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Volume 78 (1981)
- Issue 5-6 Pages 393-
- Issue 4 Pages 231-
- Issue 3 Pages 127-
- Issue 2 Pages 57-
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Volume 78, Issue 5-6
Displaying 1-24 of 24 articles from this issue
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Shuichi TAKEDA, Takeshi ABE, Masamichi OTSUKA1981 Volume 78 Issue 5-6 Pages 393-401
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSTo assess the absorption of drugs given in capsule form to rats, the method of administration was studied using gastric-cannulated rats. The body weight of these rats remained the same as even when given casein hydro-Iysate and vitamins in addition to the usual chow diet. Indomethacin (IM) capsule (2mg/capsule) was given and the plasma concentration and anti-inflammatory action of IM were studied. The maximum plasma concentration was seen at 2hr after administration of one capsule. The carrageenin-induced edema of rat hind paw was inhibited with the ingestion of only one capsule. In addition, the time course of the plasma concentration of IM correlated with that of the inhibitory effect of carrageenin-induced edema. In the case of administration of a barium sulfate capsule to the cannulated rats, the transfer of the barium sulfate was clearly observed on the X-rays. Our findings suggest that this approach to the estimation of drugs is feasible, at least in experimental animals.View full abstractDownload PDF (1361K) -
General pharmacological actionMasakazu HOJO, Yoichi YOSHIDA, Yasunori NAGASAKA, Osamu KATAYAMA, Isao ...1981 Volume 78 Issue 5-6 Pages 403-429
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe general pharmacological actions of LM-209 were studied in rats, cats, dogs, guinea pigs and mice and the findings were compared with data on clemastine fumarate (CL). LM-209 but not CL produced a slight increase in pulse pressure and tachycardia. Inhibitory effects of LM-209 against contraction of the vas deferens and nictitating membrane, mainly dominated by sympathetic innervation, were remarkably less potent than CL. Inhibitory effects of LM-209 in the gastrointestinal tract were slightly more potent than CL. LM-209 accelerated norepinephrine-induced pressor reaction, while CL inhibited these effects at the dose level inhibiting histamine-induced depressor reaction. At the oral dose level showing anti-histaminic and anti-allergic actions, LM-209 but not CL had slight anti-tussive action, in an experimental model. Local anesthetic action of LM-209 was slightly more potent than that of lidocaine. LM-209 showed the same properties and potencies as CL, in most of the general pharmacological experiments.View full abstractDownload PDF (2155K) -
Pharmacological actions of a main metabolite of LM-209, Mequitazine sulfoxide (LM-209 SO)Masakazu HOJO, Yasunori NAGASAKA, Osamu KATAYAMA, Isao SERIZAWA1981 Volume 78 Issue 5-6 Pages 431-438
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe pharmacological action of a main metabolite of Mequitazine (LM-209), Mequitazine sulfoxide (LM-209 SO), was compared with data on LM-209 to investigate whether LM-209 is metabolized in vivo to the active form and if it has. pharmacological actions. In the excised ileum of guinea-pigs, the anti-histaminic and anticholinergic activities of LM-209 SO were about 1/8 and 1/20, respectively, of LM-209. The protective activity of LM-209 SO on sudden death induced by histamine in mice was about 1/2.5 of LM-209. Acute toxicity of LM-209 SO given orally to mice was 1/3 of LM-209. In the EEG of rabbits, LM-209 SO did not affect the spontaneous pattern or the arousal and recruiting responses. The mydriatic and local anesthetic activities of LM-209 SO were significantly less than those of LM-209. Thus, the pharmacological activities and toxicity of LM-209 SO were significantly less potent than those of LM-209.View full abstractDownload PDF (630K) -
Immunostimulating actions of NeurotropinYukiyoshi YANAGIHARA, Takao SHIDA, Haruo YOSHII1981 Volume 78 Issue 5-6 Pages 439-449
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSNeurotropin (NSP) is an extract isolated from vaccinia virus-inoculated and inflamed skin of rabbits. The present study was undertaken to examine the immunostimulating actions of NSP. NSP alone did not induce a proliferation of spleen cells from mice or human peripheral blood lymphocytes (PBL). However, NSP clearly enhanced concanavalin A (Con A)-induced proliferation of both spleen cells and human PBL, but slightly inhibited lipopolysaccharide (LPS)-induced proliferation of spleen cells. NSP reversed the decreases of Con A-induced proliferation of spleen cells pretreated with mitomycin C (MMC) in a dose of 5μg/ml or irradiated at 100 to 500R, while NSP did not reverse the decreases of LPS-induced proliferation of spleen cells pretreated with MMC, in a dose of 5 to 50μg/ml, or irradiated at 100 to 1000R. NSP enhanced in a dose-dependent fashion one-way mixed lymphocytes culture (MLC) reaction using MMC-treated spleen cells from BDF1 mice as stimulator cells and those from C57BL/6 mice as responder cells, respectively. NSP reversed the considerable decrease of MLC-mediated proliferation of responder cells pretreated with MMC, in a dose of 5 to 10μg/ml, or irradiated at 100 to 250R. These results indicate that NSP activates T cell function participating in cellmediated immunity.View full abstractDownload PDF (744K) -
Effect of Neurotropin on graft-versus-host reactionYukiyoshi YANAGIHARA, Takao SHIDA, Haruo YOSHII1981 Volume 78 Issue 5-6 Pages 451-458
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSIt was reported that Neurotropin (NSP) is a new immunostimulating agent which reverses the decrease of proliferation of irradiated spleen cells from mice caused by concanavalin A or specific antigen. The present study was undertaken to examine the possibility that NSP prevents graft-versus-host reaction (GVHR) through host-versus-graft reaction (HVGR) in mice. Allogeneic (C3H/He) spleen cells were transferred intravenously into 900 R-irradiated recipient mice (BALB/c). Systemic GVHR was clearly prevented by NSP as well as by cyclophosphamide or prednisolone administered intraperitoneally into irradiated recipient mice. In recipient mice irradiated with 1000 R, a more remarkably systemic GVHR was induced as compared to recipients irradiated at 250 to 500 R. NSP suppressed the proliferation of donor cells at the induction phase of GVHR, whereas NSP did not inhibit both systemic and local GVHRs induced by cell transfer at the effector phase. A decrease in hematopoietic function following irradiation or dosing with immunosuppressive drugs was also reversed by NSP. However, NSP had no effect on increases in hematopoietic function mediated by syngeneic bone marrow transplantation into 900 R-irradiated mice. These results strongly suggest that the inhibition of allogeneic GVHR by NSP is responsible for the suppression of donor cell proliferation by adequately restoring immunologic function in irradiated recipient mice, namely HVGR.View full abstractDownload PDF (535K) -
Tsuyoshi NAGASE, Masashi SASA, Shuji TAKAORI1981 Volume 78 Issue 5-6 Pages 459-464
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSElectrophysiological studies were performed to elucidate effects of ifenprodil, an antivertigo drug, on neuron activity in the lateral vestibular nucleus (LVN) of cats anesthetized with α-chloralose. LVN neurons were classified into three types, according to the response pattern upon vestibular nerve stimulation: monosynaptic, polysynaptic I and polysynaptic II neurons, which fired spikes with the mean latencies of 1.07±0.12 (n=6), 2.20±0.19 (n=8) and 16.37±2.11 msec (n=7), respectively. Intravenous administration of ifenprodil up to 5mg/kg did not affect spike generation of monosynaptic neurons. Spike generation of polysynaptic I and II neurons was dose-dependently inhibited by ifenprodil up to 1mg/kg. However, increasing doses of the drug up to 5 and 10mg/kg produced complex effects such as an enhancement of the inhibitory effect in some neurons or a facilitation of responses in others. These results indicate that ifenprodil acts on the polysynaptic I and II neurons without affecting the monosynaptic neurons. It is likely that a small dose of ifenprodil may directly inhibit polysynaptic neurons and higher doses may indirectly enhance the responsiveness of the neurons, probably as a result of an increase in blood flow in the vertebral artery.View full abstractDownload PDF (420K) -
Effects of Sairei-Toh on anti-inflammatory action of glucocorticoidHiroko ABE, Yukiko KONISHI, Shigeru ARICHI1981 Volume 78 Issue 5-6 Pages 465-470
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSEffects of a “kanpo” -prescription; Sairei-Toh on the antiglanulomatous action of glucocorticoid were investigated using male rats. Sairei-Toh increased the activity of the antiglanulomatous action of dexamethasone although treatment with only Sairei-Toh showed no significant antiglanulomatous action, as compared with the controls. The granuloma formation was reduced by administration of dexamethasone 0.5mg/kg/day and Sairei-Toh for 4 days to almost the same extent as seen with 1.5mg/kg/day of dexamethasone. The concomitant administration of Sairei-Toh and dexamethasone slightly inhibited the increase in serum triglycerides as induced by dexamethasone but did not alter serum cholesterol levels. There was no apparent difference in body, adrenal and thymus weights between the rats treated with dexamethasone in combination with Sairei-Toh and those treated with only dexamethasone.View full abstractDownload PDF (346K) -
Michio KOJIMA, Yukitsuka KUDO, Ryuichi ISHIDA1981 Volume 78 Issue 5-6 Pages 471-482
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe present study was carried out to elucidate whether or whether not afloqualone has a hypnotic action because of its similarity in chemical structure to methaqualone. In the sleep-wakefulness cycles during the 8-hour observation period (9:00_??_17:00), afloqualone increased the percentages of resting (REST) and slow wave light sleep (SWLS) stages at a dose of 25mg/kg (p. o.), producing a moderate muscle relaxation. Even at a dose of 50mg/kg (p. o.) where a marked muscle relaxation was produced, afloqualone had no influence on the percentage of slow wave deep sleep (SWDS) stage, though it increased the percentage of SWLS and decreased the percentages of awake (AWK), REST and fast wave sleep (FWS) stages. On the other hand, tolperisone-HCI, chlormezanone, methaqualone and pentobarbital-Na, used as the reference drugs, all increased the percentage of SWDS stage, but either decreased or had no effect on the percentages of the other four stages at pharmacologically effective doses. From these results it was concluded that afloqualone seems to be devoid of a hypnotic action and has different effects on the sleep-wakefulness cycle than those of both the hypnotics and the other muscle relaxants used.View full abstractDownload PDF (784K) -
Ganglion blocking activity of 3-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-902) and the correlation between its blocking activity and its inhibitory activity towards urShinji KUBO, Kouji MORIKAWA, Mitsuo YAMAZAKI, Issei MATSUBARA, Hideo K ...1981 Volume 78 Issue 5-6 Pages 483-490
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe ganglion blocking activity of HSR-902, a new antispasmodic agent, was compared with those of atropine sulfate, butylscopolamine bromide, timepidium bromide, prifinium bromide and hexamethonium chloride. These agents inhibited the postganglionic action potential induced by preganglionic cervical sympathetic nerve stimulation in cat and the order of potency was as follows: hexamethonium chloride_??_timepidium bromide_??_butylscopolamine bromide>prifinium bromide>HSR-902_??_atropine sulfate. Moreover, the inhibitory activities were correlated with the inhibitory activities of these agents on urinary bladder contraction induced by pelvic nerve stimulation in cat which had been demonstrated in a previous report. On the nictitating membrane contraction induced by postganglionic cervical sympathetic nerve stimulation in cat, HSR-902 alone exhibited a slight inhibition. HSR-902, as well as tolazoline hydrochloride, an α-blocking agent, shifted the dose-response curve of noradrenaline-contraction in parallel to the right without decreasing maximal response in the isolated aorta of guinea pig, and the plots of Schild were found to be linear. These results suggested that the weak inhibitory activity of HSR-902 on urinary bladder contraction would be due to the weakness of its ganglion blocking activity and that it is a new antispasmodic agent with a slight α-blocking activity.View full abstractDownload PDF (1549K) -
Reexamination and improvement of the method to induce chronic serum sickness nephritis in ratsTadashi NAGAMATSU, Yoshio SUZUKI1981 Volume 78 Issue 5-6 Pages 491-499
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSWe have reexamined the method to induce chronic serum sickness nephritis in rats and established a new superior one. Protein- and enzymuria were used as an index for the severity of nephritis. First, according to the experimental procedure of Fennell et al., Wistar rats were preimmunized by administering serum albumin from several species (3mg/rat) incomplete Freund's adjuvant (CFA) s. c. at 2 week intervals for 6 weeks. From 2 weeks after the final administration, the animals were administered 3mg of antigen/rat i. v. every other week. Rats in the groups which received rabbit serum albumin (RSA) developed moderate nephritis 2 weeks after the initiation of i. v. administration of the antigen, although approx. 70% of the animals died. Second, according to the method of Yamamoto et al., Wistar rats were administered bovin serum albumin (BSA, 1mg/rat) s. c. in the dorsum or the footpads. Eight weeks later, the animals were administered BSA (1mg/rat) daily, i. v. The animals, preimmunized with antigen s. c. in the dorsum, developed severe nephritis 5 weeks after the beginning of the i. v. challenge of antigen. Third, we used Sprague Dawley and Donryu rats known to be more sensitive to the induction of experimental nephritis. The animals were preimmunized by s. c. administration of 3mg of RSA in CFA per rat, followed by i. v. administration of 1mg of RSA/rat every other day after 2 weeks. In both strains, proteinuria appeared 3 weeks after the initiation of i. v. administration of RSA. There after, the animals gradually developed more severe nephritis. After withdrawing i. v. administration of RSA at 7 weeks, consistent proteinuria was maintained until 29 weeks. The merits of this new method are from these results showing that chronic serum sickness nephritis can be produced in rats by shortened preimmunization and every other day i. v. administration of antigen.View full abstractDownload PDF (657K) -
Isao YAMAGUCHI, Yoshiaki AKIMOTO, Shinsuke NISHIYAMA, Masanori SATO, H ...1981 Volume 78 Issue 5-6 Pages 501-509
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSEffects of diltiazem on catecholamine (CA) release evoked by several secretagogues were investigated in cat adrenal glands perfused in situ with Locke solution. All compounds were introduced into the perfusion medium. It was found that the release of CA stimulated by either acetylcholine (ACh) (10-4M) or high K+ (56mM) was reduced by approximately 50 and 90% in the presence of 10-5 and 10-4M diltiazem respectively, while diltiazem at 10-6M exhibited little or no influence on the Ca release. In addition, diltiazem at a concentration of 10-6M or higher produced a dose-related decrease in the CA release evoked by introduction of CaCl2 (2.2mM) into nomically Ca2+-free perfusion medium. On the other hand, removal of Na+ from the perfusion medium (osmolarity was adjusted with osmotically equal amount of sucrose) caused an increase in release of CA from the glands. Diltiazem (10-5M or higher) also reduced this CA release, but its activity was weaker than those found in experiments with ACh, high K+, and Ca2+. In all cases, the effects were reversible on washout. On the contrary, diltiazem, even at a higher concentration of 10-4M, exhibited no inhibitory effect on the release of CA induced by acet-aldehyde (3×10-3M). It was suggested that diltiazem, through its Ca2+-antagonistic action, may reduce the evoked CA release which depends on extracellular Ca2+.View full abstractDownload PDF (582K) -
Masaki NAKAMURA, Yasunobu YOSHINAKA, Hideo SUZUKI, Yasushi WADA1981 Volume 78 Issue 5-6 Pages 511-519
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSIt has previously been reported that acemetacin, a carboxymethyl ester of indomethacin, is converted to indomethacin almost completely by in vivo enzymatic attack, and thus its pharmacological effects are considered to be derived from its active metabolite, indomethacin. Gastric erosions of a slight degree were observed after a single oral administration of acemetacin, whereas indomethacin induced very severe gastric erosions 3 to 5 hours after dosing. On the other hand, the degree of intestinal lesions induced by acemetacin which became apparent 24 hours after dosing were about the same as that induced by indomethacin. The same results were obtained following repeated administration of the drugs. In an in vitro study, indomethacin was found to cause a significant mucosal loss of the isolated rat's small intestine, while there were no changes observed in case of an acemetacin treatment. Indomethacin also markedly inhibited the prostaglandin formation in the gastric mucosa of the rat treated with a single oral dose of the drug. In this test, the inhibitory effect of acemetacin on prostaglandin formation was found to be about half as potent as that of indomethacin. From these data, the less gastric damaging effects of acemetacin as compared to indomethacin can be explained by the fact that acemetacin does not have direct irritative effects on the mucous membrane. Furthermore, it could be due in part to the different abilities of these two drugs to inhibit prostaglandin formation in the gastric mucosa.View full abstractDownload PDF (947K) -
Keigo HASHIMOTO1981 Volume 78 Issue 5-6 Pages 521-528
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSMale Wistar rats were trained to hold down a lever for reinforcement with food pellets. No external stimulus signalled the end of the required duration. The minimum duration required was gradually raised to, and fixed at, 2 seconds. This was achieved in about 1-2 months. At the end of pre-drug training, the average response duration was 2.06±0.03 seconds in a daily 10-minute session. Daily injections of pyrithiamine, a thiamine analog which causes a rapid depletion of the brain vitamin, were given after the daily experimental sessions. The average response duration increased significantly by the 8th day of pyrithiamine treatment (2mg/kg/day), without altering any other parameters examined. This pyrithiamine-induced change in duration, which was gradually diminished after the 14-day drug period, could be reversed with thiamine (2 doses of 5mg/kg). On the other hand, oxythiamine did not cause an increase in duration over the 14 days of daily injections. The results obtained suggest that pyrithiamine exerted significant effects on discrimination of duration or internal timing mechanism in rats at the doses used, perhaps because of the depletion of the brain vitamin.View full abstractDownload PDF (523K) -
Reiko HOBARA, Masako OKAZAKI, Hajime YASUHARA, Koji SAKAMOTO1981 Volume 78 Issue 5-6 Pages 529-538
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThiamine (T) deficient state and various functional and morphological changes in rat liver were induced, after several days, with T antagonists, oxythiamine (OT) or pyrithiamine (PT), and a thiamine deficient diet (TDD). The relationship between the extent of liver damage and T levels in blood, liver and urine were studied in OT treated rats fed a TDD (OTD group), PT treated rats fed a TDD (PTD group), OT treated rats (OT group), PT treated rats (PT group) and rats fed a TDD (TDD group). The T levels in blood and liver of OT group, PT group, OTD group, PTD group and TDD group were 89% and 91%, 76% and 88%, 25% and 14%, 33% and 16%, 24% and 15% compared with the data in the control group, respectively. Effects of OT or PT on T levels were not remarkable in some cases, and such may be due to the duration time of T antagonists, which was considered to be 3-15 hours in PT treated rats, and 0-18 hours in PT treated rats, as assessed by urinary T measurements. Treatment of T antagonist twice daily is recommended to obtain a definite T deficient state. Our results suggest that the extent of liver damage is related to the T levels in tissue.View full abstractDownload PDF (554K) -
Hiroshi OHTSUKI, Susumu OKABE1981 Volume 78 Issue 5-6 Pages 539-547
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe effects of ranitidine on gastric secretion stimulated with gastric secretagogues were studied in 6 Heidenhain pouch dogs (both male beagle and mongrel). Cimetidine was used as a reference drug. Either histamine 2HCl (40μg/kg), pentagastrin (2μg/kg) or carbachol (2μg/kg) was given intramuscularly, every 15min for 120min. Gastric juice was collected at each 15min interval and analyzed for volume, acidity and pepsin activity. Either ranitidine (0.3, 1 or 10mg/kg) or cimetidine (1or 10mg/kg), packed in a gelatin capsule, was given orally 60 min before the initial injection of each stimulant. Both ranitidine and cimetidine dosedependently inhibited histamine- and pentagastrin-stimulated gastric secretion (volume, acid and pepsin output) These agents also inhibited the carbachol-stimulated secretion, but the antisecretory effects were weak as compared with their effects on histamine- and pentagastrin-stimulated secretions. The antisecretory effect of ranitidine on each stimulant is roughly 2 to 17 times more potent than cimetidine on the basis of ED50 (antisecretory dose which inhibits gastric secretion by 50%). The antisecretory effect of ranitidine (10mg/kg) on pentagastrin-stimulated secretion was observed even 10hr after its oral administration.View full abstractDownload PDF (515K) -
Susumu OKABE, Keiichi TABATA, Hiroshi OHTSUKI1981 Volume 78 Issue 5-6 Pages 549-555
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSMale Donryu rats (200-220g) and mongrel dogs of both sexes (7-20kg) were used. Histamine-induced ulcers: Histamine 2HCI (100mg/kg) was given i. p. to 24 hr-fasted rats and the animals were killed 4 hr llater. Histamine 2HCI in beeswax (10mg/kg) was given i. m. to dogs once daily for 5 days and the animals were killed on the 6th day. Aspirin-induced ulcers: Aspirin (100mg/kg) was given p. o. to the 24 hr-fasted rats and dogs twice (15hr apart) and the animals were killed 9 hr after the second administration of aspirin. Either the length (mm) or area (mm2) of each ulcer was measured, summed, and used as an ulcer index. Cimetidine and gefarnate were used as reference drugs. Ranitidine dose-dependently inhibited both histamine- and aspirin-induced ulcers in rats and dogs. On the basis of ED50, the antiulcer effect of ranitidine on histamineinduced ulcers was about two times (in rats) or 9 times (in dogs) more potent than cimetidine. However, the antiulcer effect of ranitidine on aspirin-induced ulcers was 1.7 times more potent than cimetidine (in rats) or almost equal (in dogs) to cimetidine. Gefarnate had an insignificant effect on both histamine- and aspirininduced ulcers.View full abstractDownload PDF (486K) -
Hirokazu NAKAJIMA, Ryuko SHIGEHARA, Masatoyo SHIMADA, Yoshio TOTSUKA, ...1981 Volume 78 Issue 5-6 Pages 557-569
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSPreviously we have found such “bizarre stereotypy” as persistent and bloody biting activity at the legs or the tail of himself or of the cage mate given methamphetamine (MAPT, 10mg/kg) 24hrs-48hrs after long term-administration of reserpine (RE). The present investigation examined the effect of inhibition of dopamine synthesis in brain on MAPT-induced “bizarre stereotypy ” and hypermotility of RE-treated rats. Male albino Wistar rats aged 4 weeks were injected intraperitoneally with RE (1.25mg/kg) or 0.9% saline solution (1.25ml/kg) every two days for 13 days. Twenty-two hrs after the last injection, rats received a-methyl-para-tyrosine (α-MPT, 50mg/kg, 125mg/kg, 250mg/kg i. p.) or its vehicle (1ml/kg i. p.) and 2hrs later, MAPT. MAPT induced continuous licking and biting at the metal wire of the cage floor in salinetreated rats and also “bizarre stereotypy ” in RE-treated rats, but these activities were completely suppressed by pretreatment of α-MPT in each dose given (especially in 125mg/kg, 250mg/kg). Pertaining to the locomotor activities of saline-treated rats, the horizontal movements were especially enhanced by MAPT, however, the vertical movements remained unchanged. α-MPT partially inhibited such horizontal movements while it potentiated the vertical movements. Locomotor activities of RE-treated rats were depressed one day after the last injection of RE, however, after the MAPT, these activity counts were increased considerably and were also higher in comparison to the counts of saline-treated rats given MAPT. These hypermotilities in RE-treated rats were partially antagonized by pretreatment with α-MPT. It is suggested that MAPT-induced “bizarre stereotypy” of RE-treated rats is mediated by the accelerative effect of RE on MAPT-induced dopamine synthesis, while MAPT-induced hypermotility of RE-treated rats is partially related to such an acceleration of dopamine synthesis.View full abstractDownload PDF (887K) -
Effects of 3-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide (HSR-902) on the junctional transmission of pelvic nerve ending in isolated urinary bladderShinji KUBO, Kouji MORIKAWA, Mitsuo YAMAZAKI, Issei MATSUBARA, Hideo K ...1981 Volume 78 Issue 5-6 Pages 571-577
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSEffects of HSR-902, a new antispasmodic agent, on the junctional transmission of pelvic nerve ending in isolated urinary bladder was compared with those of atropine sulfate, butylscopolamine bromide, timepidium bromide and prifinium bromide. Tetrodotoxin (3×10-8g/ml) completely inhibited the contraction of isolated guinea pig urinary bladder induced by transmural stimulation (TM contraction), but hexamethonium chloride (1×10-4g/ml) and atropine sulfate (1×10-5g/ml) exhibited no inhibition and a slight inhibition, respectively. Neo-stigmine bromide (1×10-7g/ml) increased TM contraction, and the effect was completely inhibited by atropine sulfate (1×10-5ig/ml). Antispasmodic agents (1×10-7_??_1×10-7), excluding HSR-902, showed slight inhibition on TM contraction. In contract, HSR-902 (1×10-6_??_1×10-5g/ml) increased TM contraction and/or resting tone (1×10-5g/ml). Phenoxybenzamine hydrochloride (1×10-8g/ml) and tolazoline hydro-chloride (1×10-5g/ml), a-blocking agents, increased both TM contraction and resting tone. Increasing effects of HSR-902 on TM contraction and/or resting tone were completely inhibited by noradrenaline (1×10-5g/ml) with propranolol hydrochloride (1×10-5g/ml). These results suggested that these antispasmodic agents scarcely inhibited the junctional transmission in postganglionic cholinergic nerve ending induced by transmural stimulation of isolated guinea pig urinary bladder, and HSR-902 rather increased the transmission. Since it was also suggested that there was α-adrenoceptor inhibiting acetylcholine-release in the postganglionic cholinergic nerve terminal, the transmission increasing action of HSR-902 would be due to its a-blocking action.View full abstractDownload PDF (393K) -
Matsutaro MURAKAMI, Shiro TOMINAGA, Katsuhiro WATANABE1981 Volume 78 Issue 5-6 Pages 579-587
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe following 4 Wistar rat groups were sacrificed by microwave irradiation: 1) hypothermia-rebreathing anesthesia (kept 3hr at 4°C in a 4 1 box), 2) pentobarbital anesthesia (50mg/kg, s. c., 1hr after), 3) reserpinized rats (5mg/kg/day, s. c. for 3 days), and 4) nontreated control rats. Cyclic nucleotides and noradrenaline were analyzed in seven brain regions: cerebellum, pons and medulla oblongata, hypothalamus, mid brain, striatum, hippocampus, and cerebral cortex. In most part of the brain regions, the levels of cyclic AMP, cyclic GMP and noradrenaline had a tendency to decrease after the treatment by hypothermia-rebreathing or pentobarbital as compared with control animals. The levels of cyclic AMP in the cerebellum and cyclic GMP in the hypothalamus were not affected by these anesthesia. After reserpinization, the level of cyclic GMP markedly elevated in all regions of the brain except in the cerebellum. In all brain regions of the control and the hypothermia-rebreathing groups, the coefficients of correlation between cyclic AMP and noradrenaline, cyclic GMP and noradrenaline, cyclic AMP and cyclic GMP were positive, negative and negative, respectively. The cyclic AMP/cyclic GMP ratio in most of the brain regions decreased in the reserpinized group, and increased in the hypothermia-rebreathing group as compared to the control and the pentobarbital groups. From these results, it is postulated that some other neurons, not only monoaminergic neuron, regulate the level of cyclic nucleotides, and that the different sensitivity of these neurons to the anesthesia brings about various effects on the metabolism of cyclic nucleotides in each brain region.View full abstractDownload PDF (728K) -
Antiallergic actions of NeurotropinYukiyoshi YANAGIHARA, Takao SHIDA1981 Volume 78 Issue 5-6 Pages 589-597
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSNeurotropin (NSP) is an extract isolated from vaccinia virus-inoculated and inflamed skin of rabbits. The anti-allergic actions of NSP were studied in the present paper. Death from anaphylactic shock in BALB/c mice mediated by active systemic anaphylaxis (ASA) or heterologous passive systemic anaphylaxis (PSA) was completely prevented in one out of five cases by NSP given 5000μg/animal i. v.. However in mice, NSP at a dose of 10 to 1000μg/animal ix. did not have any preventive effect on death from anaphylactic shock induced by ASA, homologous PSA, or heterologous PSA. NSP slightly inhibited histamine release from rat mast cells mediated by mouse IgE antibody, calcium ionophore A23187, or compound 48/80, but this inhibition was not in a dose-dependent fashion. NSP did not behave synergistically with isoproterenol or theophyllineinduced inhibition of mouse IgE antibody-mediated histamine release from rat mast cells. NSP did not inhibit D2O-enhanced histamine release from sensitized rat mast cells. NSP clearly inhibited antigen-induced histamine release from leukocytes of mite-sensitive patients with or without asthmatic attack. Potent inhibition was observed when leukocytes taken from patients with asthmatic attack were used. These results suggest that the anti-allergic action of NSP is not responsible for elevation of cyclic AMP levels or disruption of microtubules in target cells.View full abstractDownload PDF (612K) -
(I) Relationship between the analgesic action of eptazocine and brain catecholamineTsutomu KAMEYAMA, Toshitaka NABESHIMA, Kazumasa YAMAGUCHI, Makoto UKAI ...1981 Volume 78 Issue 5-6 Pages 599-612
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe relationship between the analgesic action of eptazocine and brain catecholamine was investigated by pharmacological and neurochemical methods in comparison with pentazocine (PZC) and morphine (MOR). The analgesic action of eptazocine as determined by the pressure method was decreased by pretreatment with 6-hydroxydopamine (6-OHDA) or disulfiram. Eptazocine increased the norepinephrine (NE) level in the brain stem, but decreased the dopamine (DA) level in the cortex. Eptazocine decreased the rates of DA turnover in the cortex and the brain stem and NE turnover in the spinal cord. The analgesic action of PZC was decreased by α-methyl-p-tyrosine (α-MT), disulfiram, 6-OHDA, or reserpine. PZC decreased NE levels in the cortex and the brain stem, and DA level in the striatum. The turnover rates of NE in the brain stem and the spinal cord were increased by PZC. The analgesic action of MOR was potentiated by α-MT and attenuated by reserpine or 6-OHDA. MOR decreased NE and DA levels in the cortex and NE level in the brain stem, but increased DA level in the brain stem and NE level in the spinal cord. The turnover rates of NE in the cortex and the brain stem were increased at low doses of MOR, but those of DA in the striatum and NE in the spinal cord were decreased at high doses of MOR. These results suggest that the mechanism of eptazocine-induced analgesia is different from those of PZC and MOR in terms of the relationship to catecholamine neurons.View full abstractDownload PDF (758K) -
(II) Relationship between the analgesic action of eptazocine and brain 5-hydroxytryptamine (5-HT)Tsutomu KAMEYAMA, Toshitaka NABESHIMA, Kazumasa YAMAGUCHI, Katsuo KAMA ...1981 Volume 78 Issue 5-6 Pages 613-627
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe relationship between the analgesic action of eptazocine and brain 5-HT was investigated by pharmacological and neurochemical methods in comparison with pentazocine (PZC) and morphine (MOR). The analgesic effects of eptazocine, PZC, and MOR as determined by the pressure method were decreased by pretreatment with p-chlorophenylalanine or 5, 6-dihydroxytryptamine. The analgesic effects of all three drugs were also diminished by a lesion in the dorsal half of the spinal cord (C5_??_6) or the raphe magnus. A lesion in the central gray produced a decrease in the analgesic effects of MOR or PZC, but had a weak effect on that of eptazocine. All three drugs increased 5-hydroxyindole acetic acid (5-HIAA) levels in the brain stem, the striatum, and the spinal cord. In addition, eptazocine decreased the 5-HIAA Ievel in the cortex and the 5-HT level in the hippocampus, but increased the 5-HT level in the spinal cord. An increase of 5-HIAA level in the cortex and a decrease of 5-HT level in the brain stem were observed after PZC-administration. On the other hand, MOR decreased the 5-HT level in the brain stem and striatum. These results suggest that the effects of eptazocine on 5-HT neurons are similar to those of PZC and MOR, but part of the action mechanism of eptazocinc is different from those of PZC and MOR.View full abstractDownload PDF (1897K) -
(III) Central action of eptazocineTsutomu KAMEYAMA, Toshitaka NABESHIMA, Kazumasa YAMAGUCHI, Katsuo KAMA ...1981 Volume 78 Issue 5-6 Pages 629-645
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSPharmacological actions of eptazocine on the central nervous system were investigated by pharmacological and behavioral methods. Eptazocine produced sedation at low doses and Straub tail reaction in mice and ataxia in rats at high doses. In mice, eptazocine caused decreases in the spontaneous locomotor activities measured by the wheel cage and Animex methods, but caused an increase of the response in rats as determined by the open-field method. Eptazocine caused impairment of performance in the rotarod test and the traction test in mice, a decrease of activity of EMG, and an inhibition of flexor reflex in rats. Eptazocine decreased body temperature, potentiated pentobarbital-induced sleeping, and inhibited convulsion caused by pentylenetetrazol in mice. Fighting behavior induced by electric shock and central stimulation effect of methamphetamine were inhibited by eptazocine in mice. Eptazocine showed an inhibition of avoidance behavior in shuttle and skinner boxes in rats. These results suggest that eptazocine produces a non-specific inhibitory action on the central nervous system.View full abstractDownload PDF (975K) -
Susumu OTOMO, Shohei HIGUCHI, Shiro NAKAIKE, Kimiyo TAKESHITA, Makoto ...1981 Volume 78 Issue 5-6 Pages 647-658
Published: 1981
Released on J-STAGE: July 30, 2010
JOURNAL FREE ACCESSThe topical and systemic anti-inflammatory activities of hydrocortisone 17-butyrate 21-propionate (HBP) were studied. The systemic anti-inflammatory activities of HBP and reference steroids were examined for their effects on dinitrochlorobenzene dermatitis, carrageenin edema, cotton pellet granuloma and adjuvant arthritis in rats and by the delayed allergic edema test in mice. The topical anti-inflammatory activities of these steroids were examined for their effects on croton oil dermatitis, croton oil ear edema, carrageenin edema and cotton pellet granuloma in rats. Furthermore, effects of these steroids on liver glycogen deposition in mice, thymolysis, and decrease of serum corticosterone level in rats were examined. Systemically administered HBP was less potent than betamethasone 17-valerate (BV), but was almost equal to hydrocortisone 17-butyrate (HB) in anti-inflammatory activity, and its effects on liver glycogen deposition, thymolysis, and the decrease of serum corticosterone level. However, the topical anti-inflammatory activity of HBP was more potent than that of BV and HB, although in the same experiment, thymolytic activity of HBP was less potent than that of BV, but was almost equal to HB. The inhibitory effect of HBP on hypotonic induced hemolysis was weaker than that of BV, but was stronger than that of HB in vitro. The affinity of HBP was higher than that of BV and HB to polymorphonuclear leucocytes used as the inflammatory cells in vitro. On the other hand no marked difference was observed in the affinity to erythrocytes used as the non-inflammatory cells in vitro. These results suggest that HBP is a useful drug which has superior topical anti-inflammatory activity, but has a weak systemic effect.View full abstractDownload PDF (699K)
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