Results 101 to 110 of about 1,034 (134)

Polarization Controlled Assembly of Ultrathin Thiorphan Nanostructures on ZnO Surface Facets

Langmuir, 2023
Despite the importance of thiorphan as a small molecule with vital biological roles, its interactions with zinc oxide (ZnO) nanomaterials that are prospective in drug delivery and theranostic applications have not yet been sufficiently explored.
Egor Ukraintsev, Hadi Hematian, Bohuslav Rezek   +2 more
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Synthesis of tritium labelled thiorphan, an enkephalinase inhibitor

Journal of Labelled Compounds and Radiopharmaceuticals, 2008
AbstractTritium labelling of the enkephalinase inhibitor, thiorphan, is complicated by the presence of mercapto functional group. Reactions often used in aromatic tritiation, such as halogination and catalytic halogen/tritium displacement, are adversely affected by the presence of the divalent sulfur moeity.
Shao‐Yong Wu, Mohammad R. Masjedizadeh
openaire   +1 more source

The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice

Nature, 1980
There is both theoretical and therapeutic interest in establishing whether the signals conveyed by the enkephalins are turned off under the action of a specific peptidase which might, in this case, represent a target for a new class of psychoactive agents.
B P, Roques, M C, Fournié-Zaluski, E, Soroca, J M, Lecomte, B, Malfroy, C, Llorens, J C, Schwartz   +6 more
openaire   +2 more sources

Effect of thiorphan on response of the guinea-pig gallbladder to tachykinins

European Journal of Pharmacology, 1989
Tachykinins produced a concentration-related contraction of the isolated guinea-pig gallbladder, with a rank order of potency neurokinin A (NKA) greater than Arg-neurokinin B = neurokinin B (NKB) greater than substance P (SP). Only the effect of SP was potentiated by thiorphan (0.1-10 microM).
C. A. Maggi, R. Patacchini, RENZI, DANIELA, P. Santicioli, D. Regoli, ROVERO, PAOLO, G. Drapeau, C. Surrenti, A. Meli   +8 more
openaire   +3 more sources

The effect of inhaled thiorphan on allergen-induced airway responses in asthmatic subjects

Clinical <html_ent glyph="@amp;" ascii="&amp;"/> Experimental Allergy, 1996
SummaryBackground Neuropeptides are likely to be implicated in the pathophysiology of allergen‐induced airway responses. However, upon release in the airways, neuropeptides are potentially inactivated by neutral endopeptidase (NEP). Objective We hypothesized that NEP‐inhibition by inhaled thiorphan (TH) would increase allergen‐induced early (EAR)
Diamant, Z., van der Veen, H., Kuijpers, E. A., Bakker, P. F., Sterk, P. J.   +4 more
openaire   +3 more sources

Enantiomers of [R,S]-thiorphan: Dissociation of analgesia from enkephalinase a inhibition

Life Sciences, 1985
The [R] and [S] enantiomers of the enkephalinase A inhibitor [R,S]-thiorphan have been prepared by asymmetric synthesis. The [S] isomer is principally responsible for the angiotensin converting enzyme inhibitory activity of [R,S]-thiorphan, whereas there were only small differences in the ability of the [R] and [S] isomers to inhibit enkephalinase both
W L, Scott, L G, Mendelsohn, M L, Cohen, D A, Evans, R C, Frederickson   +4 more
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ChemInform Abstract: ASYMMETRIC SYNTHESIS OF THE ENKEPHALINASE INHIBITOR THIORPHAN

Chemischer Informationsdienst, 1985
AbstractAusgehend von den Aminoalkoholen (I) und (IV) werden zunächst die chiralen Oxazolidinone (II) und (V) dargestellt und diese enantioselektiv in die Carboximide (III) bzw. (VI) übergeführt.
D. A. EVANS, D. J. MATHRE, W. L. SCOTT
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Synthesis of constrained thiorphan analogs as inhibitors of neutral endopeptidase

Bioorganic & Medicinal Chemistry Letters, 1996
Abstract Constrained derivatives of thiorphan were prepared and found to be potent inhibitors of neutral endopeptidase 24.11.
Douglas W. Beight, Shujaath Mehdi, Jack R. Koehl, Gary A. Flynn   +3 more
openaire   +1 more source

Potentiation of stress-induced analgesia (SIA) by thiorphan and its block by naloxone

Life Sciences, 1982
Exposure of rats to inescapable footshock produces an analgesic effect. To determine if endogenously released enkephalins play a role in this phenomenom, rats were treated with the enkephalinase inhibitor thiorphan (T), exposed to inescapable stress, and tested in the tail-flick test for antinociception.
R E, Chipkin, M B, Latranyi, L C, Iorio
openaire   +2 more sources

Antitumor activity of bestatin and thiorphan in mice.

Archivum immunologiae et therapiae experimentalis, 1996
We have investigated the effect of bestatin and thiorphan on growth of murine transplantable tumors, survival time, activity of natural killer (NK) cells and macrophages in mice. The injections of thiorphan at the does of 0.5 or 5 micrograms per mouse retarded tumor growth and prolonged survival period in B16 melanoma bearing animals. Pretreatment with
J, Kowalski, D, Belowski, A, Madej, Z S, Herman   +3 more
openaire   +1 more source