Journal of pharmacobio-dynamics最新文献_第7页

Changes in alpha 2- and beta-adrenoceptors in hepatocytes from rats during treatment with 3'-methyl-4-dimethylaminoazobenzene. 3'-甲基-4-二甲氨基偶氮苯治疗期间大鼠肝细胞α 2和β肾上腺素受体的变化。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.247

F Sanae, K Kohei, M Nomura, K Miyamoto

{"title":"Changes in alpha 2- and beta-adrenoceptors in hepatocytes from rats during treatment with 3'-methyl-4-dimethylaminoazobenzene.","authors":"F Sanae, K Kohei, M Nomura, K Miyamoto","doi":"10.1248/bpb1978.15.247","DOIUrl":"https://doi.org/10.1248/bpb1978.15.247","url":null,"abstract":"A 3'-methyl-4-dimethylaminoazobenzene (3'-MeDAB) containing diet was given to 6 weeks old female Donryu rats, and the number of adrenoceptors and the response of adenylate cyclase in the hepatocytes were measured. The treatment with 3'-MeDAB led to rapid increases in [125I]iodocyanopindolol ([125I]ICYP)- and [3H]clonidine-binding sites to hepatic membranes without significant changes in the Kd values. The number or beta-adrenoceptors defined by [125I]ICYP binding sites was increased with a biphagic mode. The [3H]clonidine binding reached a peak 2 weeks after the start of the carcinogen diet and then began a slow descent. The alpha 2-adrenoceptor was defined by [3H]clonidine binding being selectively inhibited by an alpha 2-antagonist, yohimbine, but not by an alpha 1-antagonist, prazosin, or a beta-antagonist propranolol. Catecholamine responsiveness to adenylate cyclase in hepatocytes also increased during treatment with 3'-MeDAB. However, the efficacy of norepinephrine (NE) in activating cyclase was lower than that of isoproterenol (IPN) during 4 to 8 weeks of the carcinogen diet. The difference between the efficacies of IPN and NE resulted from inhibiting adenylate cyclase through alpha 2-adrenoceptors by NE. Therefore, we noticed that the increasing pattern of the number of beta-adrenoceptors did not always parallel IPN-stimulated adenylate cyclase activity and that the increase in the number of alpha 2-adrenoceptors preceded the difference between the efficacies of IPN and NE in activating adenylate cyclase.(ABSTRACT TRUNCATED AT 250 WORDS)","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 5","pages":"247-54"},"PeriodicalIF":0.0,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.247","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12500578","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

Effects of flecainide on ventricular arrhythmias, abnormal automaticity and activation in a canine model of myocardial infarction. 氟屈奈对犬心肌梗死模型室性心律失常、异常自动性和活化的影响。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.191

H Hashimoto, H Katoh, M Nakashima

{"title":"Effects of flecainide on ventricular arrhythmias, abnormal automaticity and activation in a canine model of myocardial infarction.","authors":"H Hashimoto, H Katoh, M Nakashima","doi":"10.1248/bpb1978.15.191","DOIUrl":"https://doi.org/10.1248/bpb1978.15.191","url":null,"abstract":"Effects of flecainide, a class I antiarrhythmic drug, on ventricular arrhythmias, ventricular abnormal automaticity and ventricular activation were examined in a canine model of myocardial infarction, and compared with those of lidocaine. The effects of the drugs were examined on (1) the arrhythmias developed 24 h after the left anterior descending coronary artery (LAD) ligation, (2) ventricular premature stimulation-induced arrhythmias 5 to 7 d after LAD ligation, (3) ventricular abnormal automaticity about 24 h after LAD ligation and (4) ventricular activation induced by a ventricular stimulation at various coupling intervals in animals 5 to 7 d after LAD ligation. Flecainide (1 and 3 mg/kg) showed a marked reduction in the frequency of ventricular ectopic beats 24 h after LAD ligation, and was more potent than lidocaine. The ventricular abnormal automaticity was inhibited by flecainide (1 and 3 mg/kg) and lidocaine (10 mg/kg). Flecainide (1 and 3 mg/kg) prolonged the activation time in the infarcted zones over a wide range of the coupling intervals, and produced block of seriously delayed activation. In contrast, lidocaine produced similar effects only at short coupling intervals. Ventricular premature stimulation produced ventricular arrhythmias, which were prevented by pretreatment with flecainide (3 mg/kg). In conclusion, flecainide showed antiarrhythmic effects in a canine model of myocardial infarction. A marked inhibition of ventricular abnormal automaticity and selective depression of delayed activation in the infarcted zone probably contribute to its antiarrhythmic effect.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 5","pages":"191-201"},"PeriodicalIF":0.0,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.191","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12696681","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: 1

Enhanced elimination of theophylline, phenobarbital and strychnine from the bodies of rats and mice by squalane treatment. 角鲨烷处理增强大鼠和小鼠体内茶碱、苯巴比妥和士的宁的消除。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.215

H Kamimura, N Koga, K Oguri, H Yoshimura

引用次数: 51

Study on proteoglycans having low-sulfated chondroitin 4-sulfate in human urine and serum. 人尿和血清中低硫酸软骨素-硫酸蛋白多糖的研究。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.231

T Imanari, A Shinbo, H Ochiai, T Ikei, I Koshiishi, H Toyoda

引用次数: 18

A computer program (DCN) for numerical convolution and deconvolution of pharmacokinetic functions. 一个药代动力学函数的数值卷积和反卷积的计算机程序。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.203

J M Lanao, M T Vicente, M L Sayalero, A Domínguez-Gil

{"title":"A computer program (DCN) for numerical convolution and deconvolution of pharmacokinetic functions.","authors":"J M Lanao, M T Vicente, M L Sayalero, A Domínguez-Gil","doi":"10.1248/bpb1978.15.203","DOIUrl":"https://doi.org/10.1248/bpb1978.15.203","url":null,"abstract":"A program adapted for use on microcomputers (DCN) has been developed which permits one to perform operations of numerical convolution and deconvolution using polyexponential functions, that are often implemented in pharmacokinetic analysis. The program is written in Microsoft GWBASIC and can be used in personal computers with no modification. The user supplies information relating to the coefficients and exponentials defining the polyexponential equation of the response and weighting functions and the program performs the deconvolution operation by numerical integration using trapezoidal rule and provides numerical and graphic information concerning the input function. The program can be applied to the deconvolution of many linear pharmacokinetic systems and allows one to solve problems related to drug release, absorption, distribution, as well as others. Additionally, the program is able to perform the convolution operation if information about the input and weighting functions and is also able to simulate pharmacokinetic processes. The efficacy of the program was evaluated by comparison with several deconvolution algorithms, in particular that proposed by Veng-Pedersen and Iga.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 5","pages":"203-14"},"PeriodicalIF":0.0,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.203","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12696682","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: 6

Autoimmune kidney disease in MRL/lpr mice inhibited by OK-432; II. Effect of indomethacin. OK-432抑制MRL/lpr小鼠自身免疫性肾病的研究2吲哚美辛的效果。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.255

M Mihara, Y Ohsugi

引用次数: 1

Increase of migration of cultured endothelial cells by angiotensin-converting enzyme inhibitor derived from tuna muscle. 金枪鱼肌源性血管紧张素转换酶抑制剂对培养内皮细胞迁移的影响。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.223

Y Kohama, H Oka, N Murayama, K Iida, M Itoh, M Itoh, X Ying, T Mimura

{"title":"Increase of migration of cultured endothelial cells by angiotensin-converting enzyme inhibitor derived from tuna muscle.","authors":"Y Kohama, H Oka, N Murayama, K Iida, M Itoh, M Itoh, X Ying, T Mimura","doi":"10.1248/bpb1978.15.223","DOIUrl":"https://doi.org/10.1248/bpb1978.15.223","url":null,"abstract":"The influence of angiotensin-converting enzyme (ACE) inhibitory octapeptide derived from tuna muscle (tuna AI) on the bovine aorta endothelial cell (BAEC) migration was investigated, as compared with captopril. BAEC migration was quantitated 6 d after release from contact inhibition by a teflon fence assay. The culture grown in the presence of tuna AI (1 and 10 microM) clearly exhibited an increase in migration, compared with the control. The media collected from tuna AI (1 and 10 microM)-stimulated BAECs significantly exhibited the interleukin (IL) -1 activity that was detected by the thymocyte costimulation assay with phytohemagglutinin. Although tuna AI was a weaker ACE inhibitor than captopril, the increasing effect of tuna AI on the migration and the IL-1 generation in BAECs was slightly greater than that of captopril. In quiescent BAECs, tuna AI (1 microM) apparently induced c-myc and platelet derived growth factor (PDGF) A-chain messenger ribonucleic acid (mRNA) expressions within 30 min, which persisted for 6 h. In contrast, captopril induced a very low expression of c-myc mRNA, and had no relation to PDGF A-chain mRNA expression. These results suggest that the increase of BAEC migration by tuna AI, unlike captopril, is likely related to the induction or activation of IL-1, and c-myc and PDGF mRNAs, in addition to the inhibition of the conversion of endogenous angiotensin I to angiotensin II.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 5","pages":"223-9"},"PeriodicalIF":0.0,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.223","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12696030","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: 7

Effect of benzylidene derivative (novel antirheumatic agent) on chondrocyte metabolism. 苄基衍生物(新型抗风湿药)对软骨细胞代谢的影响。

Journal of pharmacobio-dynamics Pub Date : 1992-05-01 DOI: 10.1248/bpb1978.15.239

K Watanabe, F Kimura, M Shinmei

{"title":"Effect of benzylidene derivative (novel antirheumatic agent) on chondrocyte metabolism.","authors":"K Watanabe, F Kimura, M Shinmei","doi":"10.1248/bpb1978.15.239","DOIUrl":"https://doi.org/10.1248/bpb1978.15.239","url":null,"abstract":"The effects of protocatechualdehyde (PAL), one of the metabolites of 3,4-diacetoxy benzylidene diacetate (ACP), on proteoglycan metabolism and secretion of interleukin 1 (IL-1) like activity (lymphocyte activating factor; LAF activity) were studied using rabbit articular chondrocytes culture under phorbol myristate acetate (PMA) and Ca2+ ionophore A23187 (A23187) or IL-1 alpha stimulation. In IL-1 alpha (20 u/ml) or PMA (0.1 micrograms/ml) and A23187 (0.2 micrograms/ml) treated culture of rabbit articular chondrocytes, PAL significantly reduced the degradation of 35S-proteoglycan (35S-PG) from the cells and matrix layers into the culture media in a dose dependent fashion without affecting proteoglycan synthesis. Similarly, the secretion or production of matrix metalloproteinases which degrade proteoglycans was also inhibited to the same extent under IL-1 alpha stimulated condition. However, PAL caused no effect on the secretion of IL-1 like activity by chondrocytes. These results suggest that an attractive candidate for an anti-inflammatory drug, ACP, which is a prodrug of PAL, has also a favorable action on chondrocyte metabolism in terms of proteoglycan degradation via inhibition of matrix metalloproteinases secretion or production.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 5","pages":"239-46"},"PeriodicalIF":0.0,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.239","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12696031","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

Proceedings of the 19th Symposium on Pharmacological Activity and Mechanism. Kyoto, November 21-22, 1991. Abstracts. 第十九届药理活性与机制学术研讨会论文集。1991年11月21日至22日，京都。摘要。

Journal of pharmacobio-dynamics Pub Date : 1992-04-01

引用次数: 0

Accumulation of propranolol in cultured rat fibroblasts. 心得安在培养的大鼠成纤维细胞中的积累。

Journal of pharmacobio-dynamics Pub Date : 1992-04-01 DOI: 10.1248/bpb1978.15.181

N Kita, N Sugihara, K Furuno

{"title":"Accumulation of propranolol in cultured rat fibroblasts.","authors":"N Kita, N Sugihara, K Furuno","doi":"10.1248/bpb1978.15.181","DOIUrl":"https://doi.org/10.1248/bpb1978.15.181","url":null,"abstract":"In order to clarify the involvement of phosphatidylserine (PhS) in the cellular accumulation of propranolol, we have characterized the binding of 3H-propranolol to cultured rat fibroblasts and to liposomes containing PhS. The properties of propranolol binding to the cells and liposomes were analyzed by means of a Scatchard plot. The cells contained at least two classes of propranolol binding sites, one site of high affinity/low capacity and the second site of lower affinity/higher capacity, while the liposomes contained only one class of binding site. The values of the association constant (K) and number of binding sites (n), given on a PhS basis for the propranolol binding site in the liposomes, were both very close to those of corresponding binding parameters for the high affinity/low capacity binding site in the cells. Cell death, caused by various toxic reagents, resulted in a marked decrease in propranolol accumulation in the cells. Kinetic analysis of the drug binding to dead cells showed one binding site with binding parameters comparable to those of the low affinity/high capacity binding site in the intact cells. Polar cations, methylamine and NH4Cl, completely inhibited propranolol binding to the liposomes. On the other hand, these cations partially inhibited propranolol accumulation in intact cells and failed to inhibit the drug binding to dead cells. These results suggest that PhS in cytomembranes represents the high affinity/low capacity propranolol binding site in cultured rat fibroblasts.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 4","pages":"181-9"},"PeriodicalIF":0.0,"publicationDate":"1992-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.181","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12665715","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: 2