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Buprenorphine Pharmacodynamics: A Bridge to Understanding Buprenorphine Clinical Benefits.
Drugs
January 2025
Palliative Medicine, Geisinger Medical Center, Danville, PA, USA.
Buprenorphine is an agonist at the mu opioid receptor (MOR) and antagonist at the kappa (KOR) and delta (DOR) receptors and a nociceptin receptor (NOR) ligand. Buprenorphine has a relatively low intrinsic efficacy for G-proteins and a long brain and MOR dwell time. Buprenorphine ceiling on respiratory depression has theoretically been related multiple factors such as low intrinsic efficacy at MOR, binding to six-transmembrane MOR and interactions in MOR/NOR heterodimers.
View Article and Find Full Text PDFMechanisms of Cancer-Induced Bone Pain.
J Pain Res
January 2025
Department of Anesthesiology, Beijing Friendship Hospital, Capital Medical University, Beijing, People's Republic of China.
Bone is a common site of advanced cancer metastasis, second only to the lungs and liver. Cancer-induced bone pain (CIBP) is a persistent and intense pain that is caused by a combination of inflammatory and neuropathic factors. As CIBP progresses, the degree of pain intensifies.
View Article and Find Full Text PDFAdvanced Pain Management in Patients with Terminal Cancer.
Curr Med Chem
January 2025
Department of Surgery, School of Medicine, Nazarbayev University, 5/1 Kerey and Zhanibek khandar str., 020000, Astana, Kazakhstan.
Understanding and managing pain in patients with terminal cancer is a vital aspect of palliative care, aimed at relieving suffering and improving quality of life in the final stages of illness. Studies indicate that approximately 50% of patients with stage 4 cancer report moderate to severe pain, with a quarter experiencing severe cancer-related pain. Despite opioid prescriptions in 97% of cases, a significant portion of patients continues to suffer unresolved pain during the last week of life.
View Article and Find Full Text PDFNovel tertiary diarylethylamines as functionally selective agonists of the kappa opioid receptor.
Bioorg Med Chem Lett
January 2025
Contineum Therapeutics, 3565 General Atomics Court, Suite 200, San Diego, CA 92121, United States.
Novel kappa opioid receptor (KOR) agonists that preferentially activate G-protein signaling versus β-arrestin-2 recruitment are described. Starting from a literature-reported phenol-containing diphenethylamine KOR agonist, structure-activity relationship (SAR) studies revealed replacement of the phenol with various non-hydroxylated bicyclic heteroaromatics led to tertiary diarylethylamines which retained KOR agonist activity and improved metabolic stability in human liver microsomes. Further optimizations produced compound 39, a potent activator of G-protein signaling (GTPγS EC = 14 nM, 83 % E) that did not elicit a β-arrestin-2 recruitment functional response (E < 10 %).
View Article and Find Full Text PDFOpioid Consumption Following Isolated and Recurrent Shoulder Dislocation and Reduction.
J Shoulder Elbow Surg
January 2025
Department of Orthopaedics; University Hospital Cleveland Medical Center, Cleveland, OH, USA.
Background: Recurrent shoulder dislocations often lead to multiple encounters for reduction and eventual surgical stabilization, both of which involve exposure to opioids and potentially increase the risk of chronic opioid exposure. The purpose of our study was to characterize shoulder instability and compare pre- and post-reduction opioid usage in singular dislocators (SD) and recurrent dislocators (RD).
Methods: This retrospective study was performed at a single academic institution using a prospective database.
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