Results 51 to 60 of about 27,660 (289)

Analytical and Pharmacological Characterization of 1‐(Furan‐2‐Carbonyl)‐LSD (1F‐LSD) and Comparison With 1‐(Thiophene‐2‐Carbonyl)‐LSD (1T‐LSD)

Drug Testing and Analysis, EarlyView.
The novel lysergamide 1‐(furan‐2‐carbonyl)‐LSD (1F‐LSD) was analytically characterized. 1F‐LSD showed LSD‐like activity in vivo similar to 1‐(thiophene‐2‐carbonyl)‐LSD (1T‐LSD) used for comparison. Administration studies in mice and LC–MS analysis revealed that 1F‐LSD served as a prodrug.
Simon D. Brandt, Pierce V. Kavanagh, Sarah Gare, Simon P. Elliott, Alexander Stratford, Adam L. Halberstadt   +5 more
wiley   +1 more source

Histamine and Histamine H4 Receptor Promotes Osteoclastogenesis in Rheumatoid Arthritis. [PDF]

, 2017
Histamine H4 receptor (H4R) has immune-modulatory and chemotaxic effects in various immune cells. This study aimed to determine the osteoclastogenic role of H4R in rheumatoid arthritis (RA).
Firestein, Gary S, Kim, Bo-Mi, Kim, Hae-Rim, Kim, Kyoung-Woon, Lee, Kyung-Ann, Lee, Sang-Heon   +5 more
core   +1 more source

Mirtazapine Is Associated With Shorter Hospital Stay in Pediatric Avoidant Restrictive Food Intake Disorder—A Retrospective Chart Review

International Journal of Eating Disorders, EarlyView.
ABSTRACT Objective Avoidant restrictive food intake disorder (ARFID) is a relatively new diagnostic entity, and no medication has been approved. Recent data suggest that mirtazapine, a tetracyclic antidepressant, could improve outcomes in ARFID. We conducted a retrospective chart review to examine the effects of mirtazapine on ARFID treatment in youth.
Aman Chishti, Rachael E. Groh, Tamara R. Maginot, Lisa Adler, Megan E. Shott, Walter H. Kaye, Guido K. W. Frank   +6 more
wiley   +1 more source

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie, Schaller, David, Stark, Holger, Wolber, Gerhard   +3 more
core   +1 more source

Proteomic Profiling Informs Mechanisms of Esophageal Adenocarcinoma Inhibition by Cranberry Proanthocyanidins

Molecular Nutrition &Food Research, EarlyView.
In this study we utilized proteomic profiling to investigate mechanisms linked to the cancer‐inhibitory effect of cranberry proanthocyanidins (CPACs) on reflux‐induced esophageal adenocarcinoma in a rat model. The results indicate that CPAC inhibits cancer through targeting multiple hallmarks of cancer known to be dysregulated in progression to ...
Yun Zhang, Michelle Lee, Erika de Jesus, Katherine Weh, Connor Howard, Henriette Remmer, Amy B. Howell, Laura A. Kresty   +7 more
wiley   +1 more source

Intact Cell Binding for In Vitro Prediction of Sedative and Non-sedative Histamine H1–Receptor Antagonists Based on Receptor Internalization

Journal of Pharmacological Sciences, 2008
We evaluated changes in the binding properties of sedative and non-sedative histamine H1–receptor antagonists induced by internalization of H1 receptors in intact human U373 MG astrocytoma cells.
Shigeru Hishinuma, Yuko Sato, Yusuke Kobayashi, Hiroshi Komazaki, Masaki Saito   +4 more
doaj  

TRPV1 and TRPA1 Channels Are Both Involved Downstream of Histamine-Induced Itch

Biomolecules, 2021
Two histamine receptor subtypes (HR), namely H1R and H4R, are involved in the transmission of histamine-induced itch as key components. Although exact downstream signaling mechanisms are still elusive, transient receptor potential (TRP) ion channels play
Jenny Wilzopolski, Manfred Kietzmann, Santosh K. Mishra, Holger Stark, Wolfgang Bäumer, Kristine Rossbach   +5 more
doaj   +1 more source

Increased accuracy of ligand sensing by receptor diffusion on cell surface [PDF]

Physical Review E 82, 041902 (2010), 2010
The physical limit with which a cell senses external ligand concentration corresponds to the perfect absorber, where all ligand particles are absorbed and overcounting of same ligand particles does not occur. Here we analyze how the lateral diffusion of receptors on the cell membrane affects the accuracy of sensing ligand concentration.
arxiv   +1 more source

The role of hypothalamic H1 receptor antagonism in antipsychotic-induced weight gain [PDF]

, 2013
Treatment with second generation antipsychotics (SGAs), notably olanzapine and clozapine, causes severe obesity side effects. Antagonism of histamine H1 receptors has been identified as a main cause of SGA-induced obesity, but the molecular mechanisms ...
A Lecklin, A Matsui-Sakata, A Molina-Hernandez, A Pocai, A Stefanidis, AA Hancock, AJ Whittle, AK Fulop, AY Sierra, B Kola, B Parsons, BB Lowell, BV Clineschmidt, C Carpene, C Cuerda, C Deng, C Deng, C Deng, C Rummel-Kluge, Chao Deng, CJ Hong, CJ Madden, CK Song, CT Lim, CU Correll, D Gothefors, D Kohno, DD Miller, E Nowakowska, E Sejima, EA Jorgensen, EG Lundius, EM Zwaal van der, GD Cooper, GJ Schwartz, GP Reynolds, GV Ronnett, H Umehara, H Umehara, HA Nasrallah, HL Haas, HS Vestri, IV Tabarean, J Bugajski, J Ferno, J Gomez-Ramirez, J Muench, J Nedergaard, J Sethi, J Shen, J Vehof, J-P Després, JA Kang, JC Ratliff, JE Blevins, JK Sharpe, JL Cham, JL Roerig, JM Arrang, JM Arrang, JM Lenhard, JW Saleh, K Fukagawa, K Ookuma, K Ookuma, K Tsuda, K Weston-Green, KY Wang, L-H Yang, M Han, M Hasnain, M Hert De, M Hert De, M Hert De, M Hert De, M Lopez, M Lopez, M Monda, M Poyurovsky, M Poyurovsky, M Skouroliakou, MB Passani, MD Lane, ME Bhuiyan, Meng He, MJ Wolfgang, MJ Wolfgang, MK Kim, MR Hayes, N Itowi, N Pai, P Chervinsky, P Haddad, P Seale, PBM Morentin de, PJ Martins, QH Chen, R Coccurello, R Lage, RE Brown, S Gao, S Gentile, S Obici, S Skrede, S Stanley, S Threlfell, S Virtue, SF Kim, SF Morrison, SL Kirk, SM Grundy, ST Hong, T Masaki, T Masaki, T Masaki, T Masaki, T Sakata, T Scherer, T Silverstone, T Watanabe, T Yasuda, TAP Lett, U Andersson, VL Albaugh, VL Albaugh, VS Basile, WK Kroeze, WM Pardridge, WW Blessing, XF Huang, Xu-Feng Huang   +130 more
core   +2 more sources

AI‐Driven Identification of Exceptionally Efficacious Polypharmacological Compounds That Extend the Lifespan of Caenorhabditis elegans

Aging Cell, EarlyView.
A retrospective analysis of the most effective known geroprotectors shows that they act by polypharmacological mechanisms. Using graph neural networks, we predict polypharmacological geroprotectors, validate their polypharmacological mechanisms experimentally, and show them to be exceptionally effective.
Konstantin Avchaciov, Khalyd J. Clay, Kirill A. Denisov, Olga Burmistrova, Michael Petrascheck, Peter O. Fedichev   +5 more
wiley   +1 more source