keyword
https://read.qxmd.com/read/38503897/antiemetic-activity-of-abietic-acid-possibly-through-the-5ht-3-and-muscarinic-receptors-interaction-pathways
#1
JOURNAL ARTICLE
Rubel Hasan, Abdulrahman Alshammari, Norah A Albekairi, Md Shimul Bhuia, Meher Afroz, Raihan Chowdhury, Muhammad Ali Khan, Siddique Akber Ansari, Irfan Aamer Ansari, Mohammad S Mubarak, Muhammad Torequl Islam
The present study was designed to evaluate the antiemetic activity of abietic acid (AA) using in vivo and in silico studies. To assess the effect, doses of 50 mg/kg b.w. copper sulfate (CuSO4 ⋅5H2 O) were given orally to 2-day-old chicks. The test compound (AA) was given orally at two doses of 20 and 40 mg/kg b.w. On the other hand, aprepitant (16 mg/kg), domperidone (6 mg/kg), diphenhydramine (10 mg/kg), hyoscine (21 mg/kg), and ondansetron (5 mg/kg) were administered orally as positive controls (PCs)...
March 19, 2024: Scientific Reports
https://read.qxmd.com/read/38495220/symmetrical-bispyridinium-compounds-act-as-open-channel-blockers-of-cation-selective-ion-channels
#2
JOURNAL ARTICLE
Yves Haufe, Dominik Loser, Timm Danker, Annette Nicke
Current treatments against organophosphate poisoning (OPP) do not directly address effects mediated by the overstimulation of nicotinic acetylcholine receptors (nAChR). Non-oxime bispyridinium compounds (BPC) promote acetylcholine esterase-independent recovery of organophosphate-induced paralysis. Here, we test the hypothesis that they act by positive modulatory action on nAChRs. Using two-electrode voltage clamp analysis in combination with mutagenesis and molecular docking analysis, the potency and molecular mode of action of a series of nine BPCs was investigated on human α7 and muscle-type nAChRs expressed in Xenopus laevis oocytes...
March 8, 2024: ACS Pharmacology & Translational Science
https://read.qxmd.com/read/38140516/assessment-of-quercetin-antiemetic-properties-in-vivo-and-in-silico-investigations-on-receptor-binding-affinity-and-synergistic-effects
#3
JOURNAL ARTICLE
Raihan Chowdhury, Md Shimul Bhuia, Asraful Islam Rakib, Rubel Hasan, Henrique Douglas Melo Coutinho, Isaac Moura Araújo, Irwin Rose Alencar de Menezes, Muhammad Torequl Islam
Quercetin (QUA), a flavonoid compound, is ubiquitously found in plants and has demonstrated a diverse range of biological activities. The primary objective of the current study is to assess the potential antiemetic properties of QUA using an in vivo and in silico approach. In this experiment, 4-day-old chicks were purchased to induce emesis by orally administering copper sulfate pentahydrate (CuSO4 ·5H2 O) at a dose of 50 mg/kg (orally). Domperidone (DOM) (6 mg/kg), Hyoscine (HYS) (21 mg/kg), and Ondansetron (OND) (5 mg/kg) were treated as positive controls (PCs), and distilled water and a trace amount of Tween 80 mixture was employed as a negative control (NC)...
December 18, 2023: Plants (Basel, Switzerland)
https://read.qxmd.com/read/38123184/anti-inflammatory-and-antinociceptive-effects-of-sitagliptin-in-animal-models-and-possible-mechanisms-involved-in-the-antinociceptive-activity
#4
JOURNAL ARTICLE
Valiollah Hajhashemi, Hossein Sadeghi, Fatemeh Karimi Madab
BACKGROUND: : Sitagliptin is an antidiabetic drug that inhibits dipeptidyl peptidase-4 enzyme. This study aimed to investigate the antinociceptive and anti-inflammatory effects of sitagliptin in formalin and carrageenan tests and determine the possible mechanism(s) of its antinociceptive activity. METHODS: : Male Swiss mice (25-30 g) and male Wistar rats (180-220 g) were used for formalin and carrageenan tests, respectively. In the formalin test, paw licking time and in the carrageenan test, paw thickness were considered as indexes of pain behavior and inflammation respectively...
December 21, 2023: Korean Journal of Pain
https://read.qxmd.com/read/38097487/optimizing-high-dose-melphalan
#5
REVIEW
Gunjan Shah, Sergio Giralt, Parastoo Dahi
Melphalan, has been a major component of myeloma therapy since the 1950s. In the context of hematopoietic cell transplantation (HCT), high dose melphalan (HDM) is the most common conditioning regimen used due to its potent anti-myeloma effects and manageable toxicities. Common toxicities associated with HDM include myelosuppression, gastrointestinal issues, and mucositis. Established approaches to reduce these toxicities encompass dose modification, nausea prophylaxis with 5HT3 receptor antagonists, cryotherapy, amifostine use, and growth factors...
March 2024: Blood Reviews
https://read.qxmd.com/read/38074658/comparison-of-netupitant-palonosetron-with-5-hydroxytryptamine-3-receptor-antagonist-in-preventing-of-chemotherapy-induced-nausea-and-vomiting-in-patients-undergoing-hematopoietic-stem-cell-transplantation
#6
JOURNAL ARTICLE
Hang Zhang, Qiang Zeng, Tian Dong, Xinchuan Chen, Pu Kuang, Jian Li, Qiuhui Wu, Ting Liu, Ting Niu, Zhigang Liu, Jie Ji
BACKGROUND: The use of 5-hydroxytryptamine-3 receptor antagonists (5HT3 RA) has long been considered the standard regimen for preventing chemotherapy-induced nausea and vomiting (CINV) prior to hematopoietic stem cell transplantation (HSCT). However, their therapeutic outcomes have been unsatisfactory. NEPA, an oral formulation combining the neurokinin-1 receptor antagonist netupitant and the 5HT3 RA palonosetron, has received regulatory approval for the management of highly and moderately emetogenic chemotherapy...
2023: Frontiers in Oncology
https://read.qxmd.com/read/37920212/5-7-dimethoxycoumarin-ameliorates-vincristine-induced-neuropathic-pain-potential-role-of-5ht-3-receptors-and-monoamines
#7
JOURNAL ARTICLE
Muhammad Usman, Hurmat Malik, Ahmed Tokhi, Mehreen Arif, Zilli Huma, Khalid Rauf, Robert D E Sewell
Vincristine is the drug of choice for Hodgkin's lymphoma, acute lymphoblastic leukemia, and non-Hodgkin lymphoma. Despite its significant anticancer effects, it causes dose-dependent neuropathy, leading to compulsive dose reduction. The available drugs used for vincristine-induced neuropathic pain (VINP) have a range of safety, efficacy, and tolerability issues prompting a search for new therapies. 5,7-Dimethoxycoumarin (5,7-DMC) also known as citropten, is a natural coumarin found in the essential oils of citrus plants such as lime, lemons, and bergamots, and it possesses both antidepressant and anti-inflammatory effects...
2023: Frontiers in Pharmacology
https://read.qxmd.com/read/37863383/antiemetic-effects-of-sclareol-possibly-through-5-ht-3-and-d-2-receptor-interaction-pathways-in-vivo-and-in-silico-studies
#8
JOURNAL ARTICLE
Mehedi Hasan Bappi, Abdullah Al Shamsh Prottay, Khattab Al-Khafaji, Md Showkoth Akbor, Muhammad Kamal Hossain, Md Shahazul Islam, Afia Ibnath Asha, Cassio Rocha Medeiros, Catarina Martins Tahim, Elaine Cristina Pereira Lucetti, Henrique Douglas Melo Coutinho, Hossam Kamli, Muhammad Torequl Islam
BACKGROUND: Emesis is a complex physiological phenomenon that serves as a defense against numerous toxins, stressful situations, adverse medication responses, chemotherapy, and movement. Nevertheless, preventing emesis during chemotherapy or other situations is a significant issue for researchers. Hence, the majority view contends that successfully combining therapy is the best course of action. In-vivo analysis offers a more comprehensive grasp of how compounds behave within a complex biological environment, whereas in-silico evaluation refers to the use of computational models to forecast biological interactions...
October 18, 2023: Food and Chemical Toxicology
https://read.qxmd.com/read/37620158/multimodal-imaging-for-validation-and-optimization-of-ion-channel-based-chemogenetics-in-nonhuman-primates
#9
JOURNAL ARTICLE
Yuki Hori, Yuji Nagai, Yukiko Hori, Kei Oyama, Koki Mimura, Toshiyuki Hirabayashi, Ken-Ichi Inoue, Masayuki Fujinaga, Ming-Rong Zhang, Masahiko Takada, Makoto Higuchi, Takafumi Minamimoto
Chemogenetic tools provide an opportunity to manipulate neuronal activity and behavior selectively and repeatedly in nonhuman primates (NHPs) with minimal invasiveness. Designer Receptors Exclusively Activated by Designer Drugs are one example that is based on mutated muscarinic acetylcholine receptors. Another channel-based chemogenetic system available for neuronal modulation in NHPs uses Pharmacologically Selective Actuator Modules (PSAMs), which are selectively activated by Pharmacologically Selective Effector Molecules (PSEMs)...
August 22, 2023: Journal of Neuroscience
https://read.qxmd.com/read/37584820/a-re-consideration-of-neural-receptor-mechanisms-in-chemotherapy-induced-nausea-and-vomiting-current-scenario-and-future-perspective
#10
REVIEW
Ihsan Ullah, Muhammad Ayaz
The neural mechanisms and the receptors behind the course of chemotherapy-induced nausea and vomiting (CINV) are well described and considered mechanistically multifactorial, whereas the neurobiology of nausea is not completely understood yet. Some of the anti-neoplastic medications like cisplatin result in biphasic vomiting response. The acute phase of vomiting is triggered mainly via the release of serotonin from the enterochromaffin (EC) cells in the gastrointestinal tract (GIT) and results in stimulation of dorsal vagal complex (DVC) of the vomiting center and the vomiting is initiated by downward communication to the gut via vagal efferents...
August 16, 2023: Pharmacological Reports: PR
https://read.qxmd.com/read/37042928/interaction-between-escitalopram-and-ibuprofen-or-paracetamol-dft-and-molecular-docking-on-the-drug-drug-interactions
#11
JOURNAL ARTICLE
Musa Daboe, Cemal Parlak, Amani Direm, Özgür Alver, Ponnadurai Ramasami
A large number of drugs are introduced each year to treat different diseases. Most of the time, patients suffer from more than one health problem which makes it necessary to take multiple drugs. When drugs are combined, the problem of drug-drug interaction becomes relevant. In this work, we studied the drug-drug interaction between escitalopram and ibuprofen or paracetamol using density functional theory and quantum theory of atoms in molecules. The results suggest that following the interactions, the activity of drugs changes according to site of interaction...
April 12, 2023: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/36919029/modulatory-effects-of-phytol-on-the-antiemetic-property-of-domperidone-possibly-through-the-d-2-receptor-interaction-pathway-in-vivo-and-in-silico-studies
#12
JOURNAL ARTICLE
Md Shimul Bhuia, Tawhida Islam, Md Rokonuzzman, Abdullah Al Shamsh Prottay, Fatama Akter, Md Imran Hossain, Raihan Chowdhury, Md Azim Kazi, Abul Bashar Ripon Khalipha, Henrique Doouglas Melo Coutinho, Muhammad Torequl Islam
The current study is designed to evaluate the antiemetic effect of the diterpenoid phytol (PHY) using in vivo and in silico studies. For this, emesis was induced in 4-day-old chicks by the oral administration of copper sulfate (CuSO4 .5H2 O) at 50 mg/kg. To see the possible antiemetic mechanism of PHY, we used a number of reference drugs such as domperidone (80 mg/kg), ondansetron (24 mg/kg) and hyoscine (100 mg/kg) as positive controls, while the vehicle served as a negative control group...
April 2023: 3 Biotech
https://read.qxmd.com/read/36915290/diffuse-noxious-inhibitory-controls-in-chronic-joint-inflammatory-pain-study-of-the-descending-serotonergic-modulation-mediated-through-5ht3-receptors
#13
JOURNAL ARTICLE
Raquel Pereira-Silva, Paula Serrão, Fani Lourença Neto, Isabel Martins
The loss of diffuse noxious inhibitory controls (DNIC) is recognized as a predictor of chronic pain. Mechanistically, DNIC produces analgesia by a heterotopically applied conditioning-noxious stimulus (CS) and yet underexplored descending modulatory inputs. Here, we aimed at studying DNIC in monoarthritis (MA) by exploring the spinal component of the descending serotonergic system, specifically 5-hydroxytryptamine 3 receptors (5-HT3R). MA was induced in male Wistar rats by tibiotarsal injection of complete Freund's adjuvant...
2023: Neurobiology of Pain
https://read.qxmd.com/read/36852569/the-efficacy-of-5ht3-receptor-antagonists-in-postoperative-nausea-and-vomiting-the-role-of-pharmacogenetics
#14
JOURNAL ARTICLE
Polyxeni Theodosopoulou, Martina Rekatsina, Chryssoula Staikou
INTRODUCTION: Genetic variants may affect drug efficacy on postoperative nausea and vomiting (PONV). The understanding of these mechanisms will help to identify the surgical patients who might benefit from specific prophylactic and therapeutic antiemetic treatment. The aim of the present review was to investigate gene polymorphisms that influence 5-hydroxytryptamine (serotonin) type 3 receptor antagonists (5HT3RA) efficacy in PONV. EVIDENCE AQUISITION: We included articles published from 2005 to 2022, utilizing the electronic databases PUBMED, EMBASE, COHRANE Library and ScienceDirect...
February 27, 2023: Minerva Anestesiologica
https://read.qxmd.com/read/36774658/efficacy-and-safety-of-antiemetic-regimens-for-highly-emetogenic-chemotherapy-induced-nausea-and-vomiting-a-systematic-review-and-network-meta-analysis
#15
REVIEW
Marco Filetti, Pasquale Lombardi, Raffaele Giusti, Rosa Falcone, Florian Scotte, Diana Giannarelli, Antonella Carcagnì, Valeria Altamura, Giovanni Scambia, Gennaro Daniele
BACKGROUND: Several regimens have been introduced in clinical practice in the last twenty years to treat chemotherapy-induced nausea and vomiting (CINV). However, direct comparative data remain insufficient, as many new regimes lack head-to-head comparisons. In this study, through an indirect comparison, we overcome this limit by providing the most up-to-date estimate of the efficacy and safety of all combinations used for HEC-induced nausea and vomiting. PATIENTS AND METHODS: We retrieved randomized controlled trials (RCTs) published in Pubmed, Embase, and Cochrane Library until June, 30th 2022...
April 2023: Cancer Treatment Reviews
https://read.qxmd.com/read/36737400/embryo-fetal-safety-evaluation-of-ondansetron-in-rats
#16
JOURNAL ARTICLE
Ana Carolina Casali Reis, Bárbara Campos Jorge, Suyane da Silva Moreira, Júlia Stein, Carolina Barizan Perdão, Beatriz de Matos Manoel, Arielle Cristina Arena
BACKGROUND: Ondansetron is a 5HT3 receptor antagonist, used to mitigate the effects of nausea and vomiting after chemotherapy or surgery. Since nausea and vomiting are common experiences during the first trimester of pregnancy, this antiemetic has been the main drug used during this period. METHODS: To evaluate the effects of ondansetron on the embryo-fetal development, which are still very contradictory, pregnant rats were exposed to therapeutic doses of ondansetron (1...
April 1, 2023: Birth Defects Research
https://read.qxmd.com/read/36442580/safety-evaluation-of-ondansetron-after-gestational-exposure-on-male-reproductive-parameters-in-rats
#17
JOURNAL ARTICLE
Ana Carolina Casali Reis, Bárbara Campos Jorge, Julia Stein, Suyane da Silva Moreira, Beatriz de Matos Manoel, Ariana Musa Aquino, Leticia Cardoso Valente, Cândida Aparecida Leite Kassuya, Wellerson Rodrigo Scarano, Arielle Cristina Arena
Ondansetron is a 5HT3 receptor antagonist widely used to treat hyperemesis gravidarum, although its safety is still questionable. Since 5HT3 receptors, which are the target of this drug, can interfere with brain development through changes in neurotransmitter levels, this study evaluated whether the prenatal exposure to this drug could compromise reproductive and behavioral parameters in male offspring. Pregnant rats were treated with ondansetron (1.7 and 2.5 mg/kg/body weight; gavage), from gestational day 1-21...
November 25, 2022: Regulatory Toxicology and Pharmacology: RTP
https://read.qxmd.com/read/36033477/primary-versus-secondary-antiemetic-prophylaxis-with-nk1-receptor-antagonists-in-patients-affected-by-gastrointestinal-malignancies-and-treated-with-a-doublet-or-triplet-combination-regimen-including-oxaliplatin-and-or-irinotecan-plus-fluoropyrimidines-a-propensity
#18
JOURNAL ARTICLE
Alessandro Parisi, Riccardo Giampieri, Alex Mammarella, Cristiano Felicetti, Lisa Salvatore, Maria Bensi, Maria Grazia Maratta, Antonia Strippoli, Roberto Filippi, Maria Antonietta Satolli, Angelica Petrillo, Bruno Daniele, Michele De Tursi, Pietro Di Marino, Guido Giordano, Matteo Landriscina, Pasquale Vitale, Ina Valeria Zurlo, Emanuela Dell'Aquila, Silverio Tomao, Ilaria Depetris, Francesca Romana Di Pietro, Federica Zoratto, Davide Ciardiello, Maria Vittoria Pensieri, Ornella Garrone, Barbara Galassi, Claudio Ferri, Rossana Berardi, Michele Ghidini
Aim: The aim of the current study is to investigate the impact of primary compared to secondary chemotherapy-induced nausea and vomiting (CINV) prophylaxis with NK1 receptor antagonists (NK1-RA) in patients affected by gastrointestinal malignancies and treated with oxaliplatin- and/or irinotecan-based doublet or triplet regimens. Study design and methods: Clinical data of patients affected by gastrointestinal malignancies, treated with an oxaliplatin and/or irinotecan-based doublet or triplet regimen as neo/adjuvant or advanced-line treatment, and who received NK1-RA as primary (from the first cycle of treatment) or secondary (after the onset of CINV with a previous regimen with 5HT3-RA and dexamethasone) prophylaxis for CINV, were retrospectively collected in an observational study involving 16 Italian centers...
2022: Frontiers in Oncology
https://read.qxmd.com/read/36027552/development-of-an-adrenocortical-cell-model-of-calcium-signaling-modulation-to-decipher-the-molecular-mechanisms-responsible-for-primary-aldosteronism
#19
JOURNAL ARTICLE
Bakhta Fedlaoui, Teresa Cosentino, Zeina Al Sayed, Isabelle Giscos-Douriez, Fabio L Fernandes-Rosa, Jean-Sebastien Hulot, Chris Magnus, Scott M Sternson, Maria-Christina Zennaro, Sheerazed Boulkroun
OBJECTIVE: Primary aldosteronism (PA) is the most frequent form of secondary hypertension. The identification of germline or somatic mutations in different genes coding for ion channels (KCNJ5, CACNA1D, CACNA1H and CLCN2) and ATPases (ATP1A1 and ATP2B3) defines PA as a channelopathy. These mutations promote activation of calcium signaling, the main trigger for aldosterone biosynthesis.The objective of our work was to elucidate, using chemogenetic tools, the molecular mechanisms underlying the development of PA by modulating sodium entry into the cells, mimicking some of known mutations identified in PA...
June 1, 2022: Journal of Hypertension
https://read.qxmd.com/read/35694199/prevention-and-treatment-of-neuraxial-morphine-induced-pruritus-a-scoping-review
#20
REVIEW
Leonie M Becker, Aart Jan W Teunissen, Joseph S H A Koopman
The addition of morphine to neuraxial anaesthesia leads to improved postoperative analgesia and lower opioid consumption, but is often accompanied by pruritus. Studies on preventing or treating pruritus show contradictory results. Our objective was to identify effective drugs for the prevention or treatment of pruritus by a scoping review of clinical trials. A systematic literature search was conducted in PubMed, Embase and Web of Science. We identified clinical trials investigating the prevention or treatment of neuraxial morphine-induced pruritus in adults...
2022: Journal of Pain Research
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