Szczepan Mogilski, Monika Kubacka, Artur Świerczek, Elżbieta Wyska, Katarzyna Szczepańska, Jacek Sapa, Katarzyna Kieć-Kononowicz, Dorota Łażewska
Itch and pain are closely related but distinct sensations that share largely overlapping mediators and receptors. We hypothesized that the novel, multi-target compound E153 has the potential to attenuate pain and pruritus of different origins. After the evaluation of sigma receptor affinity and pharmacokinetic studies, we tested the compound using different procedures and models of pain and pruritus. Additionally, we used pharmacological tools, such as PRE-084, RAMH, JNJ 5207852, and S1RA, to precisely determine the role of histamine H3 and sigma 1 receptors in the analgesic and antipruritic effects of the compound...
October 17, 2023: Pharmaceuticals