Results 131 to 140 of about 1,836 (178)

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
openaire   +2 more sources

Potentiation of [D-Ala2]enkephalinamide analgesia in rats by thiorphan

European Journal of Pharmacology, 1982
The effect of thiorphan, an inhibitor of enkephalin dipeptidyl carboxypeptidase, was tested in the rat tail-flick test. When given alone up to 100 mg/kg s.c., thiorphan had no effect. However, thiorphan (30 mg/kg, s.c.) potentiated intraventricularly administered [D-Ala2,Met5]enkephalinamide (DEAEM) and its [Leu5]-derivative, whereas it had no effect ...
R E, Chipkin, M Z, Latranyi, L C, Iorio, A, Barnett   +3 more
exaly   +3 more sources

Study of thiorphan degradation

International Journal of Pharmaceutics, 1988
Abstract The degradation of the enkephalinase inhibitor thiorphan was studied. Liquid chromatography UV and electrochemical detections and several techniques of spectrometry showed that the degradation was oxidative and generates diastereoisomers of the corresponding disulfide.
F. Gimenez, E. Postaire, P. Prognon, M.D. Le Hoang, J.M. Lecomte, D. Pradeau, G. Hazebroucq   +6 more
openaire   +1 more source

Asymmetric synthesis of the enkephalinase inhibitor thiorphan

The Journal of Organic Chemistry, 1985
Synthese de la N-[mercaptomethyl-2 phenyl-3 propionyl] glycine(thiorphane) a partir d'oxazolidones-2 ...
David A. Evans, David J. Mathre, William L. Scott   +2 more
openaire   +1 more source

Inhibitory potencies of UK-69 578 and thiorphan

Lancet, The, 1990
exaly   +2 more sources

Importance of the amide bond of thiorphan in the inhibitor-enkephalinase docking process demonstrated with some thiorphan isosteres.

Bioorganic & Medicinal Chemistry Letters, 1992
Abstract Syntheses and biological activities of four thiorphan isosteres or analogs are described. The central amide linkage is replaced by ketomethylene, aminomethylene, thioamide, and trans-olefinic functionalities. Double chelation mechanism for the inhibitor-enkephalinase docking process is proposed.
Monteil Thierry, Kotera Mitsuharu, Duhamel Lucette, Duhamel Pierre, Gros Claude, Noël Nadine, Schwartz Jean Charles, Lecomte Jeanne Marie   +7 more
openaire   +1 more source

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

Thiorphan potentiation of stress-induced analgesia in the mouse

Life Sciences, 1982
Experiments were done to examine the analgesic effect of thiorphan alone or in combination with stress in mice. Analgesia was assessed by measuring jump latencies from a 55 degrees C hot plate. Thiorphan exhibited weak analgesic properties evidenced by significant increases in jump latencies only after 300 mg/kg i.p. Additional experiments were done to
R, Greenberg, E H, O'Keefe
openaire   +2 more sources

Enkephalinase ‘A’ inhibition by thiorphan: Central and peripheral cardiovascular effects

European Journal of Pharmacology, 1983
On the basis of the distribution of enkephalins within the central and peripheral nervous systems as well as on responses to their administration, it has been suggested that these peptides participate in the regulation of the circulation. The present series of experiments examined the effects of thiorphan, an inhibitor of enkephalinase A, on ...
T, Baum, F T, Becker, E J, Sybertz, C, Sabin, D M, Desiderio   +4 more
openaire   +2 more sources

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