Article
Radiology, Nuclear Medicine & Medical Imaging
Mika Naganawa, Nabeel B. Nabulsi, David Matuskey, Shannan Henry, Jim Ropchan, Shu-Fei Lin, Hong Gao, Richard Pracitto, David Labaree, Ming-Rong Zhang, Tetsuya Suhara, Izumi Nishino, Helene Sabia, Satoshi Ozaki, Yiyun Huang, Richard E. Carson
Summary: Arginine vasopressin is an important hormone synthesized in the hypothalamus and stored in the posterior pituitary. The V-1B receptor (V1BR) is highly expressed in the pituitary and plays a crucial role in regulating the hypothalamic-pituitary-adrenal axis. C-11-TASP699 is a novel PET radiotracer with high affinity and selectivity for V1BR. This study characterized the pharmacokinetic and binding profiles of C-11-TASP699 in humans and investigated its utility in assessing the occupancy of the V1BR antagonist, TS-121.
JOURNAL OF NUCLEAR MEDICINE
(2022)
Article
Cardiac & Cardiovascular Systems
Fredrika Schill, Simon Timpka, Peter M. Nilsson, Olle Melander, Sofia Enhorning
Summary: The study found that elevated copeptin levels predict the development of HF in older adults, making it a risk marker for VP-driven HF susceptibility.
Article
Chemistry, Organic
Kaoru Funaki, Hidetsugu Tabata, Yusuke Nakazato, Yuka Takahashi, Tomohiko Tasaka, Hideyo Takahashi, Hideaki Natsugari, Tetsuta Oshitari
Summary: By performing the 5N-acylation reaction on 1N-methyl-1,5-benzodiazepin-2ones using (S)-2-phenylpropanoyl and (S)-2-phenylbutanoyl chlorides, the (a1S,a2S,S)-atropisomer (I) was obtained with high diastereoselectivity over the (a1R,a2R,S)-isomer (II). The preferential formation of I can be attributed to the thermodynamically preferable pi-pi stacking interaction between two benzene rings in the benzodiazepine ring and the acyl chloride during the reaction.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Review
Urology & Nephrology
Nathalia de Paula Doyle Maia, Karen de Carvalho Lopes, Fernando Freitas Gananca
Summary: This study aimed to describe the otorhinolaryngological adverse effects of the main drugs used in urological practice. The main drugs in urology were categorized into five groups, showing that they can cause dizziness, dry mouth, rhinitis, and other reactions. Physicians should be aware of these adverse effects to improve treatment adherence and minimize potential harm to patients.
INTERNATIONAL BRAZ J UROL
(2021)
Article
Biochemistry & Molecular Biology
Amelie M. Borie, Sena Agezo, Parker Lunsford, Arjen J. Boender, Ji-Dong Guo, Hong Zhu, Gordon J. Berman, Larry J. Young, Robert C. Liu
Summary: This study examines the role of oxytocin in the nucleus accumbens during pair bonding in prairie voles. The researchers found that oxytocin's actions change with social experience, regulating the trajectory of social interactions and potentially promoting the maintenance of a pair bond by inhibiting aggressive responses.
Review
Pharmacology & Pharmacy
Arianna Piffer, Mario G. Bianchetti, Corinna Leoni-Foglia, Giacomo D. Simonetti, Gregorio P. Milani, Sebastiano A. G. Lava
Summary: The use of vaptans in children for the treatment of oedematous and hyponatraemic disorders appears to be safe and effective, showing an increase in diuresis and sodium levels. However, no superiority over traditional treatment methods has been demonstrated.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2022)
Article
Urology & Nephrology
E. Cuka, M. Vespa, G. Joli, P. Manunta, T. M. Sciarrone Alibrandi
Summary: The case report describes a 37-year-old man with palmar hyperhidrosis who experienced complete resolution of symptoms when treated with tolvaptan for autosomic polycystic kidney disease. Suspension and reintroduction of tolvaptan were associated with reappearance and remission of palmar hyperhidrosis, suggesting a possible role of tolvaptan in central ACTH secretion.
JOURNAL OF NEPHROLOGY
(2022)
Review
Endocrinology & Metabolism
Svetlana Lebedeva, Arus Margaryan, Elena Smolyarchuk, Andrey Nedorubov, Maria Materenchuk, Alexander Tonevitsky, Kerim Mutig
Summary: Diabetic kidney disease is the major cause of chronic kidney disease, and enhanced plasma vasopressin levels have been associated with it. Vasopressin has diuretic effects in the kidneys and adaptive effects in other organs. Overactivation of certain vasopressin receptors can lead to kidney problems and worsen diabetic kidney disease.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Valeska Cid-Jofre, Macarena Moreno, Miguel Reyes-Parada, Georgina M. Renard
Summary: Oxytocin and vasopressin, originally known for their roles in reproduction and water homeostasis, have emerged as potential therapeutic targets for neuropsychiatric disorders. Novel ligands have been developed due to their chemical-physical characteristics, paving the way for clinical and preclinical trials in the treatment of CNS disorders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Health Care Sciences & Services
Eleni Laou, Nikolaos Papagiannakis, Androniki Papadopoulou, Theodora Choratta, Minas Sakellakis, Mariachiara Ippolito, Ioannis Pantazopoulos, Andrea Cortegiani, Athanasios Chalkias
Summary: This systematic review and meta-analysis aimed to investigate the effects of vasopressin receptor agonists in the resuscitation of hemorrhagic shock. The results showed no significant correlation between the use of vasopressin receptor agonists and mortality or hemodynamic parameters. However, due to heterogeneity in animal studies, more data are needed to draw certain conclusions.
JOURNAL OF PERSONALIZED MEDICINE
(2023)
Article
Medicine, General & Internal
Michelle N. Rheault, Charles E. Alpers, Jonathan Barratt, Stewart Bieler, Pietro Canetta, Dong-Wan Chae, Gaia Coppock, Ulysses Diva, Loreto Gesualdo, Hiddo J. L. Heerspink, Jula K. Inrig, Gianna M. Kirsztajn, Donald Kohan, Radko Komers, Laura A. Kooienga, Kenneth Lieberman, Alex Mercer, Irene L. Noronha, Vlado Perkovic, Jai Radhakrishnan, William Rote, Brad Rovin, Vladimir Tesar, Hernan Trimarchi, James Tumlin, Muh Geot Wong, Howard Trachtman, DUPRO Steering Comm, DUPLEX Investigators
Summary: In the treatment of FSGS, sparsentan showed a better reduction in proteinuria compared to irbesartan. However, there were no significant differences in eGFR slope between the two groups at 108 weeks. Both sparsentan and irbesartan demonstrated similar safety profiles.
NEW ENGLAND JOURNAL OF MEDICINE
(2023)
Article
Medicine, General & Internal
San-e Ishikawa, Hiroshi Funayama
Summary: Hyponatremia frequently occurs in congestive heart failure patients due to the release of arginine vasopressin (AVP) and salt and water retention. Recent studies have shown that hyponatremia predicts the prognosis of heart failure, increasing the risk of cardiac death and rehospitalization. Early development of hyponatremia in acute myocardial infarction also predicts worsening heart failure. The effectiveness of AVP V2 receptor inhibition and the potential benefits of a newly identified natriuretic factor in improving heart failure prognosis are still uncertain.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Chemistry, Organic
Ruyuan Ma, Yan-En Wang, Dan Xiong, Jianyou Mao
Summary: A tandem Madelung indole synthesis using methyl benzoate and N-methyl-o-toluidine as reactants has been discovered. The combination of LiN-(SiMe3)2 and CsF is crucial for the high efficiency of this tandem reaction, which produces a diverse array of N-methyl-2-phenylindoles. The scalability and poststructural modifications of this indole synthesis have also been demonstrated.
Review
Endocrinology & Metabolism
Haiyan Zheng, Ji Yeon Lim, Yerin Kim, Sang Taek Jung, Sun Wook Hwang
Summary: Oxytocin and vasopressin, neurohypophyseal hormones, play a central role in regulating bodily homeostasis and are strongly involved in downregulating pain. By modulating nociceptors, the first component of the pain signaling pathway, these peptides contribute to pain attenuation, sparking scientific interest in their physiological processes.
FRONTIERS IN NEUROENDOCRINOLOGY
(2021)
Article
Cardiac & Cardiovascular Systems
Joao Pedro Ferreira, Faiez Zannad, Stuart J. Pocock, Stefan D. Anker, Javed Butler, Gerasimos Filippatos, Martina Brueckmann, Waheed Jamal, Dominik Steubl, Elke Schueler, Milton Packer
Summary: In patients with heart failure and reduced ejection fraction, the effects of empagliflozin were similar in those using or not using MRAs. Empagliflozin treatment was associated with less discontinuation of MRAs.
JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Fabrizio Micheli, Andrea Bernardelli, Federica Bianchi, Simone Braggio, Laura Castelletti, Palmina Cavallini, Paolo Cavanni, Susanna Cremonesi, Michele Dal Cin, Aldo Feriani, Beatrice Oliosi, Teresa Semeraro, Luca Tarsi, Silvia Tomelleri, Andrea Wong, Filippo Visentini, Laura Zonzini, Christian Heidbreder
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Fabrizio Micheli, Susanna Cremonesi, Teresa Semeraro, Luca Tarsi, Silvia Tomelleri, Paolo Cavanni, Beatrice Oliosi, Elisabetta Perdona, Anna Sava, Laura Zonzini, Aldo Feriani, Simone Braggio, Christian Heidbreder
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Chemistry, Medicinal
Fabrizio Micheli, Alessia Bacchi, Simone Braggio, Laura Castelletti, Palmina Cavallini, Paolo Cavanni, Susanna Cremonesi, Michele Dal Cin, Aldo Feriani, Sylvie Gehanne, Mahmud Kajbaf, Luciano Marchio, Selena Nola, Beatrice Oliosi, Annalisa Pellacani, Elisabetfa Perdona, Anna Sava, Teresa Semeraro, Luca Tarsi, Silvia Tomelleri, Andrea Wong, Filippo Visentini, Laura Zonzini, Christian Heidbreder
JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Biochemistry & Molecular Biology
Fabrizio Micheli, Paolo Cavanni, Michela Bettati, Giorgio Bonanomi, Romano Di Fabio, Elettra Fazzolari, Carla Marchioro, Maja Roscic, Luca Tarsi, Filippo Visentini, Laura Zonzini, Angela Worby
BIOORGANIC & MEDICINAL CHEMISTRY
(2011)
Article
Chemistry, Medicinal
Fabrizio Micheli, Daniele Andreotti, Simone Braggio, Anna Checchia
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2010)
Article
Chemistry, Medicinal
Giorgio Bonanomi, Simone Braggio, Anna Maria Capelli, Anna Checchia, Romano Di Fabio, Carla Marchioro, Luca Tarsi, Giovanna Tedesco, Silvia Terreni, Angela Worby, Christian Heibreder, Fabrizio Micheli
Review
Chemistry, Medicinal
Fabrizio Micheli
Article
Chemistry, Medicinal
Francesca Spyrakis, Barbara Cellini, Stefano Bruno, Paolo Benedetti, Emanuele Carosati, Gabriele Cruciani, Fabrizio Micheli, Antonio Felici, Pietro Cozzini, Glen E. Kellogg, Carla Borri Voltattorni, Andrea Mozzarelli
Review
Chemistry, Medicinal
Fabrizio Micheli, Christian Heidbreder
EXPERT OPINION ON THERAPEUTIC PATENTS
(2013)
Article
Chemistry, Medicinal
Gabriele Costantino, Marco Mor, Chiara Pecchini, Gian Paolo Vallerini, Elisa Della Turca, Fabrizio Micheli, Angela Worby, Romano Di Fabio, Angelo Giacometti, Adelheid Roth, Emilio Merlo-Pich, Matteo Biagetti, Giorgio Bonanomi, Dino Montanari, Luca Tarsi, Federica Tonelli, Raffaele Longhi, Anna Maria Capelli
LETTERS IN DRUG DESIGN & DISCOVERY
(2013)
Article
Neurosciences
Manolo Mugnaini, Laura Iavarone, Palmina Cavallini, Cristiana Griffante, Beatrice Oliosi, Chiara Savoia, John Beaver, Eugenii A. Rabiner, Fabrizio Micheli, Christian Heidbreder, Anne Andorn, Emilio Merlo Pich, Massimo Bani
NEUROPSYCHOPHARMACOLOGY
(2013)
Article
Chemistry, Medicinal
Alessandro Grillo, Giulia Chemi, Simone Brogi, Margherita Brindisi, Nicola Relitti, Filomena Fezza, Domenico Fazio, Laura Castelletti, Elisabetta Perdona, Andrea Wong, Stefania Lamponi, Alessandra Pecorelli, Mascia Benedusi, Manuela Fantacci, Massimo Valoti, Giuseppe Valacchi, Fabrizio Micheli, Ettore Novellino, Giuseppe Campiani, Stefania Butini, Mauro Maccarrone, Sandra Gemma
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Chemistry, Medicinal
Fabrizio Micheli
Review
Pharmacology & Pharmacy
Anna Maria Capelli, Fabrizio Micheli
PHARMACEUTICAL PATENT ANALYST
(2012)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
