeine-epoxide inhibited the synaptosomal 45Ca2+ uptakes induced by two stimuli, that is, high KCl and veratrine in a concentration-dependent manner; and the inhibitions could be reversed by naloxone. However, the inhibitory action of codeine was less than that of morphine and codeine-epoxide. Since the potency ratios of the anti-nociceptive action of opiates are higher in the order of morphine>codeine-epoxide>codeine, the inhibitory effect of opiates on synaptosomal 45Ca2+ uptake may partly relate to their antinociceptive action. On the other hand, opiates significantly increased synaptosomal 45Ca2+ uptake when animals were rendered tolerant to their antinociceptive action, and data showed that the elevation of stimuli-induced 45Ca2+ uptake into the synaptosomes isolated from tolerant animals may reflect the degree of antinociceptive tolerance. Our results support the hypothesis that some of the pharmacological effects of opiates may be attributable to its ability to affect calcium accumulation in synaptosomes.抄録全体を表示PDF形式でダウンロード (429K) -
Yumiko ISHII, Issei TAKAYANAGI1982 年 32 巻 6 号 p. 1151-1155
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーThe anterior byssus retractor muscle (ABRM) of Mytilus edulis has specific dopamine receptors. We carried out a radioligand binding assay for dopamine receptors in ABRM using (3H)-haloperidol as the radioligand. High affinity binding of (3H)-haloperidol has been shown. Scatchard analysis showed a single component of binding with an apparent equilibrium constant (KD) of 1.6 nM and a maximal number of binding sites (Bmax) of 219 fmoles/mg protein. Some dopamine antagonists displaced 3 nM (3H)-haloperidol binding, and the IC50 and Ki-value of these drugs were calculated. Considering these results, this muscle is thought to be suitable for a study of the dopamine receptors.抄録全体を表示PDF形式でダウンロード (228K) -
Masanori SHIMOYAMA, Shozo KITO, Eiko ITOGA, Takenobu KISHIDA, Koji NAN ...1982 年 32 巻 6 号 p. 1157-1166
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーIn the regional distribution of /-3H-quinuclidinyl benzilate (3H-QNB) binding in human brains of neurologically unaffected cases, it was highest in the caudate nucleus which was followed by the putamen, amygdala, cerebral corteces and olfactory bulb and lowest in the substantia nigra. As to the regional distribution of 3H-spiroperidol binding in human control brains, it was highest in the caudate nucleus and was followed by the cerebral corteces, amygdala and lowest in the cerebellar cortex. In a case of striatonigral degeneration (SND), 3H-QNB binding in the putamen and thalamus was lowered and 3H-spiroperidol binding was decreased in the putamen, frontal and parietal corteces, Ammon's horn, amygdala and substantia nigra as compared to human brains of control cases. These results were noteworthy since no pathological changes were observed in the thalamus, cerebral corteces, amygdala and Ammon's horn in this case. The 3H-spiroperidol binding was increased by injection of 6-hydroxy-dopamine (6-OHDA) into the substantia nigra of rat brains by 17% as compared to the contralateral intact side. Conversely, 3H-spiroperidol binding was decreased by injection of kainic acid (KA) into the striatum of rat brains by 43% as compared to the contralateral intact side. This meant that dopamine receptors labelled by 3H-spiroperidol were at least partially localized at the postsynaptic site of the nigrostriatal dopamine neuron.抄録全体を表示PDF形式でダウンロード (480K) -
Haruyo KUNIMI, Susumu OKABE1982 年 32 巻 6 号 p. 1167-1170
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (159K) -
Kazuyoshi HORISAKA, Chieko OHNO, Yumi SUGIMOTO1982 年 32 巻 6 号 p. 1171-1174
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (163K) -
Koji SAKAMOTO, Takako KASAHARA, Sadao NAKAYAMA, Yasumitsu NAKAI, Jun'i ...1982 年 32 巻 6 号 p. 1175-1178
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (263K) -
Yoshihide YAMASAKI, Osamu SHIMAMURA, Akira KIZU, Masao NAKAGAWA, Hamao ...1982 年 32 巻 6 号 p. 1179-1181
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (158K) -
Einosuke TANAKA, Haruki KINOSHITA, Takemi YOSHIDA, Yukio KUROIWA1982 年 32 巻 6 号 p. 1182-1185
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (143K) -
Yoshikatsu MASUDA, Shigeo MURAI, Tadanobu ITOH1982 年 32 巻 6 号 p. 1186-1188
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (152K) -
Kazuko MURATA1982 年 32 巻 6 号 p. 1189-1192
発行日: 1982年
公開日: 2006/11/07
ジャーナル フリーPDF形式でダウンロード (182K)
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