A series of novel spiroether-based neurokinin-1 (NK(1)) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.
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http://dx.doi.org/10.1016/s0960-894x(02)00509-7 | DOI Listing |
Neuropeptides
October 2024
Department of Anesthesiology, Wake Forest School of Medicine, Winston-Salem, NC, USA.
Several data indicate that Substance P (SP) neurokinin type 1 receptor (NK1R) is at the center of the interaction between cancer cells and peripheral sensory neurons. Selecting the appropriate cancer cell line and its susceptibility to being modulated by NK1 antagonists are critical to studying this complex interaction. In the current study, we have focused on this selection by comparing several aspects of the triple-negative breast cancer (TNBC) cell line (MDA-MB-231) with a modified murine cell line (E0771), both expressing luciferase.
View Article and Find Full Text PDFInt J Clin Oncol
November 2024
Department of Early Clinical Development, Kyoto University Graduate School of Medicine, 54 Kawahara‑Cho, Sakyo-ku, Shogoin, Kyoto, 606‑8507, Japan.
Support Care Cancer
October 2024
Centre for Reviews and Dissemination, University of York, Heslington, York, YO10 5DD, UK.
J Geriatr Oncol
October 2024
Clinic of Oncology, HFR Fribourg Hospital, Fribourg, Switzerland. Electronic address:
Corticosteroids are used frequently in oncology and many patients require short- or long-term corticosteroid therapy. General clinical guidelines and recommendations exist on the use of corticosteroids; however, evidence is lacking for recommendations on their appropriate use in older adult with cancer. Treatment of chemotherapy-induced nausea and vomiting (CINV) has dramatically improved over the last decade with 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists and neurokinin-1 (NK-1) receptor antagonists or a combination of both.
View Article and Find Full Text PDFSurg Endosc
December 2024
Department of Anesthesiology and Perioperative Medicine, Mayo Clinic, 200 1St Street SW, Rochester, MN, 55905, USA.
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