Antipruritic and antihyperalgesic actions of loperamide and analogs

Citations of this article
Mendeley users who have this article in their library.
Get full text


Loperamide and three of its analogs were evaluated for their ability to inhibit binding to cloned human opioid receptor subtypes and to produce antipruritis and antinociception following local s.c. administration to rodents. All four compounds were fully efficacious agonists with affinities of 2 to 4 nM for the cloned human μ opioid receptor. Local s.c. injection of loperamide, ADL 01-0001 or ADL 01-0002 at the same site as the introduction of the pruritogenic compound 48/80 resulted in antipruritic activity in a mouse model of itch. Similarly, i.paw or administration of compounds ADL 01-0001, ADL 01-0002 and ADL 01-0003 to inflamed paws caused potent antinociception, inhibiting late phase formalin-induced flinching, Freund's adjuvant-induced mechanical hyperalgesia and tape stripping-induced mechanical hyperalgesia. Loperamide and its analogs were efficacious in animal models of itch and inflammatory pain, and may have potential therapeutic utility as antipruritic and antihyperalgesic agents. © 2002 Elsevier Science Inc. All rights reserved.




De Haven-Hudkins, D. L., Cowan, A., Cortes Burgos, L., Daubert, J. D., Cassel, J. A., DeHaven, R. N., … Kumar, V. (2002). Antipruritic and antihyperalgesic actions of loperamide and analogs. Life Sciences, 71(23), 2787–2796.

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free