The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Volume 25, Issue 1
Displaying 1-13 of 13 articles from this issue
  • Haruo KITAGAWA, Kaoru MIYAZU, Minoru TSURUTA, Hisashi SATOH, Tetsuyosh ...
    1975 Volume 25 Issue 1 Pages 1-14
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Absorption, distribution, excretion and metabolism after oral administration of 3H-labelled metiazinic acid were studied. The administrered radioactivity was excreted through both the urinary and fecal routes. The maximum levels of concentration in blood and most tissues were shown within 3 hr after dosing. The highest radioactivity was found in the kidney throughout all experiments. Relatively high radioactivity was observed in inflammatory-treated parts in rats. Unchanged compound, metiazinic acid S-oxide and these conjugates were found in urine and feces. Approximately 60% of the unchanged form was observed in plasma after 6 hr.
    Download PDF (469K)
  • Taichi OKA, Akira NAKANISHI, Tadao OKADA
    1975 Volume 25 Issue 1 Pages 15-24
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Pharmacological and biochemical properties were investigated on deanmino-dicarba-[Gly7]-oxytocin (Y-5350). This is a newly developed compound, in which the disulfide bond and [Pro7] of deamino-oxytocin are substituted by an ethylene linkage and glycine respectively. Bioassayed Y-5350 exhibited 202.6 u/mg of oxytocic activity, 4.6 u/mg of avian depressor activity, 441.2 u/mg of rat milk-ejecting activity and 0.02 u/mg of rat antidiuretic activity, however, a depressor activity was also evident in rats. In particular, the duration of antidiuretic activity was short. Moreover, the oxytocic activity in pregnant rats and rabbits was weak in comparison with oxytocin. Cumulative dose-response studies were carried out on the isolated rat uterus using van Dyke-Hasting solution. The intrinsic activity was the same level as that of oxytocin, and the pD2 value was 8.62. Oxytocic activity was much enhanced by the existence of 0.5 or 2 mM magnesium ion in vitro. However, the agreement between in vivo and in vitro oxytocic activity was not complete when assay was carried out in the presence of 2 mM magnesium ion. Oxytocin was inactivated by the serum of pregnant women. In the experiment using rats, oxytocin was also destroyed by the extracts of uterus, kidney and liver. In contrast, Y-5350 was not destroyed by any of the enzyme solutions mentioned above.
    Download PDF (374K)
  • Kenichiro NAKAO, Hitoshi KATO, Keijiro TAKAGI
    1975 Volume 25 Issue 1 Pages 25-34
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    The effects of beta-adrenergic receptor blocking agents administered i.v. on the blood pressure in conscious spontaneously hypertensive rats (SHR), renal hypertcnsive rats (RHR) and normotensive Wistar strain rats (NR) were studied. dl-Propranolol and dI-YB-2, 1 mg/kg i.v., caused a sustained rise in blood pressure in SHR and RHR. The maximum response of each beta-blocking agent after phentolamine, 10 mg/kg i.v., in SHR and RHR was significantly larger than that in NR. The potency ratio for the hypertensive activities of the I- and d-isomers of propranolol and YB-2 was similar to the ratio of their beta-blocking activities. The pressor effects of the beta-blocking agents after phentolamine were significantly inhibited by adrenalectomy, reserpinization and pretreatment with hexamethonium. The results suggest that the pressor effect of the beta-blocking agents may be due to their beta-blocking activities and the unmasking of alpha-receptor activities of the blood vessels. Furthermore, the greater pressor effect of the agents observed in hypertensive rats is attributed to a greater activity of the sympathetic nervous system in these rats as compared to normotensive rats.
    Download PDF (407K)
  • Tomoyoshi HOSOKAWA, Koji SUZUKI, Tsuneo OKUTOMI, Mikio SAWADA, Kunio A ...
    1975 Volume 25 Issue 1 Pages 35-39
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Ascofuranone, a fungal metabolite, significantly reduced serum lipid levels, when orally administered to male Wistar rats fed a cholesterol rich diet. The treatment also resulted in a marked reduction of hepatic and cardiac cholesterol contents without affecting the body weight gain. The serum albumin/globulin ratio increased significantly in the treated rats. This increase is presumably due to the decrease of β-lipoprotein. The mode of action differentiates from clofibrate in so far as the former effectively prevents hepatic and cardiac cholesterol deposits in the cholesterol feeding rats.
    Download PDF (169K)
  • Hisashi TAKASU
    1975 Volume 25 Issue 1 Pages 41-45
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Phospholipid metabolism in inflamed tissue of the mouse skin which had been induced by the application of 1-chloro-2, 4-dinitrobenzene (DNCB), croton oil, or irradiation of ultraviolet rays was examined, and it was found that phospholipid levels had increased in the inflamed tissues. In the case of ultraviolet rays, the increase was temporary, and the level returned to that of control after 3 or 4 days. In the case of DNCB or croton oil, the level increased after a decrease for a short period. The pattern of the increase between physical and chemical irritation was different. Increase of incorporation of 32P into phospholipid in inflamed tissue was examined, and it was observed that the level reached a maximum after one day. It is thus assumed that phospholipid plays an important role in the mechanism of inflammation.
    Download PDF (232K)
  • Yoshitsugu OSUMI, Hiroshi FUJIWARA, Ryozo OISHI, Shuji TAKAORI
    1975 Volume 25 Issue 1 Pages 47-54
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Effects of 2-chloro-l-(2, 4-dichlorophenyl) vinyl diethyl phosphate, chlorfenvinphos, on spontaneous EEG, EMG and ChE activity in the brain and red blood cells were investigated in male Wistar rats. Chlorfenvinphos up to 1 mg/kg p.o. did not affect the ChE activity and the awake-sleep cycle. In doses over 2 mg/kg, the ChE activity in the brain and red blood cells significantly decreased. The spontaneous EEG showed a prominent arousal pattern and appearance of slow wave sleep and parasleep was markedly depressed. Maximum inhibition of brain ChE activity was obtained 3 hr after the treatment and lasted for more than 72 hr. The duration of arousal pattern was proportional to the doses, however, the awake-sleep cycle returned to control on the 2nd day and a rebound increase in parasleep occurred on the 3rd day. Atropine depressed the EEG arousal pattern induced by chlorfenvinphos, without affecting ChE activity in the brain. The brain noradrenaline level was not altered with chlorfenvinphos. These results indicate that the appearance of EEG arousal pattern after chlorfenvinphos may be derived from central cholinergic activation.
    Download PDF (304K)
  • Hironori NAKANISHI, Hiroshi TAKEDA
    1975 Volume 25 Issue 1 Pages 55-61
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    The interaction of the junction potentials in response to ortho- and antidromic hypogastric nerve stimulation in mouse vas deferens was studied, using an extracellular recording method. Ortho-dromic repetitive hypogastric nerve stimulation (10 Hz, 5 min) simultaneously depressed the amplitude of the junction potentials in response to both ortho- and anti-dromic hypogastric nerve stimulation (post-tetanic depression). No time-lag in recovery from the post-tetanic depression was observed between the junction potentials recorded from two separate electrodes, indicating that the proximodistal axonal flow of available transmitter was not involved in the recovery process. Double shocks, with intervals from 10 msec to 1 sec, were applied to the hypogastric nerve. The junction potentials in response to ortho- and ortho-dromic or anti- and anti-dromic double shock were markedly facilitated. On the contrary, the junction potentials in response to ortho- and anti-dromic double shocks were not facilitated. The findings indicate, that facilitation of the junction potentials is produced by the impulses propagated in the same direction along the terminal axon and also that the origin of the facilitation may be at a pre-jtrnctional site.
    Download PDF (288K)
  • Nobuhiro INATOMI, Issei TAKAYANAGI, Keijiro TAKAGI
    1975 Volume 25 Issue 1 Pages 63-69
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Mitochondrial, microsomal and soluble fractions separated from the guinea pig taenia and from the dog longitudinal smooth muscle were used as phosphodiesterase preparations. Each preparation had low and high Km values, indicating the existence of at least two kinds of phosphodiesterase. Papaverine and Aspaminol (1, 1-diphenyl-3-piperidinobutanol hydrochloride), hydralazine, caffeine Na benzoate and aminophylline were used as test drugs. Aspaminol had little inhibitory effect on phosphodiesterase. Ki value of papaverine almost equalled the concentration (M) which was necessary to produce 50% relaxation. Relaxation of the guinea pig taenia by papaverine was preceded by an increase of intracellular cyclic AMP. Therefore, the action of papaverine is likely to be mediated by an increase in cyclic AMP, which is caused by inhibition of the phosphodiesterase-catalyzed breakdown of cyclic AMP. There was little correlation between relaxing activities of the drugs used and their antiphosphodiesterase activities. Relaxation of the smooth muscle induced by the smooth muscle relaxants excepting papaverine is not due to inhibition of phosphodiesterase.
    Download PDF (257K)
  • Suehiro NAKANISHI, Eiko SHIOHARA, Miyoko TSUKADA, Go KINOSHITA
    1975 Volume 25 Issue 1 Pages 71-73
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Download PDF (133K)
  • Tadashi FUJITA, Masahide YASUDA
    1975 Volume 25 Issue 1 Pages 73-76
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Download PDF (176K)
  • Kuk Hyun SHIN, Hideo NAKAGAWA, Susumu TSURUFUJI
    1975 Volume 25 Issue 1 Pages 76-79
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Download PDF (191K)
  • Motoo OKA, Takeshi KASHIMOTO, Futoshi IZUMI
    1975 Volume 25 Issue 1 Pages 79-81
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Download PDF (130K)
  • Keisuke TAKEDA, Hiroshi SAKURAI, Shoichi IMAI
    1975 Volume 25 Issue 1 Pages 82-84
    Published: 1975
    Released on J-STAGE: December 19, 2006
    JOURNAL FREE ACCESS
    Download PDF (122K)
feedback
Top