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1

Wpływ antagonisty glutaminianergicznego receptora metabotropowego mGluR1 na aktywność czepco-żwacza w teście doświadczalnego rozciągania ściany okrężnicy u owcy

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Kania B. F., Wielgosz M.
Medycyna Weterynaryjna
|
2013
|
tom 69
|
nr 09
The aim of this study was defining relationships between a five minute episode of mechanical colonic distensions (CD) of different degrees, which were provoked by the insertion of a balloon filled with 150 and/or200 ml of water (CD150 and/or CD200), and reticulo-ruminal motility changes, heart rate, respiration frequency as vegetative symptoms of the nociceptive effects. Futhermore, noting the influence of premedication by metabotropic glutamate receptor antagonist DL-AP3 i.c.v. 1 min. infusion in 3 different doses (4.0, 8.0 and 12.0 mg in toto) on the above symptoms in sheep. The experiment was carried out in 4 series using 12 female sheep, Polish Merinos with fistula of dorsal sac of the rumen, in the anoestrus period. In the first series (6 animals as a control group) the animals had a 200 ml 0.9% NaCl i.c.v. infusion. In the second series (6 animals) they had a 5 min episode of CD by insertion of a balloon filled with 150 and/or 200 ml of water (CD150 and/or CD200). In the third series of the experiment 6 animals had an i.c.v. DL-AP3 infusion in 3 different doses (4.0, 8.0 or 12.0 mg in toto), every week. In the fourth series, the animals had i.c.v. DL-AP3 infusions in 3 different doses (4.0, 8.0 or 12.0 mg in toto) ten minutes before CD. CD espisodes of five min duration provoke a very repetitive, statistically significant increase of heart rate/ min, reticulo-ruminal motility inhibition, and nociceptive symptoms intensivity, and this can be a new model for testing potential analgesic substances and drugs for small ruminants. DL-AP3 racemate, a metabotropic glutamate receptor mGluR₁ antagonist, can be an alternative drug in jejunal pain when it is provoked by colonic distension in sheep.
2

Receptory metabotropowe glutaminianergicze [mGluR] w procesach ostrego bolu

100%
Kania B. F., Kwapisiewicz M.
Medycyna Weterynaryjna
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2008
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tom 64
|
nr 07
866-871
The paper reviews the molecular structure, distribution and the role of metabotropic glutamate receptors (mGluRs) as excitatory aminoacid receptors. These receptors comprise a family which consists of at least eight members (mGluR₁₋₈) and coupled to various intracellular second messenger systems through G-proteins. These receptors mediate the neuromodulatory action of glutamate, and have been traditionally divided into three main groups (mGluR I, II i III) based on sequence similarity. Recent progress in the development of specific antagonists (LY 367 385, MPEP for mGluR₁) and/or agonist LY 354740, ADPC for mGluR₂⁄₃ and L-AP4 for mGluR₄) for these receptors can significantly facilitate the prophilaxy and therapy of different types of pain.
3

Wpływ 2-metylo-6-(fenyloetylo)-pirydyny - MPEP - selektywnego antagonisty receptora mGluR5 na zachowanie szczurów w teście otwartego pola w sytuacji oczekiwania na nieunikniony stres

100%
Nawrocka M., Kowalczyk M.
Medycyna Weterynaryjna
|
2012
|
tom 68
|
nr 06
The aim of the work was to assess the effects of MPEP - a selective mGluR5 receptor antagonist with anti-anxiety properties - on the behaviour of rats in a situation of predicted and inevitable stress. Wistar rats kept under a reversed light-dark cycle (the light phase starting at 8 pm) were subjected to a stress procedure including immobilisation for two hours a day during five subsequent days. Prior to the first stress, tests were performed to evaluate general motor activity and activity in the central field (a fear response). On subsequent days the tests were repeated immediately before immobilisation at 24-hour intervals. After the last immobilisation, all animals were moved to their original cages. After a 48-hour break, the animals were divided into two groups: a control group, which received 0.9% NaCl (1 mL/kg i.p.), and a test group, which received MPEP (10 mg/1mL/kg i.p.) Sixty minutes after injections, examinations preceding the expected stress were repeated in the control and test groups. A four-day stress significantly reduced the total number of passages between fields and the activity in the central field compared with the situation prior to stress. A 48-hour break after the last stress situation resulted in a significant increase in general locomotor activity and activity in the central field in the control group. In the MPEP group, general locomotor activity was significantly reduced compared with the control group, and there was also an increased proportion of passages in the central field by comparison with the control group and with the baseline prior to a stress situation. The results of this study indicate that MPEP - an mGluR5 receptor antagonist with anti-anxiety properties - may prevent psychomotor excitation caused by a situation of predicted stress and may have anti-stress properties.
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