Results 131 to 140 of about 1,394 (176)
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Potentiation of the hypoglycemic effect of insulin by thiorphan, an enkephalinase inhibitor
European Journal of Pharmacology, 1984Insulin administration to rats produced a dose-related hypoglycemia. When insulin and the enkephalinase (Enk'ase) inhibitor thiorphan (30 or 100 mg/kg s.c.) were co-administered, there was a potentiation of the hypoglycemic response to insulin; these doses of thiorphan alone had no significant effect on plasma glucose.
William Kreutner +2 more
exaly +3 more sources
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 ...
Hiramatsu Masayuki +2 more
exaly +3 more sources
Thiorphan potentiation of stress-induced analgesia in the mouse
Life Sciences, 1982Experiments 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
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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 +7 more
openaire +1 more source
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 +7 more
openaire +1 more source
Effect of thiorphan on response of the guinea-pig gallbladder to tachykinins
European Journal of Pharmacology, 1989Tachykinins 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).
Paolo Rovero +2 more
exaly +4 more sources
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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Asymmetric synthesis of the enkephalinase inhibitor thiorphan
The Journal of Organic Chemistry, 1985Synthese de la N-[mercaptomethyl-2 phenyl-3 propionyl] glycine(thiorphane) a partir d'oxazolidones-2 ...
David A. Evans +2 more
openaire +1 more source
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 ...
Jean Costentin, Patrick Kitabgi, I Dubuc
exaly +3 more sources
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 ...
Jean Costentin, Patrick Kitabgi, I Dubuc
exaly +3 more sources
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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The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice
Nature, 1980There 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 +6 more
openaire +2 more sources