Results 151 to 160 of about 2,776 (198)

Determination of thiorphan, a racecadotril metabolite, in human plasma by LC-MS/MS and its application to a bioequivalence study in Chinese subjects
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International journal of clinical pharmacology and therapeutics, 2020
OBJECTIVE The objective of this study was to use LC-MS/MS to compare the pharmacodynamic properties and bioequivalence of two 200-mg formulations of racecadotril: suspension formulation (test) and granule formulation (reference) in healthy Chinese ...
Lan Li, Chenlin Shen, Lian Tang, Yanxia Yu, Qin Zhou, Xiaohui Huang, Sudong Xue   +6 more
semanticscholar   +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

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

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

Neutral endopeptidase (NEP) inhibitors - thiorphan, sialorphin, and its derivatives exert anti-proliferative activity towards colorectal cancer cells in vitro.

Chemico-Biological Interactions, 2019
Neutral endopeptidase (NEP) is an enzyme implicated in development of different tumors, e.g. colorectal cancer (CRC). In this study, the anti-cancer effects of NEP inhibitors, thiorphan (synthetic compound) and sialorphin (naturally occurring ...
M. Mizerska-Kowalska, Joanna Kreczko-Kurzawa, B. Zdzisińska, A. Czerwonka, A. Sławińska-Brych, Z. Maćkiewicz, D. Nidzworski, M. Kandefer-Szerszeń   +7 more
semanticscholar   +1 more source

Endogenous atrial natriuretic factor after endopeptidase 24.11 inhibition by Thiorphan

Peptides, 1990
The neutral endopeptidase 24.11 (NEP) was shown to degrade atrial natriuretic factor (ANF) in kidney membranes. An infusion of Thiorphan (25 micrograms/min/kg x 90 min), a specific NEP inhibitor, induced an increase in plasma ANF (65 +/- 26 to 163 +/- 52 pg/ml), plasma renin activity and in norepinephrine concentrations at 50 minutes of infusion in ...
S, Marleau, H, Ong, M, Brochu, N, Yamaguchi, A, de Lean, P, du Souich   +5 more
openaire   +2 more sources

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
openaire   +1 more source

Quantitation of thiorphan in human plasma using LC-MS/MS and its application to a bioequivalence study.

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
Racecadotril, an anti-secretory medication, has been used as an adjuvant in an oral rehydration therapy for children experiencing severe diarrhea. Racecadotril is quickly converted to thiorphan, an active metabolite, after oral treatment, which mediates ...
Rana Said, B. Arafat, T. Arafat
semanticscholar   +1 more source

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