2026-10-11T11:56:05Z https://api.figshare.com/v2/oai

oai:figshare.com:article/32592124 2026-09-17T19:05:14Z category_4 category_13 category_15 category_16 category_19 category_734 category_106 portal_63 item_type_3 month_year_09_2026

Development and Biological Characterization of Fluorescent Dynorphins for the Visualization of Kappa Opioid Receptors Predrag Kalaba (4169968) Monika Perisic Böhm (24141907) Filip D̵ikić (24141910) Nataša Tomašević (11019445) Ruth Drdla-Schutting (24141913) Simon Hasinger (22043092) Dylan M. Ines (14342048) Alexandra Wolf (222309) Mireia Belil-Catalina (24141916) Sharon D. Bryant (2488435) Mariana Spetea (576206) Christian W. Gruber (176571) Markus Muttenthaler (176572) Erik Keimpema (17255121) Biochemistry Genetics Neuroscience Physiology Pharmacology Biological Sciences not elsewhere classified Science Policy superficial layer neurons spinal cord neurons post hoc </ kappa opioid receptors kappa opioid receptor effectively visualize kors closely related mu highly valuable tool mapping kor expression kor agonist u50 kor (> 360 wide variety somatodendritic compartment reward responses pathophysiological contexts lead tracer induced reduction including pain highly selective fluorescent dynorphins family members excitatory drive developing dynorphin developed tracer biological processes biological characterization The kappa opioid receptor (KOR) controls a wide variety of biological processes, including pain and reward responses. However, its precise spatiotemporal location remains poorly understood due to limited selective molecular tools. We addressed this problem by developing dynorphin-based fluorescent KOR tracers that are selective for KOR over its closely related mu- and delta-family members (MOR, DOR). Our lead tracer is highly selective for KOR (>360-fold over MOR and DOR) and can effectively visualize KORs in the somatodendritic compartment of cultured primary cortical neurons, as well as in superficial layer neurons of the spinal cord dorsal horn. Furthermore, it blocked the KOR agonist U50,488-induced reduction in the excitatory drive of spinal cord neurons. The developed tracer can also be immobilized with paraformaldehyde and used for <i>post hoc</i> imaging, rendering it a highly valuable tool for mapping KOR expression in physiological and pathophysiological contexts. 2026-06-25T00:00:00Z Dataset Dataset 10.1021/acs.jmedchem.5c03072.s002 https://figshare.com/articles/dataset/Development_and_Biological_Characterization_of_Fluorescent_Dynorphins_for_the_Visualization_of_Kappa_Opioid_Receptors/32592124 CC BY-NC 4.0