Results 141 to 150 of about 1,394 (176)
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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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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 ...
Michèle Brochu +2 more
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European Journal of Pharmacology, 1984
Thiorphan, an 'enkephalinase' inhibitor, and bestatin, an aminopeptidase inhibitor, decreased the turnover of noradrenaline and increased that of dopamine and serotonin in mouse brain regions. All effects were prevented by naloxone, indicating that when protected from the action of inactivating neuropeptidases endogenous enkephalins might affect ...
Catherine Llorens-Cortès +2 more
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Thiorphan, an 'enkephalinase' inhibitor, and bestatin, an aminopeptidase inhibitor, decreased the turnover of noradrenaline and increased that of dopamine and serotonin in mouse brain regions. All effects were prevented by naloxone, indicating that when protected from the action of inactivating neuropeptidases endogenous enkephalins might affect ...
Catherine Llorens-Cortès +2 more
exaly +3 more sources
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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Thiorphan and acetorphan inhibit gastric secretion by a central, non-opioid mechanism in the rat
European Journal of Pharmacology, 1988Thiorphan and its prodrug, acetorphan, are two inhibitors of enkephalinase (EC 3.4.24.11), a membrane-bound peptidase which plays an important role in the metabolic degradation of enkephalins. Since exogenous opioids have been reported to both stimulate and inhibit gastric secretion, the effects of thiorphan and acetorphan were studied in conscious ...
Claude Roze, J M Lecomte, J Chariot
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The effect of inhaled thiorphan on allergen-induced airway responses in asthmatic subjects
Clinical <html_ent glyph="@amp;" ascii="&"/> Experimental Allergy, 1996SummaryBackground 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. +4 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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Effects of thiorphan on the antinociceptive actions of intrathecal [D-Ala2,Met5]enkephalin
European Journal of Pharmacology, 1982The intrathecal administration of thiorphan (dl-3-mercapto-2-benzylpropranoyl-glycine) had no effect in doses up to 70 microgram on the rat hot plate and tail flick. Administrations of these doses of thiorphan concurrently or up to 1 h prior to the intrathecal administration of [D-Ala2, Met5] enkephalin resulted in a dose dependent, leftward shift in ...
T L, Yaksh, G J, Harty
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Potentiation of stress-induced analgesia (SIA) by thiorphan and its block by naloxone
Life Sciences, 1982Exposure 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
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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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