The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
21 巻, 5 号
選択された号の論文の17件中1~17を表示しています
  • M.A. MATIN, P.P. KAR
    1971 年 21 巻 5 号 p. 563-567
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    Eserine and mipafox have often been used as anticholinesterases to allow measurement of spontaneous release of acetylcholine from the ileum (1-4). Mipafox was chosen because of its apparent inability to release acetylcholine from smooth muscle (5). It has also been reported that values for acetylcholine release in the presence of mipafox (1) were much lower than those obtained by other workers using eserine (2, 3). It, therefore, follows that the choice of a particular anticholinesterase may influence the release of acetylcholine from smooth muscle. In order to experimentally test this possibility, we examined the effect of four cholinesterase inhibitors—eserine, prostigmine, phosphamidon and mipafox, on the spontaneous release of acetylcholine from isolated guineapig ileum.
    PAM (2-pyridyl-aldoxime methiodide) reactivates the phosphorylated (inhibited) cholinesterase (6, 7); At certain concentrations, it induces the release of acetylcholine while at others, it inhibits the acetylcholine release from rat phrenic nerve diaphragm preparation (8). The effect of PAM on the release of acetylcholine from smooth muscle has so far not been studied. The effect of PAM, if any, on the acetylcholine output from isolated guineapig ileum, in the presence of anticholinesterases, has also been examined in the present study.
  • Takeo ASAKAWA, Hiroshi YOSHIDA
    1971 年 21 巻 5 号 p. 569-583
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    A wide variety of hormones, such as epinephrine, glucagon and ACTH, increase the intracellular concentration of cyclic AMP in several tissues and cyclic AMP induces similar effects to those of many hormones (1, 2). Thus it has been proposed that cyclic AMP mediates the responses of these hormones. Increased concentrations of cyclic AMP in tissues are caused by enhanced adenyl cyclase activity or suppressed phosphodiesterase activity. The activities of these enzymes are known to be higher in the brain than in other tissues (3, 4). Cyclic AMP was previously reported by Siggins, Hoffer and Bloom (5) to interfere with neuronal activity in the cerebellum of rats. It is conceivable that cyclic AMP may play a role in regulating the activities of the cells of central nervous system as an intracellular mediator of responses to transmitters and hormone-like compounds. In support of this Kakiuchi and Rall (6) reported that on incubation of slices of rabbit cerebral cortex with histamine a large amount of cyclic AMP accumulated in the slices. Recently similar results were reported by other investigators (7-9).
    Kwiatkowski (10) first found histamine in various areas of the central nervous system and subsequently his findings have mostly been confirmed (11-15). However, little is known about the function of histamine in the central nervous system.
    Prostaglandins have been found to be present in the brain, as in other tissues, of several species (16-24) and these compounds are widely distributed throughout all regions of the brain (24). Horton (25) observed that intraventricular administration of PGE, to cats caused sedation and stupor. Spontaneous movement of the cat decreased and the cat lost interest in its surroundings. In adipose tissue and toad bladder, prostaglandin E was reported to inhibit the responses to lipolytic hormones and vasopressin, and this inhibition was attributed to inhibition of the activation of adenyl cyclase by these hormones (26-31). It is also possible that prostaglandin E may be involved in regulation of the intracellular concentration of cyclic AMP in the central nervous system.
    These observations suggest that cyclic AMP, histamine and prostaglandin E are all involved in control of the function of the central nervous system. Accordingly we investigated the responses of the central nervous system to these compounds quantitatively. The possible roles of these compounds in regulating the function of the central nervous system are discussed on the basis of the results.
  • Hidenori OHASHI
    1971 年 21 巻 5 号 p. 585-596
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    A fairly large number of papers dealing with the excitatory junction potential evoked by cholinergic nerve stimulation are now available (1-5). However, information about transmission from cholinergic nerves to smooth muscle cells is much less than about transmission from adrenergic nerves. This seems to be because there is no suitable preparation like the hypogastric nerve-vas deferens of the guinea-pig. Most smooth muscle cells previously used have both excitatory and inhibitory innervation and the excitatory response evoked by transmural stimulation may be modified by the inhibitory one.
    The aim of the present work is to investigate transmission from cholinergic nerves to smooth muscle cells using isolated strips of smooth muscle from the longitudinal layer of the upper oesophagus as far as the crop of the chicken. It has been reported that this part of the oesophagus of the chicken receives only cholinergic excitatory innervation (6, 7). As a first step toward studying the transmission, observations were made on the membrane activity of the muscle and these also are presented in this paper.
    The results show that the cholinergic nerve-smooth muscle junction operates by the substantially same manner as that for the sympathetic nerve-smooth muscle junction of the guinea-pig vas deferens or other neuro-effector junctions.
    Preliminary accounts of some of the results have already been published (8).
  • Tetsuyuki NASU, Hideaki KARAKI, Miyoshi IKEDA, Norimoto URAKAWA
    1971 年 21 巻 5 号 p. 597-603
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    Calcium ions are known to play an important role in a contraction of smooth muscle. However, as reviewed by Lüllmann (1), no correlation has been found between tissue Ca content or Ca fluxes and the contractile response of the smooth muscle to various stimulants.
    In guinea pig taenia coli, it was shown that cellular Ca fraction of relatively tightly bound form increase during contraction induced by barium or high concentration of potassium and decreased during the abolition of tension development by various inhibiting factors, and suggested that the shift of Ca into the relatively tightly bound fraction within the cell might have a concern with the tension development (2-5).
    In this paper, it was attempted to make clear an effect of histamine on Ca exchange of smooth muscle in absence or presence of antihistamine, and the above suggestion based on the nonspecific smooth muscle stimulants was confirmed in the experiments using the specific smooth muscle stimulant.
    Some of this work has already been briefly reported (6).
  • Yukio SAITO, Yutaka SAKAI, Miyoshi IKEDA, Norimoto URAKAWA
    1971 年 21 巻 5 号 p. 605-611
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    In 1953, Bülbring noted that the smooth muscle of teania coli from guinea pig showed an increase in oxygen consumption associated with tension development when stimulated by a drug such as acetylcholine, histamine or eserine (1). Recently Urakawa and his coworkers found that high concentration of potassium in Tyrode solution induced an increase in oxygen consumption accompanied by a rise of muscle tension (2), and they considered that Ca ions which entered the muscle cells through the membrane depolarized by high K might play an essential role in increasing oxygen consumption independently of an increase in muscle tension (3).
    The present experiments were undertaken to investigate effects of histamine and its antagonist on oxygen consumption, muscle tension and electrical activity in taenia coli, and the relationship between the resulting increase in oxygen consumption and Ca movement was discussed.
  • Shoichi IIDA, Yoh HISADA
    1971 年 21 巻 5 号 p. 613-619
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    In recent years, some clinical observations and experimental studies with human subjects as well as animals have showed that a bacterial protease preparation “TSP”, which is elaborated by a strain of Serratia, has anti-inflammatory activity (1).
    In the course of our present work in which combination therapy of antitumor antibiotics and anti-inflammatory drugs were used, we observed that the rat bearing ascites tumor, especially MTK-sarcoma III, was particularly susceptible to intraperitoneal administration of TSP.
    The exact reason for the selective toxicity of TSP for the rat bearing ascites sarcoma remains obscure. However, the results of the present report seem to indicate that the acute toxicity of TSP when administered intraperitoneally may not be the consequence of the formation of toxic metabolites by the interaction between TSP and tumor cells or ascitic fluid in the peritoneal cavity. Conceivably, further studies on this unexpected phenomenon will provide information concerning specific interactions between some protein and the peritoneal membrane and also alterations of the properties of plasma membranes resulting from this malignant tumor.
  • Kiyohisa KAWAI, Seiji KUZUNA, Shigeru MORIMOTO, Harumitsu ISHII, Naohi ...
    1971 年 21 巻 5 号 p. 621-639
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    Since the discovery of adramatically potent antiphlogistic or antirheumatic effect of cortisone, a number of glucocorticoid derivatives were synthesized for pharmacological evaluation and some of them have been introduced to clinical use in rheumatic diseases and other various inflammatory disorders. The large doses or prolonged use of glucocorticoids, however, produced a variety of clinical side effects such as gastro-intestinal lesion and impaired protection against infection mainly due to adaptative adrenal atrophy and immunosuppression. Enthusiastic efforts to dissociate the therapeutic effects from adverse ones in chemical structure of glucocorticoids have all resulted in failure.
    Consequently, chemical and pharmacological investigations to search for new nonsteroidal antiphlogistics different in mode of action from glucocorticoids and less in toxicity have been revived with successful introduction of some agents on the market. They consist of a variety of chemical compounds including weak organic acids such as phenylbutazone, ibufenac, and indomethacin, and moderately strong base such as benzydamine.
    Research largely concentrated upon various weak organic acids effective against inflammatory processes in experimental animals in this laboratory has resulted in presentation of 6-chloro-5-cyclohexylindan-1-carboxylic acid (TAI-284), which has strong antiinflammatory, analgesic, and antipyretic activities. The structure is as follows:
    Since no single assessment can represent the general aspects of the drug and provides a satisfactory evaluation for anti-inflammatory agents in the screening process (1), a variety of phlogistic materials, experimental animals, or sites of inflammation are required. In addition, according to Winter (2) certain less specific means of producing inflammation in the screening methods may give an efficient evaluation of anti-inflammatory agents clinically used.
    Therefore, to assess the anti-inflammatory activities of TAI-284, a variety of substances such as carrageenin, kaolin, acetic acid, croton oil, sodium urate, and Freund's complete adjuvant were used as phlogistic agents, and ultraviolet irradiation and cotton pellets were also applied.
  • Junko MORI, Takeo FUKUDA
    1971 年 21 巻 5 号 p. 641-650
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    It has been known that systemically administered local anesthetic agents such as procaine and lidocaine manifest depressant effects similar to barbiturates on the central nervous system. They abolished the tonic extensor phase of the maximal electroshock seizure in experimental animals (1-4), inhibited the reticular activating system (5), and blocked the amygdaloid (6) as well as hippocampal after-discharges (7).
    On the other hand, some discrepancies were observed between the actions of local anesthetics and of barbiturates in behavioral and electrical manifestations of convulsion. Procaine and lidocaine in larger doses induced clonic convulsions. They did not modify or even enhanced the clonic phase of electrically induced seizure (8), whereas barbiturates could suppress it. Moreover, the local anesthetics tended to enhance the spike and wave complex in EEG elicited by bemegride in rabbits, whereas barbiturates definitely inhibited it (9). These inconsistencies may be due to different mechanisms of depressant actions of local anesthetics and barbiturates on neurons of central nervous system. In fact, Galindo (10, 11 ) showed different patterns of synaptic inhibition by procaine and pentobarbital in cuneate neurons of the oblongate medulla in cats.
    We intend to search the difference in the mechanisms of inhibitory action of lidocaine and pentobarbital on the activities of reticular neurons, since the reticular formation is regarded as a site to play an important role in the manifestation of tonic convulsion (12, 13) and the activities of its neurons are closely related to cortical spikes induced by pentetrazol (14).
    The present study is concerned with the midbrain reticular neurons of which activities are influenced by stimulation of the thalamic reticular nucleus.
  • Masakazu NISHIMURA, Norimoto URAKAWA, Miyoshi IKEDA
    1971 年 21 巻 5 号 p. 651-659
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    It has been reported that mercury was contained in the tissue of, and eggs laid by hens fed experimentaly seed grains treated with methyl mercury dicyandiamide (1, 2). In the field, it has also been pointed out the remarkably high mercury contents in seed-eating birds, such as pheasants, and predatory animals living on such birds, suggesting that it may be explained by the existence of alkyl mercury treated seed grains left in the field at the sowing time (3). In 1967, Teining (4) reviewed the pharmacological effect of methyl mercury dicyandiamide on the fowl Gallus gallus L. Some other investigators also studied the retention and movement of organic mercury compounds and their transfer to eggs in birds (5, 6).
    The autoradiographic technique is one of the most useful methods to examine the body distribution of radioactive substances (7, 8). This technique has been employed actually to study the distribution of several radioactive compounds in the mouse and other small mammals (9-11), but not in any in the fowls.
    The present paper reports a retention and movements of inorganic mercury, in the form of 203Hg-mercuric nitrate, and its transfer to egg in laying quail using a whole-body autoradiographic and radioisotope tracer techniques.
  • Tomio SEGAWA, Toshikazu OKADA, Kayoko KUME
    1971 年 21 巻 5 号 p. 661-669
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
    Large amounts of 5-hydroxytryptamine (5-HT) in the mammalian duodenum are found mainly in the enterochromaffin cells. Baker (1) was the first to demonstrate that in the enterochromaffin cells of the dog's duodenal mucosa, 5-HT was stored in large granules which were sedimented in the gravitational field used for the sedimentation of mitochondria. By further equilibrium centrifugation in a sucrose density gradient the granules were partially purified from mitochondria (2). Prusoff (3) reported that even with a two density gradient centrifugation of the mitochondrial fraction succinic dehydrogenase (SDH) activity was still found in the fraction that was rich in 5-HT. Therefore, in this paper an attempt has been made to separate 5-HT storage granules from SDH. Attention has also been given to minimizing damage to the granules during separation. For this purpose urografin density gradients have been employed.
  • Masamichi SATOH, Hiroshi TAKAGI
    1971 年 21 巻 5 号 p. 671-672
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
  • Shigeru HATAKEYAMA, Tatsuro SHIGEI
    1971 年 21 巻 5 号 p. 673-675
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
  • J.N. SHARMA, G.B. SINGH, B.N DHAWAN
    1971 年 21 巻 5 号 p. 675-677
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
  • Fuminori SAKAI, Hitoshi ENDOU
    1971 年 21 巻 5 号 p. 677-679
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
  • MOTOO OKA, Futoshi IZUMI, Takeshi KASHIMOTO
    1971 年 21 巻 5 号 p. 680-682
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
  • Mieko TOMURA, Tai AKERA
    1971 年 21 巻 5 号 p. 682-685
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
  • Shiro KONISHI, Masanori OTSUKA
    1971 年 21 巻 5 号 p. 685-687
    発行日: 1971年
    公開日: 2007/02/02
    ジャーナル フリー
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