Results 171 to 180 of about 2,737 (218)
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Synthesis of tritium labelled thiorphan, an enkephalinase inhibitor
Journal of Labelled Compounds and Radiopharmaceuticals, 2008AbstractTritium 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
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Enkephalinase ‘A’ inhibition by thiorphan: Central and peripheral cardiovascular effects
European Journal of Pharmacology, 1983On 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 +4 more
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Potentiation of [D-Ala2]enkephalinamide analgesia in rats by thiorphan
European Journal of Pharmacology, 1982The 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 +3 more
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, 2016 Endogenous atrial natriuretic factor after endopeptidase 24.11 inhibition by Thiorphan
Peptides, 1990The 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 +5 more
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ChemInform Abstract: ASYMMETRIC SYNTHESIS OF THE ENKEPHALINASE INHIBITOR THIORPHAN
Chemischer Informationsdienst, 1985AbstractAusgehend 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, 1996Abstract Constrained derivatives of thiorphan were prepared and found to be potent inhibitors of neutral endopeptidase 24.11.
Douglas W. Beight +3 more
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Enantiomers of [R,S]-thiorphan: Dissociation of analgesia from enkephalinase a inhibition
Life Sciences, 1985The [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 +4 more
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Potentiation of phencyclidine-induced stereotyped behaviors in rats by thiorphan and bestatin
European Journal of Pharmacology, 1986We investigated the effects of thiorphan, a specific inhibitor of enkephalinase A and bestatin, a specific inhibitor of aminopeptidase, on the stereotyped behaviors induced by phencyclidine (PCP) in cannulated rats. The PCP-induced turning was significantly potentiated when thiorphan (50 micrograms) and bestatin (50 micrograms) were injected ...
M, Hiramatsu +4 more
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