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Information × Registration Number 0213U003654, 0110U001220 , R & D reports Title The investigation of role of cannabinoid (CB1 and CB2) vaniloid TRPV1 receptors in the action of nonsteroidal anti-inflammatory drugs and non-narcotic analgesics popup.stage_title Head Trinus Fedor Petrovich; Demchenko Anatoliy Mihaylovich, Registration Date 28-02-2013 Organization State Establishment "Institute of Pharmacology and Toxicology National Academy of Medical Science of Ukraine" popup.description2 The aim of the study was to investigate the analgesic effect of vaniloid and cannabinoid component of nonsteroidal anti-inflammatory drugs (NSAIDs) and non-narcotic analgesics (NA). The study involved the ketorolac, paracetamol, diclofenac, amizon, pirodazol. The comparative analysis of the structures of capsaicin and capsazepine, (segments A, B, C), revealed their relationship fragmented molecular structures of paracetamol, ketorolac pirodazol, amisone, diclofenac. Was study quantum chemical calculations, the ability of ketorolac pirodazol, diclofenac and paracetamol form intermolecular complexes with serine, tyrosine and dipeptide seryl-tyrosine (targets in the active site of TRPV1). It was found the greatest ability to create such complexes paracetamol. It was synthesize dipeptide seryl-tyrosine. In the model experiment was study the interaction with him of paracetamol, diclofenac, pirodazol, paracetamol and amisone, which showed the possibility of the formation of complexes with paracetamol, ketorolac and amizon. In the model experiment on the portal vein showed that paracetamol, diclofenac pirodazol against agonist and antagonist vaniloid receptor the affect the frequency and amplitude of contractions of the portal vein, it can be treated by affecting TRPV1. In the experiments in vivo, was show that capsaicin and capsazepine significantly reduced the antinociceptive activity of diclofenac and amisone at the spinal level significantly potentiate analgesic effect at the supraspinal level. There was no effect on their anti-exudative activity on the model of caragenin edema. The capsaicin significantly potentiate the antinociceptive effect of paracetamol and ketorolac reduced the effect pirodazol and in intact animals and reduced the antinociceptive activity of paracetamol and ketorolac animals with inflammation. The cannabinoid component of the test compounds showed that their characteristics (distances, angles, charges) between the optimized structure of the molecule anandamide and SR141716A close with ketorolac and low or no other NA and NSAIDs. The adminuistration of cannabinoid receptor agonists anandamide did not cause significant changes in the antinociceptive activity of the research analgesics than paracetamol. It was show the antinociceptive activity pirodazol not inferior to the hot plate model of morphine hydrochloride, and the tail-flikc model of tramadol hydrochloride. Opioid analgesics are not inherent components of action and tolerance. Pirodazolu inherent weak immunostimulatory effects. Product Description popup.authors Бершова Тетяна Анатоліївна Бобкова Людмила Станиславівна Бухтіарова Тетяна Анатоліївна Голубов Михайло Іванович Демченко Сергій Анатолійович Кокоша Олена Миколаївна Мовчан Олена Дмитрівна Мончак Ігор Леонідович Омельяненко Зінаїда Петрівна Пархоменко Петро Ілларіонович Сергеєв Валентин Сергійович Смаглій Олена Вікторівна Татьянченко Ірина Степанівна Хайрулін Андрій Рашидович Хоменко Василь Станіславович Ядловський Олег Євгенович popup.nrat_date 2020-04-02 Close