Results 141 to 150 of about 1,836 (178)

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

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).
Daniela Renzi, Paolo Santicioli, Paolo Rovero   +2 more
exaly   +4 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

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

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
openaire   +2 more sources

Naloxone-insensitive potentiation of neurotensin hypothermic effect by the enkephalinase inhibitor thiorphan

Brain Research, 1986
The hypothermic effect of neurotensin (0.1 microgram) injected i.c.v. in mice is potentiated by the enkephalinase inhibitor thiorphan (10 micrograms, i.c.v.). This potentiation is not reversed by systemic naloxone. The hypothermic effect of neurotensin is not modified by the amino-peptidase inhibitor bestatin (50 micrograms, i.c.v.) nor by the ...
A, Coquerel, I, Dubuc, J F, Menard, P, Kitabgi, J, Costentin   +4 more
exaly   +3 more sources

Effects of thiorphan on the antinociceptive actions of intrathecal [D-Ala2,Met5]enkephalin

European Journal of Pharmacology, 1982
The 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
exaly   +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

Effect of bestatin and thiorphan on [Met5]enkephalin-Arg6-Phe7-induced analgesia

European Journal of Pharmacology, 1984
We investigated the effect of bestatin, a specific inhibitor of aminopeptidase and thiorphan, a specific inhibitor of enkephalinase A, on the analgesic effect induced by the intracerebral injection of heptapeptide [Met5]enkephalin-Arg6-Phe7 (MEAP) in cannulated rats.
A, Reggiani, A, Carenzi, V, Frigeni, D, Della Bella   +3 more
openaire   +2 more sources

Potentiation of phencyclidine-induced stereotyped behaviors in rats by thiorphan and bestatin

European Journal of Pharmacology, 1986
We 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, T, Nabeshima, H, Fukaya, H, Furukawa, T, Kameyama   +4 more
exaly   +3 more sources