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Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine


Reference:

Cami-Kobeci, G., Polgar, W. E., Khroyan, T. V., Toll, L. and Husbands, S. M., 2011. Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. Journal of Medicinal Chemistry, 54 (19), pp. 6531-6537.

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    Official URL:

    http://dx.doi.org/10.1021/jm2003238

    Abstract

    The unique pharmacological profile of buprenorphine has led to its considerable success as an analgesic and as a treatment agent for drug abuse. Activation of nociceptin/orphanin FQ peptide (NOP) receptors has been postulated to account for certain aspects of buprenorphine's behavioral profile. In order to investigate the role of NOP activation further, a series of buprenorphine analogues has been synthesized with the aim of increasing affinity for the NOP receptor. Binding and functional assay data on these new compounds indicate that the area around C20 in the orvinols is key to NOP receptor activity, with several compounds displaying higher affinity than buprenorphine. One compound, 1b, was found to be a mu opioid receptor partial agonist of comparable efficacy to buprenorphine but with higher efficacy at NOP receptors.

    Details

    Item Type Articles
    CreatorsCami-Kobeci, G., Polgar, W. E., Khroyan, T. V., Toll, L. and Husbands, S. M.
    DOI10.1021/jm2003238
    DepartmentsFaculty of Science > Pharmacy & Pharmacology
    Publisher StatementHusbands_JMC_2011_54_19_6531.pdf: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jm2003238; Husbands_JMC_2011_54_19_6531.doc: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jm2003238
    RefereedYes
    StatusPublished
    ID Code27270

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