The Journal of pharmacy and pharmacology最新文献

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Modulation of NF-κB and MAPK signalling pathways by hydrolysable tannin fraction from Terminalia chebula fruits contributes to its anti-inflammatory action in RAW 264.7 cells. chebula果实水解单宁组分对NF-κB和MAPK信号通路的调节参与其对RAW 264.7细胞的抗炎作用
IF 3.3
The Journal of pharmacy and pharmacology Pub Date : 2022-05-20 DOI: 10.1093/jpp/rgab178
Sanmuga Priya Ekambaram, Jenifer Aruldhas, Aswini Srinivasan, Thamizharasi Erusappan
{"title":"Modulation of NF-κB and MAPK signalling pathways by hydrolysable tannin fraction from Terminalia chebula fruits contributes to its anti-inflammatory action in RAW 264.7 cells.","authors":"Sanmuga Priya Ekambaram,&nbsp;Jenifer Aruldhas,&nbsp;Aswini Srinivasan,&nbsp;Thamizharasi Erusappan","doi":"10.1093/jpp/rgab178","DOIUrl":"https://doi.org/10.1093/jpp/rgab178","url":null,"abstract":"<p><strong>Objectives: </strong>Hydrolysable tannin fraction (HTF) derived from Terminalia chebula fruit pericarps was assessed for its anti-inflammatory potential in LPS-induced RAW 264.7 cells. Its molecular mechanism was also established and compared with individual tannins - chebulagic acid (CH) and corilagin (CO).</p><p><strong>Methods: </strong>The effect of HTF on LPS-stimulated RAW 264.7 cells was studied by estimating the release of NO, ROS, cytokines and changes in nuclear morphology by DAPI staining. Furthermore, the effect of HTF, CO and CH was compared with the expression of p65, p38 and pERK proteins by immunoblotting and the mRNA transcript level of COX-2, iNOS and TNF-α by quantitative PCR. The in-silico interactions of various hydrolysable tannins present in HTF with molecular targets of inflammation were studied using Maestro software.</p><p><strong>Key findings: </strong>HTF at the dose levels of 25, 50 and 100 µg/ml was able to decrease the release of NO, ROS and cytokines from LPS-induced RAW 264.7 cells without disturbing the cell nuclear morphology. Investigation of molecular mechanism revealed that inhibition of NF-κB and MAPK signalling pathways was responsible for its anti-inflammatory action. The effect of HTF was higher than the individual tannins CH and CO.</p><p><strong>Conclusion: </strong>HTF can be developed as an effective anti-inflammatory agent.</p>","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":" ","pages":"718-729"},"PeriodicalIF":3.3,"publicationDate":"2022-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39604392","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: 8
Azadirachta indica A. Juss (neem) against diabetes mellitus: a critical review on its phytochemistry, pharmacology, and toxicology. 印楝抗糖尿病:植物化学、药理学和毒理学研究综述。
IF 3.3
The Journal of pharmacy and pharmacology Pub Date : 2022-05-20 DOI: 10.1093/jpp/rgab098
Shashank M Patil, Prithvi S Shirahatti, Ramith Ramu
{"title":"Azadirachta indica A. Juss (neem) against diabetes mellitus: a critical review on its phytochemistry, pharmacology, and toxicology.","authors":"Shashank M Patil,&nbsp;Prithvi S Shirahatti,&nbsp;Ramith Ramu","doi":"10.1093/jpp/rgab098","DOIUrl":"https://doi.org/10.1093/jpp/rgab098","url":null,"abstract":"<p><strong>Objective: </strong>We aim to provide a critical review focused on the various pharmacological activities of Azadirachta indica A. Juss related to diabetes management. We also emphasise on phytochemistry and toxicology of A. indica, which could provide a comprehensive approach for plant-based drug development in future.</p><p><strong>Key findings: </strong>From 2784 identified studies, only 83 were considered after double screening based on the inclusion criteria. Further, 63 pharmacological investigations were considered for review. Resultant studies deliberated on using different extracts and phytochemicals of A. indica on blood glucose level, lipid profile, oxidative stress, carbohydrate digestion enzymes, diabetic complications, glucose tolerance, and uptake of glucose.</p><p><strong>Summary: </strong>In the end, one can know the efficacy of A. indica as a potent antidiabetic herbal medicine. However, based on gaps in research, recommendations have been provided to evaluate A. indica. in a systematic manner to develop plant-based drugs, nutraceuticals, and to evaluate their clinical efficiency and safety against diabetes mellitus.</p>","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":" ","pages":"681-710"},"PeriodicalIF":3.3,"publicationDate":"2022-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39447762","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: 28
Platycarya strobilacea Sieb. et Zucc.: a review of its traditional uses, botany, phytochemistry, pharmacology and toxicology. 桔梗。调查。综述了其传统用途、植物学、植物化学、药理学和毒理学。
IF 3.3
The Journal of pharmacy and pharmacology Pub Date : 2022-05-20 DOI: 10.1093/jpp/rgab110
Peiyuan Zhao, Lizhu Han, Yunlan Wang, Jinqing Qiu, Xinbo Zhang, Zhishu Tang, Xi Duan, Xiao Song
{"title":"Platycarya strobilacea Sieb. et Zucc.: a review of its traditional uses, botany, phytochemistry, pharmacology and toxicology.","authors":"Peiyuan Zhao,&nbsp;Lizhu Han,&nbsp;Yunlan Wang,&nbsp;Jinqing Qiu,&nbsp;Xinbo Zhang,&nbsp;Zhishu Tang,&nbsp;Xi Duan,&nbsp;Xiao Song","doi":"10.1093/jpp/rgab110","DOIUrl":"https://doi.org/10.1093/jpp/rgab110","url":null,"abstract":"<p><strong>Objectives: </strong>Platycarya strobilacea Sieb. et Zucc. is the dry infructescence of P. strobilacea, a Juglandaceae plant and is a traditional Chinese medicine with great development potential and utilization value. This study summarizes the research progress on the traditional uses, botany, phytochemistry, extraction methods, pharmacology and toxicology of Platycarya strobilacea Sieb. et Zucc., and provides potential therapeutic uses and drug development prospects for this plant.</p><p><strong>Key findings: </strong>Phytochemical studies showed that this plant mainly contains volatile constituents, phenols, terpenoids and a carbohydrate. The pharmacological activity of Platycarya strobilacea Sieb. et Zucc. includes antibacterial and anti-inflammatory effects, anti-tumour effects and antioxidant effects. This plant is especially effective in the treatment of allergic rhinitis and chronic sinusitis.</p><p><strong>Summary: </strong>In this review, the phytochemistry and pharmacological effects of Platycarya strobilacea Sieb. et Zucc. are described in detail, which will have guiding significance for the future development of this drug.</p>","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":" ","pages":"646-659"},"PeriodicalIF":3.3,"publicationDate":"2022-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39318494","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
The effect of free and encapsulated cisplatin into long-circulating and pH-sensitive liposomes on IEC-6 cells during wound healing in the presence of host-microbiota. 在宿主微生物群存在的情况下,游离和包封的顺铂进入长循环和ph敏感脂质体对伤口愈合期间IEC-6细胞的影响。
IF 3.3
The Journal of pharmacy and pharmacology Pub Date : 2022-05-20 DOI: 10.1093/jpp/rgab156
Raquel Silva Araújo, Mônica Cristina Oliveira, Valbert Nascimento Cardoso, Dorothy M K Keefe, Andrea M Stringer
{"title":"The effect of free and encapsulated cisplatin into long-circulating and pH-sensitive liposomes on IEC-6 cells during wound healing in the presence of host-microbiota.","authors":"Raquel Silva Araújo,&nbsp;Mônica Cristina Oliveira,&nbsp;Valbert Nascimento Cardoso,&nbsp;Dorothy M K Keefe,&nbsp;Andrea M Stringer","doi":"10.1093/jpp/rgab156","DOIUrl":"https://doi.org/10.1093/jpp/rgab156","url":null,"abstract":"<p><strong>Objectives: </strong>To circumvent cisplatin (CDDP) toxic effects and improve the antitumoural effect, our research group developed long-circulating and pH-sensitive liposomes containing CDDP (SpHL-CDDP). This study aimed to evaluate whether SpHL-CDDP is associated with intestinal protection under in-vitro conditions in the presence of host-microbiota, compared with free CDDP.</p><p><strong>Methods: </strong>The cytotoxicity of CDDP and SpHL-CDDP were evaluated by colorimetric MTT and sulforhodamine B (SRB) assays. Epithelial proliferation was assessed by using an in-vitro wounding model in the presence of host-microbiota with intestinal epithelial cell line 6 (IEC-6) monolayers. Cytokines were determined by ELISA.</p><p><strong>Key findings: </strong>Reduced cytotoxicity of SpHL-CDDP in IEC-6 cells (minimum of 1.3-fold according to the IC50 values) was observed when compared with CDDP. The presence of microbiota or CDDP reduced the wound healing. The association of microbiota and SpHL-CDDP improved the wound healing and cell number in IEC-6 cells when compared with control. These beneficial results can be associated with increased IL-6 and IL-10 levels induced by SpHL-CDDP which were affected by the presence of microbiota.</p><p><strong>Conclusions: </strong>These results indicate that the presence of microbiota associated with SpHL-CDDP provided less intestinal cellular damages compared with CDDP and constitutes a promising candidate for clinical use.</p>","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":" ","pages":"711-717"},"PeriodicalIF":3.3,"publicationDate":"2022-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39634343","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
Triptolide ameliorates osteoarthritis by regulating nuclear factor kappa B-mediated inflammatory response. 雷公藤甲素通过调节核因子κ b介导的炎症反应来改善骨关节炎。
The Journal of pharmacy and pharmacology Pub Date : 2022-02-28 DOI: 10.1093/jpp/rgab182
Gang Liu, Laijie Wang, Muhadasi Tuerxunyiming, Jin Xu, Zaifeng Wu, Wei Wang, Hongyu Liu, Lin Lin, Qingbai Liu
{"title":"Triptolide ameliorates osteoarthritis by regulating nuclear factor kappa B-mediated inflammatory response.","authors":"Gang Liu, Laijie Wang, Muhadasi Tuerxunyiming, Jin Xu, Zaifeng Wu, Wei Wang, Hongyu Liu, Lin Lin, Qingbai Liu","doi":"10.1093/jpp/rgab182","DOIUrl":"https://doi.org/10.1093/jpp/rgab182","url":null,"abstract":"OBJECTIVES\u0000Osteoarthritis (OA) is a joint degenerative disease that commonly occurs in older people and affect the quality of life. Triptolide (TPL), a compound derived from Tripterygium wilfordii, has been shown to exhibit anti-inflammatory properties. Here, we investigated the therapeutic effect of TPL on the experimental OA as well as the underlying molecular mechanisms.\u0000\u0000\u0000METHODS\u0000OA models were established using monosodium iodoacetate (MIA) or surgery. The arthritis score and paw withdrawal threshold value of knees were used to evaluate the degree of arthritis. The level and expression of proinflammatory cytokines were evaluated by quantitative real-time PCR and ELISA kits.\u0000\u0000\u0000KEY FINDINGS\u0000In surgery and MIA-induced OA rats, TPL alleviated arthritis symptoms and reduced inflammatory cytokine production in serum. In primary chondrocytes, TPL dose-dependently reversed lipopolysaccharide (LPS)-induced cell proliferation. Moreover, LPS-induced cell apoptosis and the expressions of proinflammatory cytokines interleukin-(IL-)6, IL-8, IL-1β, IL-12, tumour necrosis factor-α (TNF-α) and interferon-gamma (INF-γ) were also attenuated by TPL. Mechanistically, the therapeutic effects of TPL on OA were effective by dampening nuclear factor kappa B (NF-κB) activity leading to reduced proinflammatory cytokines production and inflammatory response.\u0000\u0000\u0000CONCLUSIONS\u0000TPL acts as an effective therapeutic drug for OA by mediating NF-κB signalling, thereby leading to the reduced proinflammatory cytokines production and inflammatory response.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130145620","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
Protective effect of Liuwei Dihuang decoction on early diabetic nephropathy induced by streptozotocin via modulating ET-ROS axis and matrix metalloproteinase activity in rats. 六味地黄汤通过调节ET-ROS轴和基质金属蛋白酶活性对链脲佐菌素诱导的早期糖尿病肾病的保护作用。
IF 3.3
The Journal of pharmacy and pharmacology Pub Date : 2007-09-01 DOI: 10.1211/jpp.59.9.0015
Haibo He, Xianzhe Yang, Xiaowei Zeng, Mengqiong Shi, Jun Yang, Limao Wu, Lianda Li
{"title":"Protective effect of Liuwei Dihuang decoction on early diabetic nephropathy induced by streptozotocin via modulating ET-ROS axis and matrix metalloproteinase activity in rats.","authors":"Haibo He,&nbsp;Xianzhe Yang,&nbsp;Xiaowei Zeng,&nbsp;Mengqiong Shi,&nbsp;Jun Yang,&nbsp;Limao Wu,&nbsp;Lianda Li","doi":"10.1211/jpp.59.9.0015","DOIUrl":"https://doi.org/10.1211/jpp.59.9.0015","url":null,"abstract":"<p><p>We aimed to investigate the effects of Liuwei Dihuang decoction (LW) on the endothelin-1-reactive oxidative species (ET-ROS) system and matrix metalloproteinases (MMPs) in the early diabetic nephropathy induced by streptozotocin (STZ) in rats. Rats were divided into six groups as follows: the control group, the untreated model group, the treated groups with the LW (5, 10 and 15 g kg(-1), p.o.) and the aminoguanidine-treated group (100 mg kg(-1), orally). The treatment was performed for 4 weeks, beginning on the fifth week after one intraperitoneal injection of STZ (65 mg kg(-1)). In the untreated model group, increased blood glucose, decreased plasma insulin level and an impaired renal function were observed. There was an altered redox system shown by an increased malondialdehyde and decreased activity of glutathione peroxidase and superoxide dismutase in the renal cortex. An enhanced inducible nitric oxide synthetase, total nitric oxide synthase and constitutive nitric oxide synthase and a declined nitric oxide were found. An increased extracellular matrix was indicated by an abnormality of MMP-2 and MMP-9 activities and an increase in hydroxyproline. An up-regulated ET-1 level and increased mRNA expression of endothelin-converting enzyme, preproET-1 and ET( A) receptor were presented in the affected renal cortex, but no change in ET(B) receptor mRNA. The LW was most effective in reversing these changes in diabetic rats and was as effective as aminoguanidine. The benefits of the extracts in relieving the abnormalities in early diabetic nephropathy are likely to be mediated by suppression of the renal ET-ROS system and escalating the activity of MMPs.</p>","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":" ","pages":"1297-305"},"PeriodicalIF":3.3,"publicationDate":"2007-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40984844","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: 30
Increased cardiovascular responsiveness to central cholinergic stimulation in the genetically epilepsy-prone rat. 遗传性癫痫易感大鼠对中枢胆碱能刺激的心血管反应性增加。
The Journal of pharmacy and pharmacology Pub Date : 1992-09-01 DOI: 10.1016/1043-6618(92)91038-I
G. Trimarchi, C. Imperatore, F. Arcadi, A. Saija, A. De Sarro, G. De Sarro, G. Costa
{"title":"Increased cardiovascular responsiveness to central cholinergic stimulation in the genetically epilepsy-prone rat.","authors":"G. Trimarchi, C. Imperatore, F. Arcadi, A. Saija, A. De Sarro, G. De Sarro, G. Costa","doi":"10.1016/1043-6618(92)91038-I","DOIUrl":"https://doi.org/10.1016/1043-6618(92)91038-I","url":null,"abstract":"","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128465388","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
Skin wound healing: some biochemical parameters in guinea-pig. 豚鼠皮肤创面愈合的一些生化指标。
The Journal of pharmacy and pharmacology Pub Date : 1992-05-01 DOI: 10.1016/1043-6618(92)90432-B
F. Buffoni, G. Banchelli, S. Cambi, G. Ignesti, R. Pirisino, L. Raimondi, G. Vannelli
{"title":"Skin wound healing: some biochemical parameters in guinea-pig.","authors":"F. Buffoni, G. Banchelli, S. Cambi, G. Ignesti, R. Pirisino, L. Raimondi, G. Vannelli","doi":"10.1016/1043-6618(92)90432-B","DOIUrl":"https://doi.org/10.1016/1043-6618(92)90432-B","url":null,"abstract":"","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"20 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"117059026","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: 21
Effects of methylene blue on the uptake, release and metabolism of noradrenaline in mesenteric arterial vessels. 亚甲蓝对肠系膜动脉血管去甲肾上腺素摄取、释放和代谢的影响。
The Journal of pharmacy and pharmacology Pub Date : 1989-06-01 DOI: 10.1097/00132586-198906000-00053
P. Soares-da-Silva, M. Caramona
{"title":"Effects of methylene blue on the uptake, release and metabolism of noradrenaline in mesenteric arterial vessels.","authors":"P. Soares-da-Silva, M. Caramona","doi":"10.1097/00132586-198906000-00053","DOIUrl":"https://doi.org/10.1097/00132586-198906000-00053","url":null,"abstract":"Methylene blue (3, 10 and 30 microM) increased the spontaneous outflow of endogenous dopamine and noradrenaline from sympathetic nerves supplying the dog mesenteric artery and drastically reduced the formation of endogenous dihydroxyphenylglycol (DOPEG). In addition, it decreased the accumulation of [3H]noradrenaline in the tissue, reduced the formation of [3H]DOPEG and [3H]normetanephrine, without altering the formation of [3H]dihydroxymandelic acid. In tissue homogenates of the same blood vessel, methylene blue 30 and 100 microM produced a significant reduction in the deamination of 5-hydroxytryptamine (5-HT), beta-phenylethylamine (beta-PEA) and tyramine. Methylene blue increased the accumulation of [3H]isoprenaline in the tissue, and markedly reduced the formation of [3H]O-methylisoprenaline ([3H]OMI). These results show that methylene blue alters the storage and disposition of the adrenergic transmitter.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"17 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1989-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128072521","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
Alcuronium pharmacodynamics in dogs: effect-concentration relationships in the diaphragmatic and limb muscles. 阿库溴铵在狗体内的药效学:横膈膜和肢体肌肉的效应-浓度关系。
The Journal of pharmacy and pharmacology Pub Date : 1988-04-01 DOI: 10.1097/00132586-198804000-00029
J. Walker, C. Shanks, C. Borton, K. Brown
{"title":"Alcuronium pharmacodynamics in dogs: effect-concentration relationships in the diaphragmatic and limb muscles.","authors":"J. Walker, C. Shanks, C. Borton, K. Brown","doi":"10.1097/00132586-198804000-00029","DOIUrl":"https://doi.org/10.1097/00132586-198804000-00029","url":null,"abstract":"Previous studies suggest that the muscles of the diaphragm are less sensitive to neuromuscular blocking agents than the limb muscles. However, this difference has not been characterized directly in terms of relaxant drug plasma concentrations. The pharmacodynamics of the non-depolarizing muscle relaxant alcuronium were therefore investigated in nine dogs using a constant-rate infusion regimen with simultaneous measurement of muscle paralysis in the limb and diaphragm. Maximum paralysis between 95 and 100% was achieved in both muscle groups, within approximately the same time interval. However, during onset of and offset of effect, the pharmacodynamic parameters ECp50 and ECp95 for the limb muscle were lower than in the diaphragm. From a pharmacodynamic effect model it was also predicted that Css(50) and Css(95) for the limb muscles are half those values for the diaphragm. Thus, the diaphragm is less sensitive to the action of alcuronium than are limb muscles. The half-time for equilibration of alcuronium between plasma and the effect site was two-fold lower for the diaphragm, and the rate of recovery from paralysis in diaphragmatic muscles was twice that observed in limb muscles. Collectively, these data suggest that there is a greater margin of safety in the diaphragmatic muscles and that the response of the peripheral limb muscles to nerve stimulation provides only a conservative index of recovery from competitive neuromuscular block in the diaphragmatic muscles.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"19 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1988-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133658202","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
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