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Volume 75, Issue 4
Displaying 1-9 of 9 articles from this issue
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Kaito TSURUMI, Satsuki HAYANO, Junichi HASEGAWA, Hajime FUJIMURA1979 Volume 75 Issue 4 Pages 309-314
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSTo examine the effect of spasmogens on propulsive motility in the intestine, cathartic activity o drugs was investigated. Mice, rats and guinea pigs were individually observed in cages with 20 separate small rooms in which a sheet of filter paper covered the bottom of cage for observation of the feces. The effect was evaluated 1 hr after drug administration. Cathartic activity of spasmogens was the most marked in mice followed by rats, but was rarely observed in guinea pigs. Cholinergic drugs and cholinesterase inhibitors had a cathartic effect in mice and rats, but the activity differed. Drugs such as acetylcholine and physostigmine produced a low cathartic activity even at sublethal and lethal doses. Other drugs as bethanechol, pilocarpine and neostigmine had a dose dependent cathartic effect at doses below lethal ones and were found to be clinically useful for intestinal relaxation after laparotomy. Among autacoids which contract the intestine by direct action on smooth muscles, histamine and bradykinin had no cathartic effect in mice and rats. 5-HT and prostaglandin E2 were dose dependent with a marked cathartic effect in both species. 5-HTP produced the same cathartic activity as that seen with 5-HT in mice, but had no cathartic effect in rats. The cathartic effect of BaCl2 was low, but dose dependent in both species. We recommend this method for the study of the effect of various compounds on the propulsive motility of the intestine.View full abstractDownload PDF (8275K) -
Hideomi FUKUDA, Yoshihisa KUDO, Eriko TAKEUCHI1979 Volume 75 Issue 4 Pages 315-319
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffects of four benzodiazepine derivatives on γ-activity were examined in the anesthetized rat. Diazepam and 5-(o-chlorophenyl)-1-methyl-7-nitro-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one(ID-690) in a dose of 2.5 mg/kg (i.p.) showed depressant effects on γ-activity. The depressant effects of 5.0 mg/kg (i.p.) lasted for more than 60 min. Nitrazepam had a slightly weaker effect than the above two drugs and the effect was evident after an administration of 5.0 mg/kg; the effect of 10 mg/kg(i.p.) lasted for more than 90 min. The effect of clonazepam was much weaker than effects of the other three drugs. A dose of 20 mg/kg(i.p.) was required to produce an obvious depressant action, and the effect appeared after a longer latency of about 20 min. ID 690 (5.0 mg/kg, i.p.) depressed the augmented response of the γ-activity in response to pinna stimulation. The effect of diazepam on the augmented responses was observed with the same dose. In contrast, much higher doses of nitrazepam and clonazepam were required to induce an obvious depressant effect on the augmented γ-activity. It is suggested that the difference in potency in depressing γ-activity of these derivatives is one of the factors characterizing their pharmacological properties.View full abstractDownload PDF (6050K) -
Naohisa FUKUDA, Yoshiaki SAJI, Yuji NAGAWA1979 Volume 75 Issue 4 Pages 321-331
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSBehavioral and EEG changes induced by brain stem compression and the effect of TRH were studied. The compression was given for 1 to 6 min by inflating a balloon chronically implanted on the dorsal surface of the cat brain stem in the 4th ventricle via cisterna magna. Within 10 to 36 sec after the start of the compression, the cats turned sideways and became motionless in a spastic extension of four legs, and thereafter all reverted to a normal position, after 45 to 120 min, although slight movements or head-up position was observed in some animals. The cortical EEG patterns observed after the compression were initially a brief rush of low amplitude-fast waves (EEG arousal) followed by a flattened and/or spike pattern, and subsequently these shifted to high amplitude-slow waves with or without an accompanying EEG arousal. These behavioral and EEG alterations were remarkably improved by i.v. administration of TRH as follows: eight of 12 cats with 1 mg/kg and one of 4 cats with 0.5 mg/kg promptly changed from the lateral to a crouching or abdominal position, and thereafter never turned sideways again. Partial recovery such as movements of forelegs, struggling or head-up in the lateral position, rolling or slight shift of position was also observed within several min in three cats with 1 mg/kg as well as in two cats with 0.5 mg/kg. Furthermore, TRH induced a dose dependent, persistent EEG arousal in all cats. These results show that TRH ameliorates deterioration in behavior and the EEG, this deterioration being similar to clinical states of disturbance in consciousness induced by compressing the brain stem.View full abstractDownload PDF (14189K) -
Part II. Effects on the peripheral organsKoroku HASHIMOTO, Shigeyuki SHINTANI, Shuji YAMASHITA, Seiso TEI, Masa ...1979 Volume 75 Issue 4 Pages 333-364
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSPharmacological properties of procaterol (PRO) in the peripheral organs were examined in comparison with those of salbutamol (SAL) and isoproterenol (ISO). PRO slightly enhanced twitch tension of the tibialis anterior muscle but affected little the mono- and poly-synaptic spinal reflexes and ganglionic transmission. PRO depressed spontaneous contractions of the isolated ileum, non-pregnant and pregnant uterus and also the gastrointestinal and uterine movements in vivo. PRO prolonged the time of peroral charcoal transport in the intestine. Potencies of PRO in producing these effects were between those of ISO and SAL except those on the uterus in which PRO was more potent than ISO and SAL. PRO depressed gastric and bile secretion but had no effect on pancreatic secretion. ISO, PRO and SAL reduced resistance of the common carotid, femoral and renal arteries and the relative potencies of PRO and SAL to ISO were significantly less in the renal artery than in the other arteries. In accelerating heart rate in conscious rats and dogs, PRO (p.o. or s.c.) was almost equipotent to SAL. Urine flow, GFR, RPF, free water and osmolar clearance and also excretion of electrolytes were reduced by PRO with the concomitant fall of systemic blood pressure. PRO had no effect on blood coagulation and hemolysis but inhibited carrageenin edema and an increase in permeability of blood vessels induced by acetic acid. PRO had no α-adrenolytic, cholinolytic and anti-histaminic effects.View full abstractDownload PDF (36242K) -
—Biochemical and morphological changes in the thiamine deficient rat—Emiko OGUCHI, Masako OKAZAKI, Hajime YASUHARA, Koji SAKAMOTO1979 Volume 75 Issue 4 Pages 365-381
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSWe studied biochemical changes in the rat liver in a thiamine (T) deficient state as induced by oxythiamine (OT), pyrithiamine (PT) and thiamine deficient diet(TDD) and simultaneously observed morphological changes under light and electron microscope. Severe loss of weight was observed in the OT treated rats fed on TDD (OTD) and such was frequently accompanied by a complete loss of righting reflex. Biochemical changes commonly found in T deficient groups were decrease in serum total protein, alkaline phosphatase activity and liver lipids, and increase in serum total cholesterol and transaminase activity. Microscopically, most of the liver cells were atrophied and necrosis was observed in the OTD group. Electron microscopically, ultrastructural changes revealed active Kupffer cells, microvilli and Golgi apparatus, and decrease in rough endoplasmic reticulum (rER) associated with increasing detached ribosomes and smooth ER. Abnormal nucleus and mitochondria were found in the OTD group. These results suggest that a T deficiency occurs readily and easily within a short time when a T antagonist, particularly OT, is used together with the TDD, while a much longer time is required to produce a T deficiency with only the TDD.View full abstractDownload PDF (33191K) -
Kazumi AKIBA, Atsushi MIYAMOTO, Tomoharu SUZUKI, Ken ANEZAKI, Takeshi ...1979 Volume 75 Issue 4 Pages 383-390
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSThe action of d-pseudoephedrine on bronchial smooth muscle, respiratory resistance and blood pressure was compared with that of 1-ephedrine. The following results were obtained. 1) Administration of dl-isoproterenol on isolated guinea pig tracheal muscle previously constricted with acetylcholine (ACh) or histamine (His) was the most effective and d-pseudoephedrine had the same effect as 1-ephedrine. The relaxing effect of dl-isoproterenol, 1-ephedrine or d-pseudoephedrine on ACh or His induced tracheal constriction was competitively antagonized by the pretreatment of propranolol. 2) The intravenous or sublingual administration of d-pseudoephedrine on the increased respiratory resistance induced by His produced the same effect as 1-ephedrine. 3) The increase in blood pressure with d-pseudoephedrine was weaker than that of 1-ephedrine. 4) When 1-ephedrine or d-pseudoephedrine was repeatedly injected into the same animal, sighs of tachyphylaxis were observed. It was found that d-pseudoephedrine, the main alkaloid of Ephedrine Helba, exhibited the relaxing effect on bronchial smooth muscle as did 1-ephedrine. The respiratory resistance increased by His was inhibited by the sublingual administration of d-pseudoephedrine and 1-ephedrine.View full abstractDownload PDF (7829K) -
Ken ANEZAKI, Ryuichiro ANDO, Tsukasa SAKURADA, Takeshi TADANO, Shinobu ...1979 Volume 75 Issue 4 Pages 391-397
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffects of diazepam were examined on the whine reaction elicited by LH stimulation and on unit activities in the LH and Abm in cats. Results were as follows: Diazepam increased the threshold of whine reaction induced by the LH stimulation. The spontaneous firing frequency of Abm neurons was 5 to 30 spikes/sec and in all 6 neurons isolated the firing frequency increased by non-nociceptive and/or clap-stimulation. Diazepam decreased the spontaneous firing frequency of all Abm neurons isolated and the increased firing frequency elicited by non-nociceptive and/or clap-stimulation was also depressed by diazepam. The spontaneous firing frequency of neurons in the LH was 1 to 5 spikes/sec and all 6 neurons isolated firing frequency increased by non-nociceptive stimulation. Only one of 6 neurons, however, was activated by clap-stimulation. Diazepam decreased the spontaneous firing frequency of all LH neurons. Out of 6 neurons responsive to non-nociceptive stimulation, 3 were also depressed by diazepam. The other neurons were not affected by diazepam. These results suggest that depressed action of diazepam on the whine reaction elicited by the LH stimulation maybe related to the decrease of firing in the Abm and/or the LH by diazepam.View full abstractDownload PDF (7470K) -
Hideo KANETA, Kenichi KUJIRA, Toshiaki SHIGENAGA, Kimikazu ITAYA1979 Volume 75 Issue 4 Pages 399-403
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSNorepinephrine (NE) content in the brain slightly but significantly increased when γ-oryzanol (100 mg/kg, s.c.) was given once daily for 1, 5 or 10 days, while NE in the gastric area was not affected. The turnover rate of brain NE tended to decrease with the administration of γ-oryzanol. From the results, it is likely that successive doses of γ-oryzanol increase brain NE by inhibiting degradation or release of NE.View full abstractDownload PDF (4981K) -
Hideo NAKAMURA, Katsumi ISHII, Satoru MOTOYOSHI, Chieko IMAZU, Yuichi ...1979 Volume 75 Issue 4 Pages 405-417
Published: 1979
Released on J-STAGE: March 29, 2007
JOURNAL FREE ACCESSEffect of tolmetin sodium on the pain-like responses caused by various nociceptive stimuli was examined in experimental animals. Tolmetin sodium showed a potent inhibitory activity on the acetic acid-induced writhing in mice and rats, and its potency(ED50=23.4 and 3.01 mg/kg, p.o.)was about 2.4 ?? 10.3 times that of ibuprofen and aspirin. The hypertension induced by intraarterial injection of bradykinin toward the spleen of dogs was inhibited by tolmetin sodium(ED50=80 mg/kg, i.v.), but the hypertension by a simultaneous injection of bradykinin and PGE1 was not inhibited by tolmetin sodium and sulpyrine, though pentazocine inhibited both hypertensions. The pain-like response caused by pressing mechanically the inflamed paws or joints of rats induced by kaolin-carrageenin or adjuvant was inhibited by tolmetin sodium(30 ?? 100 or 20 ?? 40 mg/kg, p.o., respectively), and the potency was approximately equal that of ibuprofen and phenylbutazone. Tolmetin sodium produced a significant inhibition of the pain-like response induced by electrical stimulation of tooth pulp of dogs, but showed no effect when the methods of Haffner and D'Amour-Smith were applied to mice. Anti-writhing action of tolmetin sodium was not antagonized by naloxone. From these results, it was concluded that tolmetin sodium has a potent inhibitory activity on the pain-like responses induced by the chemical nociceptive stimuli and by the mechanical pressure stimulus of the inflamed tissue, especially on the writhing. The analgesic activity probably involves a peripheral mechanism.View full abstractDownload PDF (17185K)
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