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A. W. Lipkowski
Researcher at University of Warsaw
Publications - 10
Citations - 740
A. W. Lipkowski is an academic researcher from University of Warsaw. The author has contributed to research in topics: Opioid receptor & Opioid antagonist. The author has an hindex of 7, co-authored 10 publications receiving 728 citations. Previous affiliations of A. W. Lipkowski include Polish Academy of Sciences.
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Journal ArticleDOI
Binaltorphimine and nor-binaltorphimine, potent and selective k-opioid receptor antagonists
TL;DR: BNI and nor-BNI represent the first highly selective kappa opioids receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with kappa opioid receptors in vitro and in vivo.
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Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
TL;DR: The pharmacologic data suggest that only one antagonist pharmacophore may be required for kappa selectivity and that the other morphinan portion of the molecule confers selectivity by interacting with a unique subsite proximal to the antagonist pharmacphore recognition locus.
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Superpotent [Dmt1]Dermorphin Tetrapeptides Containing the 4-Aminotetrahydro-2-benzazepin-3-one Scaffold with Mixed μ/δ Opioid Receptor Agonistic Properties
Bart Vandormael,Danai-Dionysia Fourla,Alexandra Gramowski-Voss,Piotr Kosson,Dieter G. Weiss,Olaf Schröder,A. W. Lipkowski,Zafiroula Georgoussi,Dirk Tourwé +8 more
TL;DR: Functional electrophysiological in vitro assays using primary cortical and spinal cord networks showed that the most potent ligand H-Dmt-NMe-d-Ala-Aba-Gly-NH(2) (BVD03) displayed mixed μ/δ opioid agonist properties with picomolar functional potencies.
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Binaltorphimine-related bivalent ligands and their .kappa. opioid receptor antagonist selectivity [Erratum to document cited in CA108(17):150771q]
Journal ArticleDOI
Investigation of the structural requirements for the kappa-selective opioid receptor antagonist, 6 beta,6 beta'-[ethylenebis(oxyethyleneimino)]bis[17-(cyclopropylmethyl)- 4,5 alpha-epoxymorphinan-3,14-diol] (TENA).
TL;DR: The results obtained with 2 are consistent with the requirement of a second opiate pharmacophore (rather than a second basic nitrogen in the spacer) for the kappa antagonist activity of TENA, but the potent agonism associated with these monomers do not allow a firm conclusion in this regard.