All issues
Volume 94 (1989)
- Issue 6 Pages 329-
- Issue 5 Pages 257-
- Issue 4 Pages 207-
- Issue 3 Pages 159-
- Issue 2 Pages 91-
- Issue 1 Pages 1-
Volume 94, Issue 5
Displaying 1-7 of 7 articles from this issue
- |<
- <
- 1
- >
- >|
-
Akira OHGA, Shigeo ITO1989Volume 94Issue 5 Pages 257-268
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSThe smooth muscles of the gastrointestinal tract and blood vessels are innervated by nonadrenergic, non-cholinergic (NANC) inhibitory neurons. The transmitter (s) in relation to NANC inhibitory neurons remains unknown, but there are two main working hypotheses, the purinergic and VlPergic nerve hypotheses, at present. Although there is a large amount of data supporting the purinergic hypothesis, definitive evidence is still lacking. VIP seems to be regarded as a likely candidate for the neurotransmitters of some NANC inhibitory neurons. However, the data presented are still incomplete. For the purinergic hypothesis, the discrepancies seem to be greater in the stomach and oesophagus and those for the VlPergic hypothesis, in the guinea pig taenia coli. Moreover, there are many examples of the co-existence of peptides or of peptides and synthesizing enzymes of amines or acetylcholine in the gastrointestinal tract. Therefore, it is possible that NANC inhibitory neurons liberate more than one active inhibitory substance and/or there are different types of NANC inhibitory neurons in the gastrointestinal tract. Much more evidence seem to be needed before the neurotransmitter (s) of NANC inhibitory neurons in the gastrointestinal tract and blood vessels can be identified.View full abstractDownload PDF (9456K) -
Takemi FUKUDA, Yasuto MORIMOTO, Toshihiko MORIMOTO, Hidenori SHOJI, Sh ...1989Volume 94Issue 5 Pages 269-280
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSN-[(1-butyl-2-pyrrolidinyl) methyl]-2-methyl-5-sulfamoyl-2, 3-dihydrobenzofuran-7-carboxamide hydrochloride (Y-20024) was synthesized in our laboratories in anticipation of developing a new psychotropic drug. In the present study, the pharmacological properties of Y-20024 were compared with those of sulpiride (SPR) and haloperidol (HPD). Administered orally, Y-20024 was 10 times stronger than SPR in inhibiting apomorphine (0.5 mg/kg, s.c.) -induced hyperactivity in mice; administered intravenously or intracerebroventricularly, it was 2 times or one third as strong, respectively. Y-20024 was almost equipotent to SPR in antagonizing apomorphine (0.1 mg/kg, s.c.)-induced vomiting in dogs. Combined with methamphetamine (5 mg/kg, i.p.), Y-20024 and SPR induced mortality dose-dependently in rats, but HPD did not. The mammotropic activity of Y-20024 administered orally once a day for 5 days was almost equipotent to that of SPR. From these results, Y-20024, pharmacologically similar to SPR, but superior in bioavailability and penetration through the blood brain barrier, may have potential usefulness as an antipsychotic drug.View full abstractDownload PDF (8361K) -
Mitsuo UMEMOTO, Shigeru NAKAMURA, Shigetoshi OKUMURA, Tamayo SEKIGUCHI ...1989Volume 94Issue 5 Pages 281-287
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSDirect measurements under a microscope have been employed to evaluate experimental gastric ulcers, but the following problems have been left unsettled: it takes too much time, and much experience is required to perform accurate, objective measurements. The present study demonstrates the usefulness of image analysis technology for evaluating anti-ulcer drugs. With this newly developed method, the region of gastric mucosal injury can be automatically and/or mechanically chosen on the basis of three different factors: intensity, hue and purity. Consequently, this method can be used to rapidly obtain analytical data such as the number, area and length of gastric ulcers. Effect of NNP, a preparation containing aldioxa, on three different types of experimental ulcer formation (stress-induced, ethanol-induced, and pylorus-ligation) was studied by image analysis technology. In all cases, NNP (2, 562 mg/kg, p.o.) almost completely inhibited the formation of rat gastric ulcer. From the finding that image analysis technology is very useful for evaluating anti-ulcer drugs, we conclude that this method will help further the development of anti-ulcer drugs.View full abstractDownload PDF (4965K) -
Sadao NAKAYAMA, Kyoko KODAMA, Katsuji OGUCHI1989Volume 94Issue 5 Pages 289-297
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSThe effect of human placenta hydrolysate (Laennec) on residual liver regeneration after about 70% partial hepatectomy (PH) in normal and CCl4-induced cirrhosis rats was examined. Both intravenous or subcutaneous injections of Laennec increased the regeneration rate of the residual liver after PH in normal rats. Intravenous injection of Laennec inhibited the decrease of liver total protein, and it decreased the level of serum transaminase (GOT, GPT). The regeneration rate of the residual liver after PH in CCl4-induced cirrhosis (CCl4-PH) rats increased by intravenous or subcutaneous injection of Laennec. Laennec also inhibited the increase of serum GOT caused by CCl4-PH. In the pathological examination of the regenerating liver, intravenous injection of Laennec minimized the pathological changes caused by PH or CCl4-PH such as vacuolation and necrosis in the hepatocytes. The enhancement of cytoplasma regeneration in hepatocytes was noticed by intravenous injection of Laennec, but that by subcutaneous Laennec was slight. Intravenous injection of Laennec also minimized the lipid deposition in liver caused by CCl4-PH. Laennec had no effect on the pseudolobule formation caused by CCl4. Thus, the effect of intravenous injection of Laennec on the liver regeneration in PH rats was much more potent than that by the subcutaneous injection.View full abstractDownload PDF (7244K) -
Kazushi KUSHIKU, Masayoshi ABE, Hideji MORISHITA, Tatsuo FURUKAWA1989Volume 94Issue 5 Pages 299-307
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESS1) In pentobarbital-anesthetized dogs, intravenous administration of CN-100 at 40 mg/kg exhibited a transient hypotension, accompanied with a slight respiratory excitation and a temporal increase of heart rate followed by slight and gradual decrease at 20 and 40 mg/kg. 2) In isolated guinea pig atria, CN-100 (10-4, 10-5g/ml) decreased the heart rate, without influencing the myocardial contraction. 3) In anesthetized dogs, the vertebral and carotid blood flow slightly and gradually increased at 5 ?? 20 mg/kg and decreased at 40 mg/kg. The drug at 20 mg/kg similarly increased the femoral flow. 4) In anesthetized dogs, CN-100 (40 mg/kg) slightly potentiated hypertensive responses to noradrenaline and adrenaline, without affecting heart rate responses to these amines. 5) In anesthetized dogs, CN-100 (40 mg/kg) scarcely had effect on the blood pressure rise and bradycardia induced by respective proximal and distal end stimulation of the severed vagus nerve, but enhanced the hypertension due to the carotid sinus reflex. CN-100 augmented the tachycardia elicited by pre- and postganglionic stellate stimulation in spinal dogs. 6) In isolated guinea pig trachea muscle, CN-100 (3×10-6 g/ml) reduced the resting tone and relaxation response to noradrenaline, but slightly enhanced contractile responses to field stimulation and acetylcholine. 7) These results suggest that CN-100 exerts weak cardiovascular and autonomic nervous actions.View full abstractDownload PDF (6510K) -
Mitsuo MURAYAMA, Yoshinori NAMIKI1989Volume 94Issue 5 Pages 309-317
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSThe analgesic effect and the acute toxicity of a medical drug “kako-bushi-matsu” (S-01), which was produced through several processings of raw aconite roots, were examined in comparison with those of ibuprofen, indomethacin and aspirin. S-01 (p.o.) inhibited the acetic acid- and phenylquinone-induced writhing dose-dependently. From the ED50 values, indomethacin showed more potent inhibitory action on the phenylquinone-induced writhing than on the acetic acid-induced writhing. Ibuprofen and aspirin showed the same tendency as indomethacin. The potency of the writhing inhibition by S-01 was almost to the same degree in both writhing methods. In the tail pressure method, S-01 raised the pain threshold ratio to almost the same degree as ibuprofen did. In Randall-Selitto's method, the analgesic effect of S-01 on inflamed foot was less than that of ibuprofen. In the normal foot, S-01 raised the pain threshold ratio dose-dependently, but ibuprofen did not influence the pain threshold ratio. On adjuvant-induced arthritic pain, S-01 and ibuprofen had an analgesic action, and this action of S-01 was less than that of ibuprofen. The oral LD50 value of S-01 was more than 10, 000 mg/kg in mice and rats of both sexes. The above evidence indicates that S-01 has analgesic action and suggests that the mode of the analgesic action of S-01 may differ from those of ibuprofen, indomethacin and aspirin, which inhibit prostaglandin biosynthesis.View full abstractDownload PDF (6209K) -
Koichi OTANI, Noriko SHIMA, Masami DOTEUCHI1989Volume 94Issue 5 Pages 319-328
Published: 1989
Released on J-STAGE: February 20, 2007
JOURNAL FREE ACCESSAntagonistic actions of S-145 ((±)-5(Z)-7-[3-endo[(phenylsulfonyl)aminoJbicyclo[2.2.1]hept-2-exo-yl]heptenoic acid) against U-46619, a thromboxane A2 mimic, were studied using isolated thoracic aorta of the rat and the trachea, lung parenchyma and ileum of the guinea pig. S-145 as well as SQ-29548 and ONO-3708 inhibited the contraction of aorta induced by U-46619 in a concentration-dependent manner. The IC50 value of each compound was 1.4, 14.5 and 52.6 nM. S-145 also inhibited contractions of the aorta induced by high concentrations of PGE1, PGE2 and PGF2α, but failed to affect the responses to K+, Ca2+, NE, 5-HT, and angiotensin II. Contractions of trachea and lung parenchyma of the guinea pig induced by U-46619 were concentration-dependently. inhibited by S-145, but those induced by histamine and leukotriene D4 were not affected. Ileac contractions by PGE2 and PGF2α were not inhibited by S-145. The(+)-isomer of S-145 was more potent and the(-)-isomer was less potent than S-145 for antagonistic action against U-46619. These results suggest that S-145 is a potent and specific antagonist to the thromboxane A2 receptor; and in the aorta, the thromboxane A2 receptor may respond to high concentrations of PGs.View full abstractDownload PDF (6348K)
- |<
- <
- 1
- >
- >|