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V2 receptor

Ewa Szczepanska-Sadowska, Katarzyna Czarzasta, Agnieszka Cudnoch-Jedrzejewska
PURPOSE OF REVIEW: In many instances, the renin-angiotensin system (RAS) and the vasopressinergic system (VPS) are jointly activated by the same stimuli and engaged in the regulation of the same processes. RECENT FINDINGS: Angiotensin II (Ang II) and arginine vasopressin (AVP), which are the main active compounds of the RAS and the VPS, interact at several levels. Firstly, Ang II, acting on AT1 receptors (AT1R), plays a significant role in the release of AVP from vasopressinergic neurons and AVP, stimulating V1a receptors (V1aR), regulates the release of renin in the kidney...
March 19, 2018: Current Hypertension Reports
Wei-Chun Chang, Wei-Chung Cheng, Bi-Hua Cheng, Lumin Chen, Li-Jing Ju, Yu-Jer Ou, Long-Bin Jeng, Mei-Due Yang, Yao-Ching Hung, Wen-Lung Ma
Cholesterol affects cancer progression, and acetyl-CoA is the primary cholesterogenesis substrate. The previous work has defined cholesterol bioflux via lipoprotein/receptor route is the gastric cancer (GCa) prognosis biosignature. The prognosis importance of acetyl-CoA to cholesterogenesis (mevalonate pathway) in GCa is yet to be defined. Using Kaplan-Meier Plotter web-based gene survival analyzer and The Cancer Genome Atlas (TCGA)-database analyzed with DBdriver.v2 platform, we revealed acetyl-CoA production and the mevalonate pathway are associated with GCa prognosis...
March 1, 2018: Cancer Medicine
Yuichiro Kishimoto, Yoshinobu Nakamura, Shingo Harada, Takeshi Onohara, Satoru Kishimoto, Tomohiro Kurashiki, Yoshikazu Fujiwara, Motonobu Nishimura
BACKGROUND: Oral administration of tolvaptan, a vasopressin V2 receptor antagonist, significantly reduces deterioration of renal function, which has recently been highlighted as an exacerbating factor for adverse events in patients with acute heart failure. In the present study we tested the hypothesis that concomitant administration of tolvaptan with a conventional diuretic is beneficial for perioperative body fluid management in patients who have undergone cardiac surgery.Methods and Results:In all, 280 patients who underwent cardiac surgery were prospectively randomized to concomitant treatment with tolvaptan and a conventional diuretic (tolvaptan group; 147 patients) or treatment with a conventional diuretic alone (control group; 133 patients)...
February 21, 2018: Circulation Journal: Official Journal of the Japanese Circulation Society
Christina Demuth, Anne Tranberg Madsen, Britta Weber, Lin Wu, Peter Meldgaard, Boe Sandahl Sorensen
BACKGROUND: Lung cancer patients with an activating mutation in the EGFR (epidermal growth factor receptor) can develop resistance to erlotinib treatment, which is often mediated by the T790M resistance mutation in EGFR. The difficulties in obtaining biopsies at progression make it challenging to investigate the appearance of the T790M mutation at progression in large patient cohorts. We have used cell free DNA (cfDNA) from patients treated with erlotinib to investigate if the development of a T790M mutation coincides with the presence of an activating EGFR mutation in the pre-treatment blood sample...
February 15, 2018: BMC Cancer
Michele Iovino, Massimo Iacoviello, Giovanni De Pergola, Brunella Licchelli, Emanuela Iovino, Edoardo Guastamacchia, Vito Angelo Giagulli, Vincenzo Triggiani
The nonapeptide hormone vasopressin (VP), synthesized by the hypothalamic supraoptic and paraventricular nuclei, exerts important effects on cardiovascular system via its receptors V1, V2 and V3. Patients with congestive heart failure (CHF) present elevated plasma VP levels that induce vasoconstriction, left ventricular hypertrophy, and free water reabsorption that leads to edema and hyponatremia, markers of advanced CHF. Vaptans, antagonists of VP receptors, are able to increase urine output and plasma sodium levels without the increased risk of arrhythmic death induced by diuretics, even though, further studies are needed to establish a possible role of these drugs in the treatment of CHF...
February 11, 2018: Endocrine, Metabolic & Immune Disorders Drug Targets
Laia Sans-Atxer, Dominique Joly
Standard of care therapies for autosomal dominant polycystic kidney disease (ADPKD) may limit morbidity and mortality due to disease-related complications, but they do not delay disease progression. Tolvaptan, a selective vasopressin V2 receptor antagonist, delays the increase in kidney volume (a surrogate marker for disease progression), slows the decline in renal function, and reduces pain in ADPKD patients with relatively preserved renal function. The most common adverse events of tolvaptan are linked to its aquaretic effect, and rare cases of idiosyncratic hepatitis were observed...
2018: International Journal of Nephrology and Renovascular Disease
Anne-Sophie Salabert, Erick Mora-Ramirez, Marie Beaurain, Mathieu Alonso, Charlotte Fontan, Hafid Belhadj Tahar, Marie Laure Boizeau, Mathieu Tafani, Manuel Bardiès, Pierre Payoux
INTRODUCTION: The aim of this work was to study the biodistribution, metabolism and radiation dosimetry of rats injected with [18F]FNM using PET/CT images. This novel radiotracer targeting NMDA receptor has potential for investigation for neurological and psychiatric diseases. METHODS: Free fraction and stability in fresh human plasma were determined in vitro. PET/CT was performed on anesthetized rats. Organs were identified and 3D volumes of interest (VOIs) were manually drawn on the CT in the center of each organ...
December 21, 2017: Nuclear Medicine and Biology
Gheun-Ho Kim
Amyotrophic lateral sclerosis (ALS) patients rarely present with either syndrome of inappropriate antidiuretic hormone secretion or generalized edema. Tolvaptan is a selective vasopressin V2 receptor antagonist that produces effective aquaresis, and its use in ALS patients has not been previously reported. A 50-year-old male ALS patient was admitted because of both generalized edema and dilutional hyponatremia. These manifestations were refractory to conventional diuretics and fluid therapy, but a very brisk diuresis was induced by tolvaptan administration...
December 2017: Electrolyte & Blood Pressure: E & BP
Mi Liu, Ying Sun, Man Xu, Xiaowen Yu, Yue Zhang, Songming Huang, Guixia Ding, Aihua Zhang, Zhanjun Jia
Downregulation of aquaporins (AQPs) in obstructive kidney disease has been well demonstrated with elusive mechanisms. Our previous study indicated that mitochondrial dysfunction played crucial role in this process. However, it is still uncertain that how mitochondrial dysfunction affected the AQPs in obstructive kidney disease. This study was to investigate the role of mitochondria-derived oxidative stress in mediating obstruction-induced downregulation of AQPs. After UUO for 7 days, renal SOD2 (mitochondria-specific SOD) was reduced by 85%...
December 20, 2017: American Journal of Physiology. Renal Physiology
Shunichi Imai, Masahiro Shinoda, Hideaki Obara, Minoru Kitago, Taizo Hibi, Yuta Abe, Hiroshi Yagi, Kentaro Matsubara, Hisanobu Higashi, Osamu Itano, Yuko Kitagawa
BACKGROUND Tolvaptan, an antagonist of the vasopressin V2 receptor is a novel oral diuretic that promotes water excretion selectively. We have used furosemide as a primary diuretic and added human atrial natriuretic peptide (hANP) if necessary for fluid management postoperatively in living-donor liver transplantation (LDLT) recipients. Recently we introduced tolvaptan and used both tolvaptan and furosemide as primary diuretics. MATERIAL AND METHODS Clinical outcomes were compared between LDLT recipients whose postoperative fluid management was performed before (control group, n=10) and after (tolvaptan group, n=16) introduction of tolvaptan...
January 9, 2018: Annals of Transplantation: Quarterly of the Polish Transplantation Society
Floris H Groenendijk, Agnes Jager, Fatima Cardoso, Carolien H M van Deurzen
AIM: To evaluate the use of the MammaPrint assay, a 70-gene risk signature for early breast cancers, and to correlate genomic risk stratification with individual clinicopathological parameters and clinical risk as assessed by Adjuvant! Online. METHODS: A Dutch Pathology Registry (PALGA)-based cohort study consisting of 1916 patients for which 1946 MammaPrint assay results were synoptically reported from 2013 to 2016. We could retrospectively assess clinical risk for 1146 tumors (58...
January 5, 2018: Breast: Official Journal of the European Society of Mastology
Khurram Jamil, Stephen Chris Pappas, Krishna R Devarakonda
Terlipressin, a synthetic, systemic vasoconstrictor with selective activity at vasopressin-1 (V1) receptors, is a pro-drug for the endogenous/natural porcine hormone [Lys8]-vasopressin (LVP). We investigated binding and receptor-mediated cellular activities of terlipressin, LVP, and endogenous human hormone [Arg8]-vasopressin (AVP) at V1 and vasopressin-2 (V2) receptors. Cell membrane homogenates of Chinese hamster ovary cells expressing human V1 and V2 receptors were used in competitive binding assays to measure receptor-binding activity...
2018: Journal of Experimental Pharmacology
Alpesh N Amin, Jesse D Ortendahl, Amanda L Harmon, Siddhesh A Kamat, Robert A Stellhorn, Sandra L Chase, Shirin V Sundar
OBJECTIVE: Assess characteristics of patients with heart failure (HF) and hyponatremia (HN) using tolvaptan, a selective vasopressin V2-receptor antagonist, for sodium correction, and estimate the budget impact of tolvaptan use in a hospital. METHODS: The Premier hospital database was analyzed to assess the utilization of tolvaptan, characteristics of users and non-users, and hospitalization costs among patients with HF and HN. Using these findings, a model was developed to estimate tolvaptan costs in proportion to total medical costs of managing patients with HF and HN, and the budget impact of tolvaptan use...
March 2018: Current Medical Research and Opinion
Rania Nasrallah, Joseph Zimpelmann, David Eckert, Jamie Ghossein, Sean Geddes, Jean-Claude Beique, Jean-Francois Thibodeau, Chris R J Kennedy, Kevin D Burns, Richard L Hébert
PGE2 regulates glomerular hemodynamics, renin secretion, and tubular transport. This study examined the contribution of PGE2 EP1 receptors to sodium and water homeostasis. Male EP1-/- mice were bred with hypertensive TTRhRen mice (Htn) to evaluate blood pressure and kidney function at 8 weeks of age in four groups: wildtype (WT), EP1-/-, Htn, HtnEP1-/-. Blood pressure and water balance were unaffected by EP1 deletion. COX1 and mPGE2 synthase were increased and COX2 was decreased in mice lacking EP1, with increases in EP3 and reductions in EP2 and EP4 mRNA throughout the nephron...
December 18, 2017: Laboratory Investigation; a Journal of Technical Methods and Pathology
Lauretta Odogwu, Luckson Mathieu, Kirsten B Goldberg, Gideon M Blumenthal, Erin Larkins, Mallorie H Fiero, Lisa Rodriguez, Karen Bijwaard, Eunice Y Lee, Reena Philip, Ingrid Fan, Martha Donoghue, Patricia Keegan, Amy McKee, Richard Pazdur
On March 30, 2017, the U.S. Food and Drug Administration (FDA) approved osimertinib for the treatment of patients with metastatic, epidermal growth factor receptor (EGFR) T790M mutation-positive, non-small cell lung cancer (NSCLC), as detected by an FDA-approved test, whose disease has progressed following EGFR tyrosine kinase inhibitor (TKI) therapy. Approval was based on demonstration of a statistically significant difference in the primary endpoint of progression-free survival (PFS) when comparing osimertinib with chemotherapy in an international, multicenter, open-label, randomized trial (AURA3)...
December 14, 2017: Oncologist
Masanori Atsukawa, Akihito Tsubota, Keizo Kato, Hiroshi Abe, Noritomo Shimada, Toru Asano, Tadashi Ikegami, Mai Koeda, Tomomi Okubo, Taeang Arai, Ai Nakagawa-Iwashita, Yuji Yoshida, Korenobu Hayama, Norio Itokawa, Chisa Kondo, Yoshimichi Chuganji, Yasushi Matsuzaki, Katsuhiko Iwakiri
BACKGROUND AND AIM: This study aimed to clarify the factors predictive of treatment response to tolvaptan (V2-receptor antagonist) for cirrhotic patients with hepatic edema in a real-world setting. METHODS: In this retrospective, multicenter study, tolvaptan was orally administered at a dose of 7.5 mg once a day. Patients with a decrease in body weight of 1.5 kg or greater from baseline were characterized as responders at day 7. RESULTS: Of 229 patients, 210 were subjected to this analysis...
December 7, 2017: Journal of Gastroenterology and Hepatology
Tatsuya Saito, Yasuko Tanaka, Yoshiyuki Morishita, Kenichi Ishibashi
Autosomal Dominant Polycystic Kidney Disease (ADPKD) is caused by the mutation of polycystins (PC-1 or PC-2), in which cysts start from the collecting duct to extend to all nephron segments with eventual end stage renal failure. The cyst development is attenuated by a vasopressin V2 receptor antagonist tolvaptan which, however, will not affect proximal tubule cysts devoid of V2 receptor. Aquaporin-11 (AQP11) is expressed selectively in the proximal tubule of the kidney and AQP11-null kidneys have a disruptive PC-1 trafficking to the plasma membrane to develop polycystic kidneys...
March 2018: Biochemistry and Biophysics Reports
Shivani Joshi, Per Brandstrom, Niels Gregersen, Søren Rittig, Jane Hvarregaard Christensen
Early diagnosis and treatment of congenital nephrogenic diabetes insipidus (CNDI) are essential due to the risk of intellectual disability caused by repeated episodes of dehydration and rapid rehydration. Timely genetic testing for disease-causing variants in the arginine vasopressin receptor 2 ( AVPR2 ) gene is possible in at-risk newborns with a known family history of X-linked CNDI. In this study, a Swedish male with no family history was diagnosed with CNDI at 6 months of age during an episode of gastroenteritis...
September 2017: Case Reports in Nephrology and Dialysis
Luca Visconti, Valeria Cernaro, Sebastiano Calimeri, Antonio Lacquaniti, Francesca De Gregorio, Carlo Alberto Ricciardi, Viviana Lacava, Domenico Santoro, Michele Buemi
The impact of water intake has been studied in several renal diseases. For example, increasing water intake is useful to prevent primary and secondary nephrolithiasis. In autosomal dominant polycystic kidney disease, arginine vasopressin (AVP) is involved in the progression of the disease, and water intake could play a therapeutic role by inhibiting the synthesis of AVP, but its efficacy is still controversial. Conversely, the use of aquaretics, which are antagonists of AVP V2 receptors, results in the reduction of the increase rate of total kidney volume with a slower decline of glomerular filtration rate...
November 14, 2017: Journal of Renal Nutrition
B J Kramers, M Storm, R T Gansevoort
Autosomal dominant polycystic kidney disease (ADPKD) is the most common hereditary renal disease, with a global prevalence of 10 per 10,000. It is characterized by the formation of numerous cysts in both kidneys, and leads to renal function loss; the majority of patients will eventually need renal replacement therapy. It is possible to screen patients' presymptomatic family members from a young age, but this has not historically been recommended as until recently there were no treatment options. This year, the vasopressin V2 receptor antagonist tolvaptan was approved for prescription in ADPKD, to slow the rate of renal function decline...
2017: Nederlands Tijdschrift Voor Geneeskunde
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