BU08073 a buprenorphine analog with partial agonist activity at μ-receptors in vitro but long-lasting opioid antagonist activity in vivo in mice

Autor: Khroyan, T. V., Wu, J., Polgar, W. E., Cami-Kobeci, G., Fotaki, N., Husbands, Stephen M., Toll, Lawrence

Publikováno v: Khroyan, T V, Wu, J, Polgar, W E, Cami-Kobeci, G, Fotaki, N, Husbands, S M & Toll, L 2014, ' BU08073 a buprenorphine analog with partial agonist activity at μ-receptors in vitro but long-lasting opioid antagonist activity in vivo in mice ', British Journal of Pharmacology, vol. 172, no. 2, pp. 668-680 . https://doi.org/10.1111/bph.12796

Background and Purpose Buprenorphine is a potent analgesic with high affinity at μ, δ and κ and moderate affinity at nociceptin opioid (NOP) receptors. Nevertheless, NOP receptor activation modulates the in vivo activity of buprenorphine. Structur

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______1378::082094b839d9af3f87cc49f180663458
https://purehost.bath.ac.uk/ws/files/60198606/Accepted_version.pdf

Activities of mixed NOP and μ-opioid receptor ligands

Autor: Spagnolo, B, Calo, G, Polgar, W E, Jiang, F, Olsen, C M, Berzetei-Gurske, I, Khroyan, T V, Husbands, S M, Lewis, J W, Toll, L, Zaveri, N T

Compounds that activate both NOP and mu-opioid receptors might be useful as analgesics and drug abuse medications. Studies were carried out to better understand the biological activity of such compounds.Binding affinities were determined on membranes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::fbe74a5db84cea5ffa78b925b6766f96
https://europepmc.org/articles/PMC2241792/

Tento výsledek nelze pro nepřihlášené uživatele zobrazit.
K zobrazení výsledku je třeba se přihlásit.

Activities of mixed NOP and μ-opioid receptor ligands.

Autor: Spagnolo, B., Calo, G., Polgar, W. E., Jiang, F., Olsen, C. M., Berzetei-Gurske, I., Khroyan, T. V., Husbands, S. M., Lewis, J. W., Toll, L., Zaveri, N. T.

Publikováno v: British Journal of Pharmacology; Feb2008, Vol. 153 Issue 3, p609-619, 11p, 1 Diagram, 3 Charts, 5 Graphs

Characterization of opiates, neuroleptics, and synthetic analogs at ORL1 and opioid receptors

Autor: Zaveri, N., Polgar, W. E., Olsen, C. M., Kelson, A. B., Grundt, P., Lewis, J. W., Toll, L.

Publikováno v: European Journal of Pharmacology; 2001, Vol. 428 Issue: 1 p29-36, 8p