Non-competitive metabotropic glutamate subtype 5 receptor antagonist (SIB-1893) decreases body temperature in rats.
نویسندگان
چکیده
This study examined the effect of (E)-2-methyl-6-(2-phenylethynyl)-pyridine (SIB-1893), a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist, on body temperature in freely moving Wistar rats. Temperature was monitored using programmed microchips, implanted subcutaneously in rats, at several times: 0, 5, 10, 20, 30, 45, 60, 90, 120 and 180 min after intraperitoneal administration of SIB-1893 at increasing doses of 10, 20 and 30 mg/kg. The results analyzed with two-way ANOVA with repeated measures on time revealed that SIB-1893 at 30 mg/kg considerably lowered the body temperature in animals at 90, 120 and 180 min after its systemic injection. In contrast, the drug at 10 and 20 mg/kg remained without effect on the body temperature in rats. Based on our preclinical study, one can conclude that SIB-1893 produces hypothermia in freely moving rats in a dose-dependent manner.
منابع مشابه
Sib 1893 possesses pro- and anticonvulsant activity in the electroshock seizure threshold test in mice.
SIB 1893, a non-competitive antagonist of group I metabotropic glutamate receptor subtype 5, administered at the doses ranging between 0.5-2 mg/kg markedly lowered the electroconvulsive threshold, whereas if applied at the higher dose of 40 mg/kg, it significantly raised the threshold for electroconvulsions in mice, exhibiting both pro- and anticonvulsive properties in this test.
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SIB 1893, a non-competitive antagonist of group I metabotropic glutamate receptor subtype 5, administered at doses ranging from 0.25 to 10 mg/kg, failed to influence pentetrazole-induced convulsions in mice. Moreover, SIB 1893 (10 and 20 mg/kg) did not affect the protective action of valproate, ethosuximide, phenobarbital and clonazepam in this test. Similarly, the mGluR5 antagonist did not mod...
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SIB 1893 (a non-competitive antagonist of group I metabotropic glutamate receptors), given at 40 mg/kg (but not at 20-30 mg/kg), shortened the afterdischarge duration in amygdala-kindled rats, being ineffective on other seizure parameters - seizure severity, seizure duration, and afterdischarge threshold. Oxcarbazepine (at 7.5 mg/kg, but not at 5 mg/kg), a newer antiepileptic drug, reduced seiz...
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We have used potent and selective non-competitive antagonists of metabotropic glutamate receptor subtype 5 (mGlu5) -- 2-methyl-6-phenylethynylpyridine (MPEP), [6-methyl-2-(phenylazo)-3-pyridinol] (SIB-1757) and [(E)-2-methyl-6-(2-phenylethenyl)pyridine] (SIB-1893) - to examine whether endogenous activation of this particular metabotropic glutamate receptor subtype contributes to neuronal degene...
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Cell lines expressing the human metabotropic glutamate receptor subtype 5a (hmGluR5a) and hmGluR1b were used as targets in an automated high-throughput screening (HTS) system that measures changes in intracellular Ca2+ ([Ca2+]i) using fluorescence detection. This functional screen was used to identify the mGluR5-selective antagonist, SIB-1757 [6-methyl-2-(phenylazo)-3-pyridinol], which inhibite...
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عنوان ژورنال:
- Pharmacological reports : PR
دوره 57 6 شماره
صفحات -
تاریخ انتشار 2005