pyrazole derivatives

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Sep 21, 2014 - In this study, effects of subacute administration of mianserin on diabetic hyperalgesia and allodynia, which developed 4 weeks.
Fourth International Meeting on Pharmacy & Pharmaceutical Sciences 18-21 September 2014, Istanbul

PP 231 CENTRALLY AND PERIPHERALLY MEDIATED ANTINOCICEPTIVE ACTIVITIES OF SOME 1,3,5-TRIARYL-4,5-DIHYDRO-1HPYRAZOLE DERIVATIVES HARIKA AYDIN , UMUT IRFAN UÇEL , UMIDE DEMIR OZKAY , OZGUR DEVRIM CAN ANADOLU UNIVERSITY, FACULTY OF PHARMACY, DEPARTMENT OF PHARMACOLOGY, ESKISEHIR, TURKEY Some new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives were synthesized via the treatment of 1,3-diaryl-2-propen-1ones with phenylhydrazine hydrochloride derivatives in hot acetic acid. The antinociceptive properties of the compounds were evaluated by hot-plate, tail-clip and acetic acid induced writhing tests in mice. Motor coordination of the animals was evaluated in a Rota-rod model. Morphine sulphate used as a reference drug in all nociceptive tests. Statistical evaluation of the obtained data indicated that compounds 2c, 2e, 2g, 2h, 2j, 2l, and 2m, when administrated at 100 mg/kg, increased the reaction time of animals both in hot plate and tail clip tests. Additionally, the same compounds reduced the number of acetic acid induced writhing behaviors. Obtained data exhibited antinociceptive effect of these compounds on supraspinal, spinal and peripheral nociceptive pathways. Besides, in the Rota-rod tests, 2c, 2e, 2g, 2h, 2j, 2l, and 2m did not cause any change in the motor coordination of mice, indicating that the observed antinociceptive effect is specific. These results supported the previous papers reporting the antinociceptive potential of various pyrazoline derivative compounds.

PP 232 ANTIDEPRESSANT-LIKE ACTIVITY OF SOME AROYL PROPIONIC ACID-HYDRAZONE DERIVATIVES FEYZA ALYU 1, HARIKA AYDIN 1, OZGUR DEVRIM CAN 1, YUSUF OZTURK 1, GULHAN TURAN-ZITOUNI 2 1 2

ANADOLU UNIVERSITY, FACULTY OF PHARMACY, DEPARTMENT OF PHARMACOLOGY, ESKISEHIR, TURKEY ANADOLU UNIVERSITY, FACULTY OF PHARMACY, DEPARTMENT OF PHARMACEUTICAL CHEMISTRY, ESKISEHIR, TURKEY

The aim of the present study was examining the effect of some 4-[4-[2-(2-(4-substituted benzylidene)hydrazinyl)-2-oxoethoxy] phenyl]-4-oxobutanoic acid derivatives on depression, anxiety and spontaneous locomotor activity parameters of mice. In tail suspension tests, when administrated at 50 mg/kg dose, compounds 2a, 2b, 2d, 2e, 2f, 2g and 2i in the series, caused significant reduction in the immobility time of mice. Additionally, in modified forced swimming tests, the same compounds decreased the immobility and increased the swimming times of mice without any change in climbing durations. Data obtain from these two tests clearly pointed out the antidepressant-like effects of the aforementioned compounds. Exact mechanism of the antidepressant action exhibited in the present study need to be clarified with further detailed investigations. On the other hand, none of the compounds changed the exploratory parameters in hole-board tests or total numbers of spontaneous locomotor activities in activity cage measurements at the applied dose. In other words, neither anxiolytic nor sedative effects induced by the test compounds.

PP 233 ANTIHYPERALGESIC AND ANTIALLODYNIC EFFECT OF MIANSERIN ON DIABETIC NEUROPATHIC PAIN IN RATS UMUT IRFAN UCEL , OZGUR DEVRIM CAN , UMIDE DEMIR OZKAY ANADOLU UNIVERSITY, FACULTY OF PHARMACY, DEPARTMENT OF PHARMACOLOGY, ESKISEHIR, TURKEY In this study, effects of subacute administration of mianserin on diabetic hyperalgesia and allodynia, which developed 4 weeks after streptozotocin injection, were investigated using several experimental pain-induction methods in rats with diabetes. Mianserin administered at 30 and 45 mg/kg doses during 7 and 14 days not only showed opioid-mediated acute anti-nociceptive activity but also effectively improved mechanical and thermal hyperalgesia caused by diabetic neuropathy. In addition to having an anti-hyperalgesic effect, mianserin attenuated diabetes-related mechanical and thermal allodynia. To the best of our knowledge, this is the first study to show that the anti-hyperalgesic and anti-allodynic effects of mianserin, an atypical anti-depressant, in the experimental diabetes model were comparable to those of the reference drug pregabalin (dose, 10 mg/kg). However, the pharmacological mechanisms underlying these anti-hyperalgesic, and anti-allodynic effects of mianserin remain to be elucidated. The results of this study will provide a pre-clinical basis for new approaches of proper drug selection for the treatment of neuropathic pain, which has a high incidence among diabetes patients. Nevertheless, for mianserin to be considered an effective alternative drug for the treatment of diabetic neuropathy, it is necessary to confirm the results of this pre-clinical study in clinical studies.

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