Results 81 to 90 of about 108,380,509 (205)

Potent, Brain-Penetrant, Hydroisoindoline-Based Human Neurokinin-1 Receptor Antagonists

, 2016
3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK1) receptor antagonist with a long ...
Terence Hamill (2375251), Marc M. Kurtz (2375242), Alana Upthagrove (2375236), Song Zheng (2375248), Kwei-Lan C. Tsao (2125189), Jinlong Jiang (1394881), Xinchun Tong (2065036), Alan Wheeldon (2375257), Geoge A. Doss (2375245), WaiSi Eng (2375239), Stephen M. Krause (2375260), Sanjeev Kumar (377400), Robert J. DeVita (523842), Christine Ryan (2259877), Gary G. Chicchi (1780462), Emma J. Carlson (2375254), Donald Burns (2375266), Jaime L. Bunda (2375263), Richard Tschirret-Guth (2125198), Richard Hargreaves (269258), Sander G. Mills (2085178), Koppara Samuel (1370235)   +21 more
core   +1 more source

Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists [PDF]

, 2019
Neurokinins (or tachykinins) are peptides that modulate a wide variety of human physiology through the neurokinin G protein-coupled receptor family, implicated in a diverse array of pathological processes.
Schöppe, Jendrik; https://orcid.org/, Plückthun, Andreas; https://orcid.org/, Schütz, Marco, Klenk, Christoph; https://orcid.org/, Doré, Andrew S, Ehrenmann, Janosch; https://orcid.org/, Rucktooa, Prakash, Ehrenmann, Janosch (author), Andreas Plückthun, Rucktooa P, Andrew S. Doré, Schöppe J, Klenk, Christoph (author), Prakash Rucktooa, Klenk C, Janosch Ehrenmann, Christoph Klenk, Schütz M, Doré, Andrew S. (author), Schütz, Marco (author), Doré AS, Marco Schütz, Ehrenmann J, Plückthun A, Plückthun, Andreas (author), Schöppe, Jendrik (author), Jendrik Schöppe, Rucktooa, Prakash (author)   +27 more
core   +1 more source

Volume Transmission of Substance P in Striatum Induced by Intraplantar Formalin Injection Attenuates Nociceptive Responses via Activation of the Neurokinin 1 Receptor

Journal of Pharmacological Sciences, 2013
.: To clarify a role of substance P (SP) in an endogenous pain control mechanism involving the rat striatum, striatal SP release was measured over time by microdialysis following intraplantar injection of 0.4% formalin.
Yoki Nakamura, Hiroki Izumi, Takumi Shimizu, Kazue Hisaoka-Nakashima, Norimitsu Morioka, Yoshihiro Nakata   +5 more
doaj   +1 more source

Effects of a neurokinin-1 receptor antagonist in the acute phase after thoracic spinal cord injury in a rat model. [PDF]

Front Mol Neurosci, 2023
Zheng G, Harms AK, Tail M, Zhang H, Nimmo A, Skutella T, Kiening K, Unterberg A, Zweckberger K, Younsi A.   +9 more
europepmc   +1 more source

Computational Analysis of the Neurokinin-1 Receptor Interactions with Antagonists [PDF]

Biophysical Journal, 2021
Marcelo Cardoso dos, Reis Melo, Cesar de, la Fuente-Nunez   +3 more
openaire   +1 more source

A New Hope for Woman with Vasomotor Symptoms: Neurokinin B Antagonists

KNDy (kisspeptine, neurokinin B, dynorphin) neurons, located in the hypothalamus, play a crucial role in the development of vasomotor symptoms (VSM) in menopausal women.
Christian Unogu, Stefania Bochynska, Anna Kostrzak, Marzena Maciejewska-Jeske, Blazej Meczekalski, Anna Szeliga, Gregory Bala   +6 more
core   +1 more source

Neurokinin-1 Receptor Resensitization Precedes Receptor Recycling

, 2020
Following agonist binding, neurokinin-1 receptors undergo rapid desensitization followed by internalization and recycling. Desensitization requires receptor phosphorylation but does not require internalization, whereas resensitization is thought to ...
V J Bennett, S A Perrine, M A Simmons
core  

Combined neurokinin-1 receptor antagonist and sorafenib is a promising approach for hepatocellular carcinoma therapy

Egyptian Liver Journal
Background HCC (Hepatocellular carcinoma) is the most common primary malignant cancer in the liver. Treatment options to incurable HCC such as sorafenib, an oral multikinase inhibitor, had numerous side effects and questionable effectiveness.
Heba E. Sedky, Yasmine N. Elwany, Eman S. El Alfy, Mona N. Elwany, Yasmin M. Nabil, Hazem F. Manna, Mohamed A. Abdelaziz, Wessam F. El Hadidy   +7 more
doaj   +1 more source

Antitumor Strategies Targeting Peptidergic Systems

Encyclopedia
Peptidergic systems show promise as targets for fighting tumors. While some peptides encourage the growth and spread of tumor cells and angiogenic mechanisms, others display antitumor properties. As such, peptide ligands and receptor antagonists could be
Francisco D. Rodríguez, Rafael Coveñas
doaj   +1 more source

NK-1 Receptor Antagonists and Pruritus: Review of Current Literature

Dermatology and Therapy, 2019
The discovery of the first neurokinin 1 (NK-1) receptor antagonist was a turning point in the prevention of chemotherapy-induced nausea and vomiting. The NK-1 antagonists are a novel class of drugs that possess antidepressant, anxiolytic, and antiemetic ...
Marcelina Pojawa-Gołąb, Kamila Jaworecka, Adam Reich   +2 more
doaj   +1 more source