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Chinese Journal of Structural Chemistry 2019年第9期38卷 1421-1431页

作者： ZIBA Tavakoli Department of Chemistry Genaveh Branch Islamic Azad University Department of Chemistry Gachsaran Branch Islamic Azad University

In the present work, the interaction between drug granisetron(GRS) and BN(7,7-7) nanotube by density functional theory(DFT) calculations in the solvent water has been investigated. The non-bonded interaction effects of the molecule GRS with BN(7,7-7) nanotube on chemical shift tensors, natural charge and electronic properties such as the energy gap between HOMO and LUMO, global hardness, electronegativity and electronic chemical potential have been also detected. The natural bond orbital(NBO) analysis suggested that charge transfer depended between GRS and nanotube and induces a dipole moment in the complex. Then, the possibility of the use of BN(7,7-7) nanotube for GRS delivery to the diseased cells has been established.

关键词： granisetron BN(7,7-7) nanotube DFT adsorption NBO

Carbon monoxide contributes to the constipating effects of granisetron in rat colon

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World Journal of Gastroenterology 2016年第42期22卷 9333-9345页

作者： Carmela Nacci Margherita Fanelli Maria Assunta Potenza Valentina Leo Monica Montagnani Maria Antonietta De Salvia Department of Biomedical Sciences and Human Oncology - Pharmacology Section Medical School University of Bari "Aldo Moro" Department of Interdisciplinary Medicine Medical School University of Bari "Aldo Moro"

AIM To investigate the mechanisms underlying the potential contribution of the heme oxygenase/carbon monoxide(HO/CO) pathway in the constipating effects of granisetron. METHODS For in vivo studies, gastrointestinal motility was evaluated in male rats acutely treated with granisetron [25, 50, 75 μg/kg/subcutaneous(sc)], zinc protoporphyrin IX [Zn PPIX, 50 μg/kg/intraperitoneal(ip)] and hemin(50 μmol/L/kg/ip), alone or in combination. For in vitro studies, the contractile neurogenic response to electrical field stimulation(EFS, 3, 5, 10 Hz, 14 V, 1 ms, pulse trains lasting 10 s), as well as the contractile myogenic response to acetylcholine(ACh, 0.1-100 μmol/L) were evaluated on colon specimens incubated with granisetron(3 μmol/L, 15 min), Zn PPIX(10 μmol/L, 60 min) or CO-releasing molecule-3(CORM-3, 100, 200, 400 μmol/L) alone or in combination. These experiments were performed under co-treatment withor without atropine(3 μmol/L, a muscarinic receptor antagonist) or NG-nitro-L-Arginine(L-NNA, 100 μmol/L, a nitric oxide synthase inhibitor).RESULTS Administration of granisetron(50, 75 μg/kg) in vivo significantly increased the time to first defecation(P = 0.045 vs vehicle-treated rats), clearly suggesting a constipating effect of this drug. Although administration of Zn PPIX or hemin alone had no effect on this gastrointestinal motility parameter, Zn PPIX co-administered with granisetron abolished the granisetron-induced constipation. On the other hand, co-administration of hemin and granisetron did not modify the increased constipation observed under granisetron alone. When administered in vitro, granisetron alone(3 μmol/L) did not significantly modify the colon's contractile response to either EFS or ACh. Incubation with Zn PPIX alone(10 μmol/L) significantly reduced the colon's contractile response to EFS(P = 0.016) but had no effect on contractile response to ACh. Co-administration of Zn PPIX and atropine(3 μmol/L) abolished the Zn PPIX-mediated decrease in contrac

关键词： granisetron Carbon monoxide Heme oxygenase Colon Contraction Neurogenic response Myogenic response

Cathodic adsorptive stripping voltammetry of an anti-emetic agent granisetron in pharmaceutical formulation and biological matrix

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Journal of Pharmaceutical Analysis 2012年第6期2卷 443-449页

作者： Rajeev Jain Ramkishor Sharma School of Studies in Chemistry Jiwaji University

granisetron showed one well-defined reduction peak at Hanging Mercury Drop Electrode （HMDE） in the potential range from -1.3 to -1.5 V due to reduction of C=N bond. Solid-phase extraction technique was employed for extraction of granisetron from spiked human plasma. granisetron showed peak current enhancement of 4.45% at square-wave voltammetry and 5.33% at cyclic voltammetry as compared with the non stripping techniques. The proposed voltammetric method allowed quantification of granisetron in pharmaceutical formulation over the target concentration range of 5-200 ng/mL with detection limit 13.63 ng/mL, whereas in human plasma 50-225 ng/mL with detection limit 11.75 ng/mL.

关键词： granisetron Human plasma Solid-phase extraction Pharmaceuticalformulation Voltammetry Hanging mercury dropelectrode

granisetron Transdermal Patch for Treatment of Nausea in Patients Undergoing Cisplatin Based Chemotherapy for Cervical Cancer

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Journal of Cancer Therapy 2012年第6期3卷 1159-1163页

作者： Helen Dunnington Rodney Hunter Michael Frumovitz Judith Smith College of Pharmacy Texas Southern University Houston USA University of Texas M. D. Anderson Cancer Center Houston USA. University of Texas Medical School at Houston Houston USA University of Texas Medical School at Houston Houston USA&College of Pharmacy Texas Southern University Houston USA&University of Texas M. D. Anderson Cancer Center Houston USA

Objective: The purpose of this study was to define the incidence of chemotherapy-induced nausea and vomiting (CINV) in newly diagnosed cervical cancer patients receiving cisplatin and radiation treatment;and to determine if the granisetron transdermal patch (Sancuso?) would be appropriate to recommend as part of standard antiemetic regimen for the cisplatin radiation chemotherapy order set. Methods: This is a retrospective case-controlled study of cervical cancer patients receiving cisplatin chemotherapy with radiation (cisXRT);comparing patients receiving the granisetron transdermal patch to matched patients receiving oral 5HT3 blockers. All patients prescribed cisXRT between September 15th 2008 and November 30, 2011 were identified using pharmacy dispensing records. Patients were included if they received at least a partial dose of cisXRT and Sancuso? patch as standard antiemetic prophylaxis prior to cisXRT for cervical cancer treatment. Exclusion criteria included concomitant investigational agents, biotherapy and/or chemotherapy agents;prior chemotherapy;or incomplete or restricted medical records. Patients will be matched based on age. Patients were matched 3:1 (oral:patch). A total of 404 patients that received and completed cisXRT were identified utilizing an existing de-identified database from previous study were reviewed to evaluate parameters of interest. Results: A total of 285 patients’ medication records were reviewed for Sancuso? use, and 47 were identified. Of these 47 charts only five patient cases met eligibility criteria to be included in the study. All five patients that received the granisetron patch had at least three known risk factors for nausea. The nausea/vomiting in these patients did not worsen after receiving the Sancuso? patch, and four out of five had subjective improvement. CINV was unrelated to changes in laboratory values or incidence of other toxicity and was not dose-related. Conclusions: While no definitive conclusions could be d

关键词： granisetron Nausea Vomiting Cisplatin Radiation

granisetron——一种防治癌症化疗所致呕吐的新药

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四川生理科学杂志 1996年第1期18卷 33-35页

作者：朱玲华西医科大学药理教研室成都610041

granisetron为一种新型镇吐药,是5-HT_3受体选择性竞争拮抗剂,能有效地防治癌症化疗所致的恶心、呕吐,对放疗引起的呕吐也有效。granisetron与其它镇吐药相比,疗效确实,病人容易接受,极具应用潜力,最近已为美国FDA批准应用于临床。

关键词： granisetron 化疗所致呕吐防治癌症受体拮抗剂延迟呕吐锥体外系反应镇吐药灭吐灵癌症化疗临床试验

静脉注射与口服granisetron在CAP疗法中的止吐效果

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国际妇产科学杂志 1995年第5期 316-317页

作者：刘雅琴

对以往止吐治疗困难的施行CAP(环磷酰胺、阿霉素、顺铂)疗法中的卵巢癌患者使用5-羟色胺(5-hydroxytryptamine,5-HT)受体拮抗剂granisetron进行预防性的静脉注射或口服给药,探讨其止吐效果和副作用。对象是在卵巢癌化疗中恶心呕吐严重... 详细信息

对以往止吐治疗困难的施行CAP(环磷酰胺、阿霉素、顺铂)疗法中的卵巢癌患者使用5-羟色胺(5-hydroxytryptamine,5-HT)受体拮抗剂granisetron进行预防性的静脉注射或口服给药,探讨其止吐效果和副作用。对象是在卵巢癌化疗中恶心呕吐严重,对以往的止吐治疗药无效的7例。本次化疗是在第1天静脉滴注顺铂50mg一天、第1～5天分别静脉滴注表阿霉

关键词：止吐药静脉注射 granisetron CAP 疗法

格兰西农(granisetron)预防放射性呕吐

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国际输血及血液学杂志 1995年第6期 377-377页

作者：陈宁

骨髓移植(BMT)前预处理方案经常采用全身照射(TBI),其方法包括多次小剂量级(120～200cGy)及单剂量级缓慢(>6～8小时)或快速(约1小时)照射。目前以单剂量级快速照射应用更广,但该方法常引起严重恶心、呕吐而影响治疗,许多传

关键词：剂量级患者安定安定药放疗后甲氧氯普胺灭吐灵 granisetron TBI 镇吐药受体拮抗剂维持量氟甲去氢氢化可的松地塞米松

5-Hydroxytryptamine:a potential therapeutic target in amyotrophic lateral sclerosis

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Neural Regeneration Research 2023年第9期18卷 2047-2055页

作者： Shi-Shi Jiang Meng-Ni Gong Wei Rao Wen Chai Wen-Zhi Chen Xiong Zhang Hong-Bing Nie Ren-Shi Xu Medical College of Nanchang University Department of NeurologyJiangxi Provincial People’s HospitalThe First Affiliated Hospital of Nanchang Medical CollegeClinical College of Nanchang Medical CollegeNanchangJiangxi ProvinceChina Department of Neurology The First Affiliated Hospital of Nanchang UniversityNanchangJiangxi ProvinceChina Department of Neurology Maoming People’s HospitalMaomingGuangdong ProvinceChina

Previous studies have indicated that the pathogenesis of amyotrophic lateral sclerosis(ALS) is closely linked to 5-hydroxytryptamine(5-HT).To investigate this further,we administered 5-HT receptor antagonists to SOD1*G93A transgenic(ALS mouse model) and wide-type *** involved intraperitoneal injections of either granisetron,piboserod,or ritanserin,which inhibit the 5-HT3,5-HT4,and 5-HT2 receptors,*** transgenic mice were found to have fewer5-HT-positive cells in the spinal cord compared with wide-type *** found that the administration of granisetron reduced the body weight of the transgenic mice,while piboserod and ritanserin worsened the motor functioning,as assessed using a hanging wire ***,none of the 5-HT receptor antagonists affected the disease *** analyzed the distribution and/or expression of TAR DNA binding protein 43(TDP-43) and superoxide dismutase 1 G93A(SOD1-G93A),which fo rm abnormal aggregates in *** found that the expression of these proteins increased following the administration of all three 5-HT receptor *** addition,the disease-related mislocalization of TD P-43 to the cytoplasm increased markedly for all three *** ce rtain anatomical regions,the 5-HT receptor antagonists also led to a marked increase in the number of astrocytes and microglia and a decrease in the number of *** results indicate that 5-HT deficiency may play a role in the pathogenesis of amyotrophic lateral sclerosis by inducing the abnormal expression and/or distribution of TDP-43 and SOD1-G93A and by activating glial cells.5-HT co uld therefore be a potential therapeutic target for amyotrophic lateral sclerosis.

关键词： 5-hydroxytryptamine amyotrophic lateral sclerosis astrocytes granisetron microglia neuron piboserod ritanserin SOD1-G93A TAR DNA-binding protein 43