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Volume 41 (1986)
- Issue 4 Pages 431-
- Issue 3 Pages 267-
- Issue 2 Pages 139-
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Volume 41, Issue 3
Displaying 1-21 of 21 articles from this issue
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S.N. DUBE, A.K. GHOSH, K. JEEVARATHINAM, D. KUMAR, S. DAS GUPTA, B.P. ...1986 Volume 41 Issue 3 Pages 267-271
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSDiethyxime, a non-quaternary cholinesterase reactivator was evaluated for its antidotal efficacy against organophosphorus intoxication in rats using the protection index, cholinesterase reactivation and neuromuscular function as the experimental protocol. Diethyxime along with atropine produced a marked anti-dotal effect against dimethyl dichlorovinyl phosphate (DDVP) poisoning on all the parameters studied. The action of diethyxime was mainly peripheral. The protective efficacy against diisopropyl fluorophosphate (DFP) poisoning was not observed with this reactivator.View full abstractDownload PDF (331K) -
Yoshiki KUNO, Kazuko AOKI, Midori KAJIWARA, Kaori ISHII, Tetsuo OKA1986 Volume 41 Issue 3 Pages 273-281
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSPrevious studies have shown that three distinct enzymes, amastatin-sensitive aminopeptidase, captopril-sensitive peptidyl dipeptidase A, and phosphoramidon-sensitive endopeptidase-24.11, played a critical role in the inactivation of enkephalins in isolated preparations. In the present study, therefore, the rank order of the potency of three endogenous opioid peptides, [Met5]-enkephalin, [Leu5]-enkephalin, and β-endorphin, in three isolated preparations, guinea-pig ileum, mouse vas deferens, and rat vas deferens, was estimated in the presence of the mixture of three peptidase inhibitors, amastatin, captopril, and phosphoramidon. [Met5]-Enkephalin was approximately three-fold more potent than [Leu5]-enkephalin and four-fold more potent than β-endorphin in guinea-pig ileum in which three opioid peptides were indicated to act on mu-receptors. Additionally, [Met5]-enkephalin was slightly but significantly more potent than [Leu5]-enkephalin and approximately twenty-fold more potent than β-endorphin at delta-receptor sites in mouse vas deferens. Moreover, [Met5]-enkephalin was approximately three-fold more potent than [Leu5]-enkephalin, but sixty-fold less potent than β-endorphin in rat vas deferens in which the opioid-receptor type interacting with enkephalins could not be determined. In conclusion, the well-known rank order of the potency of three endogenous opioid peptides was shown to be altered in both guinea-pig ileum and mouse vas deferens but not in rat vas deferens by the pretreatment of the preparations with the mixture of three peptidase inhibitors.View full abstractDownload PDF (709K) -
Hajimu YAMAMOTO, Yoshiki NAKAMURA, Yasuo KUNOH, Kenji ICHIHARA, Mitsua ...1986 Volume 41 Issue 3 Pages 283-292
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSEffects of (-)cis-2, 3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1, 5-benzothiazepin-4-(5H)-one hydrochloride (BTM-1086) on various experimental gastric and duodenal ulcers were studied in rats. In the pylorus-ligated ulcer, restraint and water immersion stress ulcer, and drug-induced ulcer (indomethacin, aspirin, reserpine, serotonin, cysteamine), BTM-1086 prevented the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibited the histamine-induced gastric ulcer. The inhibitory activities of BTM-1086 were significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day, p.o., ×14) showed a significant healing effect, which was higher than that of propantheline bromide. BTM-1086 at a dose of 0.2 mg/kg, i.d., remarkably inhibited the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K+ as well as the increments of the volume and Na+ in the gastric secretion were prevented dose-dependently by pretreatment with BTM-1086.View full abstractDownload PDF (770K) -
Heitaroh IWATA, Akira OHTA, Akemichi BABA1986 Volume 41 Issue 3 Pages 293-297
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESS[3H]-Arachidonic acid incorporation into phospholipids of synaptosomal lysates prepared from veratridine-treated synaptosomes was examined. Synaptosomal lysates were shown to acylate exogenously added lysophosphatidylcholine, lysophosphatidylinositol, and lysophosphatidylethanolamine, when incubated with [3H]-arachidonic acid, ATP, CoA and MgCl2, yielding the respective phospholipids. Preincubation of synaptosomes with veratridine for 30 sec gave rise to an increase in [3H]-arachidonic acid incorporation into phosphatidylethanolamine, but not phosphatidylcholine nor phosphatidylinositol, indicating that lysophosphatidylethanolamine might be produced by veratridine. This increase of radioactivity in phosphatidylethanolamine caused by veratridine was completely inhibited by 1 μM tetrodotoxin or in calcium-free condition. These observations show that lysophosphatidylethanolamine was formed in a calcium-dependent manner and accumulated in synaptosomes treated with veratridine, which may relate to its action on the sodium channel and enhanced calcium influx.View full abstractDownload PDF (391K) -
Different Effects of Various Vasodilators on Autoregulation of Renal Blood Flow in Anesthetized DogsNobuyuki OGAWA, Hiroshi ONO1986 Volume 41 Issue 3 Pages 299-306
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSIn order to examine whether the autoregulation of renal blood flow is equally influenced by all kinds of vasodilators, kidney perfusion experiments were performed in anesthetized dogs. The perfused kidney usually showed excellent autoregulation of blood flow over the perfusion pressure between 120 and 200 mmHg. Renal blood flow was increased by the renal arterial infusion of diltiazem (100 μg/min), papaverine (10 mg/min) or nicorandil (300 μg/min) (at the basal perfusion pressure of 100 mmHg) and was maintained at an increased level while the infusion was continued. On the other hand, renal blood flow was increased only transiently by the infusion of nitroglycerin (50 μg/min), and the blood flow gradually decreased to the basal level in spite of the continuous infusion. Infusions of diltiazem and papaverine abolished the autoregulation of renal blood flow besides the vasodilator effect, but infusions of nitroglycerin and nicorandil have no effect on the autoregulation. Furthermore, sodium nitroprusside (30 μg/min) and sodium nitrite (5 mg/min), which are assumed to produce vasodilation through cyclic GMP, also have no effect on the autoregulation of renal blood flow. In conclusion, all the vasodilators do not influence the renal blood flow autoregulation, and vasodilation caused by cyclic GMP is unconnected with the myogenic mechanism regulating the renal blood flow.View full abstractDownload PDF (578K) -
Hitoshi ITO, Keishiro SHIMURA1986 Volume 41 Issue 3 Pages 307-314
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe antitumor effects of Xiao-Chai-Hu-Tang (Shosaiko-To: SHX) with or without 5-fluorouracil (5-FU) or cyclophosphamide (CY) were examined in an experimental system of lung metastasis induced by Lewis lung carcinoma in C57BL/6crSlc mice. Lewis lung carcinoma cells were implanted into the footpads of the mice. Ten days later, the implanted tumors were surgically removed. The effects of SHX were evaluated by the number of lung surface nodules present 14 days after removal of the implanted tumor. The administration of SHX, p.o. (300 mg/kg×2/day ×10) caused the antimetastatic effect. Therapy with SHX plus 5-FU or CY significantly inhibited the development of lung metastases. The number of peritoneal macrophages and the degree of the binding of C3 cleavage products (C3b) to macrophages were enhanced in the mice treated with SHX. Lung metastases were inhibited by the i.v. administration of peritoneal macrophages activated with SHX, p.o. These findings raise the possibility that SHX may have clinical value in the prevention of cancer metastasis.View full abstractDownload PDF (574K) -
Soichi YOSHIDA, Tetsuro KUGA1986 Volume 41 Issue 3 Pages 315-323
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSTwo kinds of electrical stimulation, low frequency stimulation (5 Hz, 1 msec, 5 pulses, every 20 sec) and high frequency stimulation (30 Hz, 0.05-0.1 msec, 10 pulses, every 20 sec), produced contractions in the isolated guinea-pig vas deferens. These responses were blocked by tetrodotoxin but not hexamethonium. Phentolamine potentiated the contractions produced by low frequency stimulation, while it reduced the contractions produced by high frequency stimulation. Diametrically, 5-hydroxytryptamine reduced the contractions produced by low frequency stimulation, while it potentiated the contractions produced by high frequency stimulation. These inhibitory and potentiating actions of 5-hydroxytryptamine were reversed by cyproheptadine and 2-bromolysergic acid diethylamide. Moreover, that 5-hydroxytryptamine produced a depolarization of the smooth muscle membrane was shown by the sucrose gap technique. The results suggest that a 5-hydroxytryptamine receptor exists pre and postsynaptically in the neuro-effector transmission of the guinea-pig vas deferens, that the stimulation of the presynaptic receptor by 5-hydroxytryptamine inhibits the release of a transmitter from noradrenergic nerves, and that the stimulation of the postsynaptic receptor by a high concentration of 5-hydroxytryptamine produces a depolarization of the smooth muscle membrane, and this relates to the potentiation of contractile responses.View full abstractDownload PDF (726K) -
Kouichi TAKEUCHI, Katsutoshi GOTO, Yutaka KASUYA1986 Volume 41 Issue 3 Pages 325-333
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe effects of newly synthesized 5-imidazoline derivatives on the dose-response relationship to norepinephrine were investigated in the normal and denervated vasa deferentia of the rat. Three derivatives (K-3827, K-4011 and K-4300) exerted α-antagonistic action, the potency of which was similar to that of tolazoline. The pA2 values of these derivatives and currently known α-antagonists (tolazoline, phentolamine and prazosin, but not yohimbine) in the denervated tissue were slightly but significantly larger than those in the normal tissue. All imidazoline derivatives and α-antagonists produced an increase in the maximum response to norepinephrine in the normal vas deferens. In the denervated tissue, however, K-3827, K-4011 and α-antagonists caused only a rightward shift of the dose-response curve to norepinephrine, but not an increase in the maximum response, i.e., relatively pure α-antagonism. In contrast, the other 3 imidazoline derivatives, K-4299 and K-6342 which exhibited neither α-agonistic nor antagonistic action and K-4300, increased the maximum response to norepinephrine even after denervation. Their effects were nonspecific in that they also potentiated acetylcholine-induced contractions in both normal and denervated tissues. These 3 imidazoline derivatives antagonized the action of diltiazem. The effects of imidazoline derivatives and α-antagonists were discussed in relation to those of denervation, and the drug enhancement by 3 imidazoline derivatives was analyzed from the viewpoint of calcium movement.View full abstractDownload PDF (604K) -
Hiroshi NARITA, Hideo YABANA, Kohei KIKKAWA, Kiyoshi MIYAZAKI, Tomihir ...1986 Volume 41 Issue 3 Pages 335-344
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSWe studied the arrhythmogenic activity of denopamine, in relation to its positive inotropic action, in dogs and compared it with those of catecholamines. The positive inotropic activities of the compounds as expressed in terms of the ED100 (μg/kg, i.v.), that increased LV dp/dt max of anesthetized dogs by 100% of the control were 8.0 for denopamine, 0.27 for norepinephrine, 0.03 for isoproterenol, 3.8 for dobutamine and 16 for dopamine. On the other hand, the doses of these drugs at which the "non-sinus/total rate" increased significantly (about 30% of total beats, μg/kg, i.v.) were more than 1000 for denopamine, 1.0 for norepinephrine and isoproterenol, and 300 for dobutamine and dopamine in coronary ligated dogs. The ratios of these doses to the ED100 are more than 126 for denopamine, 80 for dobutamine, 33 for isoproterenol, 19 for dopamine and 3.8 for norepinephrine. Arrhythmogenic activity of denopamine was also weaker than those of dobutamine and dopamine in halothane anesthetized dogs. The arrhythmogenic activity of dobutamine was weak as reported, but that of denopamine was the weakest among the drugs tested.View full abstractDownload PDF (723K) -
Yoshihisa KUDO, Kazuho OZAKI, Atsuo MIYAKAWA, Takehiko AMANO, Akihiko ...1986 Volume 41 Issue 3 Pages 345-351
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSFor monitoring the changes in intracellular free Ca2+ concentration ([Ca2+]i), we developed a simple system combining a fluorescence microscope, an image intensifier, a video-camera, a cathode ray tube display and a photodiode, employing quin2 as a Ca2+ indicator. We recorded increases of the fluorescence intensity due to [Ca2+]i rises, when high K+ medium, neurotransmitter and Ca2+ ionophore were applied to the single cells of nervous system origin in culture. The present system is capable of simultaneous detection of the [Ca2+]i changes from multiple separate cells.View full abstractDownload PDF (594K) -
Katsuharu TSUCHIDA, Hironaka AIHARA1986 Volume 41 Issue 3 Pages 353-361
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSEffects of a K ionophore, lonomycin A (K+:Na+=6:1), on the action potential and contractile force in canine cardiac Purkinje fibers were examined. Lonomycin A increased the developed and resting tensions. The agent shortened the action potential, decreased the plateau height and suppressed the automaticity. In addition, lonomycin A also shortened the duration of the slow action potential response, and it shortened the action potential duration to about the same extent in the presence and absence of tetrodotoxin. In quiescent Purkinje fibers, lonomycin A decreased K content in both 1.8 mM Ca Tyrode's solution (contracture observed) and 0.18 mM Ca Tyrode's solution (contracture not observed). These results suggest that lonomycin A-induced changes in the action potential configuration of Purkinje fibers is mainly due to the increase in K conductance, and the increase is induced irrespective of the degree of the increased [Ca2+]i.View full abstractDownload PDF (639K) -
Hiroyasu OKUNO, Hiroshi HAZAMA, Toshihiko MURASE, Yasuko SHIOZAKI, Yos ...1986 Volume 41 Issue 3 Pages 363-371
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe drug metabolizing activity of rat liver during long-term administration of carbon tetrachloride (CCl4), and its relationship with the content of hydroxyproline (Hyp) in the liver were examined. The contents of cytochrome P-450 (P-450) and cytochrome b5 (b5) and the metabolization of aniline, aminopyrine, 7-ethoxycoumarin (7-EC) and benzo(a)pyrene (B(a)P) in the microsomal fraction were examined five days after the final administration of CCl4. The contents of P-450 and b5 and the activity to metabolize the four substrates were gradually reduced as the Hyp content in the liver increased. However, aminopyrine N-demethylation and B(a)P hydroxylation, particularly the latter, was more reduced than aniline hydroxylation and 7-EC O-deethylation in the early stage of hepatic fibrosis. Such differences may be due mainly to the different P-450 subtypes affected by CCl4.View full abstractDownload PDF (694K) -
Yasunobu OKUMA, Yoshitsugu OSUMI1986 Volume 41 Issue 3 Pages 373-379
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSA possible role of the cholinergic mechanism within the dorsal motor nucleus of the vagus (NDV) in the regulation of gastric functions was examined in urethane anesthetized rats. Pretreatment with atropine (1-5 nmole), intracerebroventricularly inhibited the increase in both gastric acid output and mucosal blood flow (MBF), as induced by electrical stimulation of the lateral hypothalamic area (LHA). Bethanechol, microinjected into the dorsal vagal complex (the NDV, the nucleus tractus solitarius and area postrema) induced dose-dependent (5-30 nmole) increases in gastric acid output and MBF, while nicotine was without effect. Pretreatment with atropine 3 nmole microinjected into the dorsal vagal complex completely blocked the increases induced by electrical stimulation of the LHA. Furthermore, the increases in these gastric parameters induced by the administration of 2-deoxy-D-glucose (2-DG) were also significantly inhibited by atropine microinjected into the dorsal vagal complex. These results suggest that neurotransmission of the central descending pathway to the NDV in excitatory regulation of gastric functions is probably mediated through cholinergic muscarinic receptors.View full abstractDownload PDF (627K) -
Hidetada KOMATSU, Yasuo TAKEHANA, Shuichiro HAMANO, Arao UJIIE, Seiji ...1986 Volume 41 Issue 3 Pages 381-391
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSEffects of OKY-046, a selective inhibitor of thromboxane (TX)A2 synthetase and a platelet aggregation inhibitor, on in vitro and in vivo models of cerebral vasospasm were studied. The contraction of the isolated rabbit basilar artery by an exposure to 1.0 ml of whole rabbit blood plus 0.05 or 0.1 units/ml of thrombin was diminished by the treatment with 10-4 M of OKY-046 and/or 10-6 M of cinanserin. When the whole blood of rabbits treated intravenously with 1 mg/kg/min of OKY-046 was used, the contraction of the basilar artery was decreased to about half of the control contraction. Angiographically recognized cerebral vasospasm in vivo, by a transorbital injection of 5.0 to 7.0 ml of autologous arterial blood into the cisterna magna of dogs, was suppressed by 0.05 and 0.5 μg of OKY-046. Moreover, the decrease in the regional cerebral blood flow in autologous blood infused-dogs was inhibited by 0.5 μg of OKY-046. The increase in TXB2 in the cerebrospinal fluid of dogs was significantly inhibited, and the level of 6-keto-PGF1α was slightly increased by the treatment of OKY-046. The ratio of 6-keto-PGF1α/TXB2 was increased from 1.5 to 5.2 in OKY-046-treated dogs. No effect on the basal tone and response to vasoactive agonists such as norepinephrine, KCl and PGE1 was observed in the isolated spiral thoracic aorta of guinea pigs or rabbits. Taken together with our previous findings, we conclude that the inhibition of cerebral vasospasm in the in vitro and in vivo models by the treatment of OKY-046 might be due to an inhibition of platelet aggregation, an inhibition of TXA2 generation and an increase in the ratio of PGI2/TXA2.View full abstractDownload PDF (770K) -
Seiji HIRAKU, Ken TANIGUCHI, Korekiyo WAKITANI, Nagashige OMAWARI, Hei ...1986 Volume 41 Issue 3 Pages 393-401
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe effects of (E)-3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propenoic acid (OKY-046) on thromboxane A2 (TXA2) synthetase in vitro and on experimental animal models of sudden death and cerebral infarction were studied. IC50 values of OKY-046 for the TXA2 synthetase of human, rabbit, dog and guinea pig washed platelets were 0.004, 0.004, 0.26 and 2.4 μM, respectively. OKY-046 at concentrations up to 1 mM, however, did not inhibit prostacyclin (PGI2) synthetase from bovine aorta microsomes or cyclooxygenase and PGE2 isomerase from sheep seminal vesicle microsomes. Similarly, platelet 12-lipoxygenase was not affected by OKY-046. Evidence for a re-direction of arachidonate metabolism from thromboxane synthesis toward PGI2 synthesis was obtained using rat peritoneal cells. Namely, OKY-046 increased PGI2 production accompanied by an inhibition of TXA2 production at a concentration of more than 1 μM. OKY-046 at a dose of 0.1 mg/kg (i.v.) in dogs inhibited the aortic and mesenteric arterial contraction of rabbit induced by the addition of arachidonate to extracorporated blood of the dogs. OKY-046 at a dose of 0.3 mg/kg (i.v.) prevented the arachidonate-induced sudden death and also decreased the incidence of cerebral infarction induced by injection of arachidonate into the internal carotid artery in rabbits. Aspirin also decreased the incidence of cerebral infarction at a dose of 30 mg/kg (i.v.). These results suggest that OKY-046 may be valuable for the treatment of cerebrovascular and cardiovascular diseases associated with vasoconstriction and thrombosis due to TXA2.View full abstractDownload PDF (707K) -
Masahiro NISHIBORI, Ryozo OISHI, Yoshinori ITOH, Kiyomi SAEKI1986 Volume 41 Issue 3 Pages 403-408
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe effect of GABA-mimetics on histaminergic activity in the mouse brain was investigated. Systemic administration of muscimol (2 and 5 mg/kg), THIP (5-15 mg/kg) and aminooxyacetic acid (AOAA) (25 mg/kg) but not baclofen (2.5-15 mg/kg) inhibited the pargyline (65 mg/kg)-induced accumulation of tele-methylhistamine (t-MH). There was no regional difference in the inhibitory effect of muscimol on the t-MH accumulation by pargyline treatment. Muscimol and AOAA also inhibited decrease in the histamine (HA) level induced by α-fluoromethylhistidine (50 mg/kg), a specific inhibitor of histidine decarboxylase. These results suggest that these GABA-mimetics reduce the HA turnover in the mouse brain.View full abstractDownload PDF (391K) -
Hisato KITAGAWA, Toshihiro HAYASHI, Fumiyo TAKEDA, Fumihiko KINEKAWA, ...1986 Volume 41 Issue 3 Pages 409-414
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSThe role of antimuscarinic action in gastric mucosal protection against necrotizing agents and the role of such mucosal protection in antiulcerogenic action were studied in rats with i.v. administered antimuscarinic agents. Pirenzepine, as well as PGE2, prevented the gastric mucosal lesions induced by all necrotizing agents (99.5% ethanol, 0.6 N HCl, 0.15 N NaOH, 0.4 N HCl-50 mM taurocholate), but atropine did not prevent the HCl-induced lesions. Cimetidine inhibited only the ethanol-induced lesions even at the antisecretory dose. Higher doses of pirenzepine (5-fold) and atropine (10-fold) were required to inhibit the gastric secretion in Shay rats than in vagally stimulated rats. There was no difference between the antisecretory doses of cimetidine in Shay rats and vagally stimulated rats. PGE2 (0.03-0.1 mg/kg) did not affect gastric secretion. The protective doses of pirenzepine and atropine against mucosal lesions induced by necrotizing agents were similar to the dose in inhibiting vagally stimulated acid secretion and water-immersion stress-induced lesions. PGE2 (100 μg/kg) did not prevent the water-immersion stress induced gastric lesions. These results suggested that antimuscarinic agents protect the gastric mucosa from necrotizing agents via a blocking action on the activation of the intrinsic cholinergic nerve. However, antiulcerogenic action is more deeply concerned with antisecretory action than cytoprotection.View full abstractDownload PDF (412K) -
Kyozo YAMANAKA, Shigeru KIGOSHI, Ikunobu MURAMATSU1986 Volume 41 Issue 3 Pages 415-418
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSIn microsomes of bovine adrenal medulla, there were two affinity binding sites for carbamylcholine with a high and a low affinity. Copper (1-10 μM) largely enhanced the affinity of carbamylcholine at the low affinity binding site, with a slight increase in the affinity at the high affinity binding site. On the other hand, copper slightly decreased the binding affinity of pirenzepine and atropine. Thus, low concentrations of copper modulate the muscarinic receptors in the adrenal medulla by selectively increasing agonist affinity.View full abstractDownload PDF (278K) -
Takashi ARIMA, Naomi SAMURA, Yasuyuki NOMURA, Tomio SEGAWA1986 Volume 41 Issue 3 Pages 419-423
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSTo determine the affinity of tiapride to D-1, D-2, D-3 and D-4 subtypes of dopamine (DA) receptors, inhibitory effects of tiapride on [3H]-cis-flupenthixol, [3H]spiperone and [3H]N-propylapomorphine binding were examined in the rat striatum and bovine caudate nucleus membranes and compared to those of sulpiride and haloperidol. The IC50 values of tiapride, sulpiride and haloperidol were estimated as follows: 1440, 132 and 0.295 μM for D-1 ; 45.8, 8.8 and 0.004 μM for D-2; greater than 100, greater than 100 and 0.64 μM for D-3; 11.7, 2.88 and 0.0044 μM for D-4, respectively. It is suggested that the affinity of tiapride is high to D-2 and D-4, but is not high to D-1 and D-3. The affinity pattern of tiapride to each DA receptor subtype is similar to but lower than those of sulpiride and haloperidol. In the D-2 receptor assay, the IC50 values of tiapride and sulpiride were 1/22.7 and 1/19.1 of those in the presence of 100 mM NaCl, respectively, suggesting that benzamide drug binds to the D-2 subtype with higher affinity in the presence of Na+ than in the control.View full abstractDownload PDF (375K) -
Koji SAKAMOTO, Mayumi TONOOKA, Koichiro ABE, Kenichi USAMI, Takako KAS ...1986 Volume 41 Issue 3 Pages 424-426
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSWe have investigated the effect of a therapeutic agent for liver disease, Laennec, on the GOT leakage from freshly isolated and primary cultured rat hepatocytes which were treated with CCl4. By treatment with Laennec together with CCl4, the GOT leakage from isolated hepatocytes increased and that from cultured hepatocytes decreased, compared to those incubated only with CCl4. The results suggest that it is better to use primary cultured hepatocytes than to use freshly isolated hepatocytes to evaluate therapeutic agents for liver disease.View full abstractDownload PDF (254K) -
Manabu SHIBATA, Tsuyako OHKUBO, Hiroshi TAKAHASHI, Reizo INOKI1986 Volume 41 Issue 3 Pages 427-429
Published: 1986
Released on J-STAGE: September 15, 2006
JOURNAL FREE ACCESSCombination of bradykinin with substance P exerted synergistic effects on vascular permeability and pain response in mouse paw. Denervation of sciatic nerve reduced significantly bradykinin-induced vascular permeability, suggesting the involvement of sensory nerves. The bradykinin-induced vascular permeability was also reduced by intravenous injection of a substance P-antagonist. The results suggest that neuronal substance P takes part in the action of bradykinin on inflammation and pain sensation.View full abstractDownload PDF (179K)
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