Journal of pharmacobio-dynamics最新文献

Methylprednisolone reduces the nephrotoxicity caused by cisplatin. 甲基强的松龙减少顺铂引起的肾毒性。

Journal of pharmacobio-dynamics Pub Date : 1992-12-01 DOI: 10.1248/bpb1978.15.693

J Uozumi, Y Koikawa, T Ueda

引用次数: 0

A tiaramide derivative, 5-chloro-3-(4-hydroxypiperadinocarbonylmethyl)benzothiazoline-2-one (HPR-611), a potent inhibitor of anaphylactic chemical mediator release--a distinctive feature from disodium cromoglycate. 一种甲酰胺衍生物，5-氯-3-(4-羟基吡啶羰基甲基)苯并噻唑啉-2- 1 (hrp -611)，是一种有效的过敏性化学介质释放抑制剂，是异甘糖酸二钠的一个显著特征。

Journal of pharmacobio-dynamics Pub Date : 1992-12-01 DOI: 10.1248/bpb1978.15.673

T Nabe, H Hashii, S Matsubara, K Yasui, H Yamamura, M Horiba, S Watanabe-Kohno, K Ohata

{"title":"A tiaramide derivative, 5-chloro-3-(4-hydroxypiperadinocarbonylmethyl)benzothiazoline-2-one (HPR-611), a potent inhibitor of anaphylactic chemical mediator release--a distinctive feature from disodium cromoglycate.","authors":"T Nabe, H Hashii, S Matsubara, K Yasui, H Yamamura, M Horiba, S Watanabe-Kohno, K Ohata","doi":"10.1248/bpb1978.15.673","DOIUrl":"https://doi.org/10.1248/bpb1978.15.673","url":null,"abstract":"Effects of a tiaramide derivative, 5-chloro-3-(4-hydroxypiperadinocarbonylmethyl)benzothiazoline++ +-2-one (HPR-611), on anaphylactic chemical mediator release from rat peritoneal exudate cells (RPEC), guinea pig lung fragments (GPLF) and human lung fragments (HLF) were investigated in comparison with those of tiaramide and disodium cromoglycate (DSCG). HPR-611 at 10(-6) - 10(-4) g/ml showed a concentration-dependent inhibition of the histamine release from RPEC regardless of its pretreatment time. Tiaramide also inhibited the release with slightly less potency than HPR-611. The treatment of DSCG 1 min before antigen challenge markedly prevented the release but the inhibitory potency was clearly deteriorated by prolongation of the pretreatment time. Tiaramide tended to influence the anaphylactic release of histamine from GPLF with only 20% inhibition of the release at either 10(-5) or 10(-4) g/ml, whereas HPR-611 at 10(-5) and 10(-4) g/ml significantly suppressed the release in a concentration-dependent fashion. DSCG was not effective on that even at higher concentrations. Anaphylactic release of not only histamine but also immunoreactive leukotriene B4 (i-LTB4) and i-LTC4 from HLF was markedly inhibited by 10(-8) - 10(-4) g/ml of HPR-611. Tiaramide inhibited the release to a somewhat less extent than HPR-611, while nominal or no inhibitions by DSCG were found. From these results, it is clearly apparent that anti-allergic actions of HPR-611 are quite different from those of DSCG.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.673","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12459105","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Effects of nanomolar to submillimolar carteolol on noradrenaline release in the absence and presence of uptake1 and uptake2 blockers in guinea pig pulmonary arteries. 纳摩尔至亚毫摩尔卡替洛尔对豚鼠肺动脉中摄取1和摄取2阻滞剂缺失和存在时去甲肾上腺素释放的影响。

Journal of pharmacobio-dynamics Pub Date : 1992-12-01 DOI: 10.1248/bpb1978.15.687

N Matsushita, M Kuwahara, Y Goshima, Y Misu

{"title":"Effects of nanomolar to submillimolar carteolol on noradrenaline release in the absence and presence of uptake1 and uptake2 blockers in guinea pig pulmonary arteries.","authors":"N Matsushita, M Kuwahara, Y Goshima, Y Misu","doi":"10.1248/bpb1978.15.687","DOIUrl":"https://doi.org/10.1248/bpb1978.15.687","url":null,"abstract":"Effects of nanomolar to submillimolar carteolol, a non-selective beta-antagonist, on the evoked release at 1 Hz and the spontaneous release in the absence and presence of uptake1 and uptake2 blockers were studied in pulmonary arteries, isolated from guinea pigs, and then preloaded with [3H]noradrenaline. dl-Carteolol at 10(-8), 10(-7) and 10(-6) M applied at the increasing concentrations inhibited the evoked [3H]-release in untreated arteries and in desipramine and corticosterone-treated arteries. The spontaneous [3H]-release slightly but significantly increased or tended to increase in untreated arteries. dl-Carteolol at 10(-5) and 10(-4) M clearly and concentration-dependently increased the spontaneous [3H]-release in untreated and cocaine-treated arteries. This increase was markedly inhibited by further pretreatment with normetanephrine. The evoked [3H]-release was not altered by dl-carteolol at 10(-5) M, but increased at 10(-4) M. This increase was not modified by cocaine and by cocaine and normetanephrine. d-Carteolol at 10(-5) and 10(-4) M produced effects similar to those of dl-carteolol. Nanomolar to micromolar dl-carteolol inhibits the evoked [3H]-release, which supports our previous conclusion that this inhibition is due to blockade of tonically functioning presynaptic beta 2-adrenoceptors. Carteolol at the higher concentrations seems to become a substrate for an uptake2 mechanism and to produce an unknown sympathomimetic activity in guinea pig pulmonary arteries.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.687","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471548","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Characteristics of 1,3-bis-(2-ethoxycarbonylchromon-5-yloxy)-2-((S)- lysyloxy)propane dihydrochloride (N-556), a prodrug for the oral delivery of disodium cromoglycate, in absorption and excretion in rats and rabbits. 口服甘糖酸二钠前药1,3-二-(2-乙氧羰基铬-5-氧基)-2-(S)-氧基)丙烷二盐酸盐(N-556)在大鼠和家兔体内的吸收和排泄特性。

Journal of pharmacobio-dynamics Pub Date : 1992-12-01 DOI: 10.1248/bpb1978.15.681

A Yoshimi, H Hashizume, M Kitagawa, K Nishimura, N Kakeya

{"title":"Characteristics of 1,3-bis-(2-ethoxycarbonylchromon-5-yloxy)-2-((S)- lysyloxy)propane dihydrochloride (N-556), a prodrug for the oral delivery of disodium cromoglycate, in absorption and excretion in rats and rabbits.","authors":"A Yoshimi, H Hashizume, M Kitagawa, K Nishimura, N Kakeya","doi":"10.1248/bpb1978.15.681","DOIUrl":"https://doi.org/10.1248/bpb1978.15.681","url":null,"abstract":"The absorption and excretion of 1,3-bis-(2-ethoxycarbonylchromon-5-yloxy)-2- ((S)-lysyloxy)propane dihydrochloride (N-556), which is a prodrug for the oral delivery of disodium cromoglycate (DSCG), were studied in rats and rabbits. In both animal species, the plasma concentration of DSCG after oral administration of N-556 peaked within 1.0 h, and thereafter declined with a half-life of about 1.2 h in rats and rabbits. The area under the plasma DSCG level versus time curve (AUC) increased in proportion to the dose of N-556 in both animals. The bioavailability of N-556 as calculated from AUC was about 6% in rats and 40% in rabbits, whereas that of DSCG was only 0.1% in rats and 2.5% in rabbits. About 2% and 15% of the dose were respectively excreted as DSCG in the urine and bile after the oral administration of N-556 in rats. The ratio of biliary excretion to urinary excretion (B/U) after the oral administration of N-556 was about twice that after the intravenous injection of DSCG. In rabbits, the urinary and biliary excretions of DSCG after oral administration of N-556 were about 25% and 5%, respectively. The B/U ratio after the oral administration of N-556 in rabbits was similar to that after intravenous administration of DSCG. The difference in the systemic bioavailability of N-556 between rats and rabbits thus appears to be due to a first-pass effect, in addition to a difference in the absorption rate.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.681","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471547","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 9

Production of phytochelatins in Polygonum cuspidatum on exposure to copper but not to zinc. 虎杖暴露于铜而非锌环境下植物螯合素的产生。

Journal of pharmacobio-dynamics Pub Date : 1992-12-01 DOI: 10.1248/bpb1978.15.667

H Imahara, T Hatayama, S Kuroda, Y Horie, E Inoue, T Wakatsuki, T Kitamura, S Fujimoto, A Ohara, K Hashimoto

{"title":"Production of phytochelatins in Polygonum cuspidatum on exposure to copper but not to zinc.","authors":"H Imahara, T Hatayama, S Kuroda, Y Horie, E Inoue, T Wakatsuki, T Kitamura, S Fujimoto, A Ohara, K Hashimoto","doi":"10.1248/bpb1978.15.667","DOIUrl":"https://doi.org/10.1248/bpb1978.15.667","url":null,"abstract":"We studied cellular resistance to copper of plant cells Polygonum cuspidatum. When callus of P. cuspidatum was incubated on medium containing 100 microM cupric sulfate, the callus grew as well as the control callus did. The copper content of the callus, however, was elevated to a similar level of the medium. When cell extracts of callus exposed to 100 microM cupric sulfate were fractionated by gel filtration chromatography, a specific copper peak was eluted at the region of molecular weights between 4000 and 1000. Since an appearance of the copper-containing materials was inhibited by buthionine sulfoximine and the partially purified copper-containing materials contained only three amino acids: glutamic acid, glycine and cystine, the materials were supposed to be gamma-glutamyl peptides phytochelatins. Callus of P. cuspidatum synthesized phytochelatins from 50 microM cupric sulfate and maximally at 100-150 microM cupric sulfate. When induction of phytochelatins by another heavy metal, zinc, was analyzed, the callus, however, did not synthesize phytochelatins on exposure to zinc sulfate up to 1 mM. These findings suggested that phytochelatins were required for resistance to copper but probably not to zinc in the plant cells.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.667","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12536064","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Effects of long-term administration of (4S)-1-methyl-3-[(2S)-2-[N-((1S)-1-ethoxycarbonyl-3- phenylpropyl)amino]propionyl]-2-oxoimidazolidine-4-carboxylic acid hydrochloride (TA-6366), a new angiotensin I converting enzyme (ACE) inhibitor, from the pre-hypertensive stage on morphological change and mechanical property related to sodium ion permeability in aorta of spontaneously hypertensive rats (SHRs). 新型血管紧张素I转换酶(ACE)抑制剂(4S)-1-甲基-3-[(2S)-2-[N-(1S)-1-乙氧基羰基-3-苯丙基)氨基]丙酰]-2-氧咪唑烷-4-羧酸盐酸盐(TA-6366)对自发性高血压大鼠主动脉钠离子通透性相关形态学变化和力学性能的影响

Journal of pharmacobio-dynamics Pub Date : 1992-11-01 DOI: 10.1248/bpb1978.15.657

M Kubo, K Kobayashi, R Ishida

{"title":"Effects of long-term administration of (4S)-1-methyl-3-[(2S)-2-[N-((1S)-1-ethoxycarbonyl-3- phenylpropyl)amino]propionyl]-2-oxoimidazolidine-4-carboxylic acid hydrochloride (TA-6366), a new angiotensin I converting enzyme (ACE) inhibitor, from the pre-hypertensive stage on morphological change and mechanical property related to sodium ion permeability in aorta of spontaneously hypertensive rats (SHRs).","authors":"M Kubo, K Kobayashi, R Ishida","doi":"10.1248/bpb1978.15.657","DOIUrl":"https://doi.org/10.1248/bpb1978.15.657","url":null,"abstract":"Effects of (4S)-1-methyl-3-[(2S)-2-[N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)amino]- propionyl]-2-oxoimidazolidine-4-carboxylic acid hydrochloride (TA-6366) on morphological change and mechanical property related to sodium ion permeability in the aorta of spontaneously hypertensive rats (SHRs) were examined, as compared with those of enalapril and captopril. Ten-week oral administration of TA-6366 (1 and 5 mg/kg/d) from 4 weeks of age impeded aortic media-thickening together with a rise in blood pressure in SHRs. Concomitantly, aorta weights in both groups were markedly decreased. The higher dose of TA-6366 almost fully suppressed the accelerated tension development induced by K(+)-free medium and decreased total sodium ion content in the aorta. These vascular effects of TA-6366 was more prominent than those of enalapril and captopril at 5 mg/kg/d. The difference in potencies on the above vascular parameters between TA-6366 and these drugs seemed to be mainly related to the difference in their antihypertensive activities. These results suggest that TA-6366 has preventive effects against progression of vascular diseases, particularly atherosclerosis, accompanied with hypertension.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.657","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12464663","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Comparison of the effects of halothane and propranolol on the effective refractory period and the ventricular activation in a canine myocardial infarction model. 氟烷与心得安对犬心肌梗死模型有效不应期及心室活动影响的比较。

Journal of pharmacobio-dynamics Pub Date : 1992-11-01 DOI: 10.1248/bpb1978.15.623

H Hashimoto, S Imamura, K Ikeda, M Nakashima

{"title":"Comparison of the effects of halothane and propranolol on the effective refractory period and the ventricular activation in a canine myocardial infarction model.","authors":"H Hashimoto, S Imamura, K Ikeda, M Nakashima","doi":"10.1248/bpb1978.15.623","DOIUrl":"https://doi.org/10.1248/bpb1978.15.623","url":null,"abstract":"The effects of halothane on the effective refractory period (ERP) and the ventricular activation were examined in a canine myocardial infarction model, and compared with those of propranolol. Halothane reduced the heart rate and prolonged the ERP in both normal and infarcted zones. A prolongation of ERP with halothane was also observed during atrial pacing at the same rate as in control, but the effect was less than during sinus rhythm. Halothane (1 MAC) further delayed or blocked the delayed activation in the infarcted zones with only slight effects on the activation of the normal zones. Propranolol (0.2 mg/kg) prolonged ERP during sinus rhythm, but it did not affect either the ERP or ventricular activation during atrial pacing. In conclusion, halothane produced a selective depression of the delayed activation and the prolongation of ERP, which may be caused by both direct effects on the myocardium and secondary effects such as a reduction of the heart rate. These effects of halothane may contribute to its antiarrhythmic effects in the myocardial infarction model which have been previously reported.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.623","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12464079","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Journal of pharmacobio-dynamics Pub Date : 1992-11-01 DOI: 10.1248/bpb1978.15.617

Y Kondo, A Kato, H Hojo, S Nozoe, M Takeuchi, K Ochi

引用次数: 61

Pharmacological studies on 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one (T-614), a novel antiinflammatory agent. 3rd communication: the involvement of bradykinin in its analgesic actions. 新型抗炎药3-甲酰基氨基-7-甲基磺酰基氨基-6-苯氧基- 4h -1-苯并吡喃-4-酮(T-614)的药理研究。第三通讯:缓激肽参与其镇痛作用。

Journal of pharmacobio-dynamics Pub Date : 1992-11-01 DOI: 10.1248/bpb1978.15.641

K Tanaka, T Shimotori, S Makino, M Eguchi, K Asaoka, R Kitamura, C Yoshida

{"title":"Pharmacological studies on 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one (T-614), a novel antiinflammatory agent. 3rd communication: the involvement of bradykinin in its analgesic actions.","authors":"K Tanaka, T Shimotori, S Makino, M Eguchi, K Asaoka, R Kitamura, C Yoshida","doi":"10.1248/bpb1978.15.641","DOIUrl":"https://doi.org/10.1248/bpb1978.15.641","url":null,"abstract":"In order to elucidate the analgesic mechanism of 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-on e (T-614), its effects on the kinin-forming system were examined both in vivo and in vitro. T-614, at doses more than 10 mg/kg p.o., exhibited a significant inhibitory effect on the increased levels of bradykinin released into the pouch fluid of kaolin-induced inflammation in rats. In the kaolin-induced writhing response in mice, which is shown to be mainly dependent on the action of bradykinin, T-614 reduced not only the writhing frequency but also the peritoneal levels of bradykinin in a dose-dependent manner. Whereas, in the zymosan-induced writhing response in which prostaglandin I2 (PGI2) is shown to be an important mediator, it did not exert an obvious inhibition on either writhing responses or peritoneal PGI2 levels at a highest dose of 100 mg/kg. T-614 did not inhibit the activities of serine proteases, such as trypsin, thrombin, kallikrein and plasmin. Furthermore, it did not affect the kinin-forming enzymes of rat plasma in vitro. The above results suggest that the analgesic effects of T-614 may be partly mediated by the inhibition of bradykinin release in the local inflamed tissue.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.641","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12464661","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 19

The effects of adenine and dimethyl sulfoxide on the mouse pancreas. 腺嘌呤和二甲亚砜对小鼠胰腺的影响。

Journal of pharmacobio-dynamics Pub Date : 1992-11-01 DOI: 10.1248/bpb1978.15.605

Y Okazaki, T Minami, K Natsui

{"title":"The effects of adenine and dimethyl sulfoxide on the mouse pancreas.","authors":"Y Okazaki, T Minami, K Natsui","doi":"10.1248/bpb1978.15.605","DOIUrl":"https://doi.org/10.1248/bpb1978.15.605","url":null,"abstract":"The authors have studied the effects of dimethyl sulfoxide (DMSO) on the plasma alpha-amylase activity in mice that sustained a pancreatic injury induced by an oral administration of adenine. In mice given a 5% solution of DMSO as drinking water for 3 d prior to the administration of adenine (175 mg/kg), and also drank this DMSO solution until the end of the experiment, hyperemia of the pancreas was observed and the level of plasma alpha-amylase activity became significantly higher than the level seen in the control mice. A pathological examination also revealed vacuolation and zymogenic degranulation. Further, the plasma alpha-amylase activity level increased only in mice given this 5% DMSO solution, and no increase was noted in mice given a 3% or a 1% DMSO solution for drinking water. Further, the pancreatic lipid peroxide level of mice given this 5% DMSO solution was significantly higher than the level seen in the control group. Based on the above results and associated data, it is thought that an oral administration of adenine can induce a pancreatic injury in the mouse, and that this injury is sustained with the assistance of DMSO.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.605","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12458839","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3