1,4-dihidropiridīnu atvasinājumu (oksidētā diflurona, D3-72 un V-1-53-2) analgētiskās darbības noteikšana ar Tail Flick metodi
Date
2011
Authors
Tereņina, Olga
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Publisher
Latvijas Universitāte
Abstract
Analgētiskās vielas tiek lietotas lai remdētu sāpes. Atkarībā no sāpju intensitātes vai lokalizācijas tiek lietotas dažādas analgētiskas vielas: opiāti, NSPL, ne - opiātu analgētiķi (piem., Flupirtin, Paracetamol).Pirms farmakoloģiskās vielas izmanto cilvēkiem, tās tiek testētas uz dzīvniekiem, lai pārliecinātos par to drošību, efektivitāti, iedarbības veidu, blaknēm un citiem rādītājiem. Eksperimentāli sāpju noteikšanas testi tiek iedalīti divās kategorijās: akūto sāpju testi, kad tiek izmantoti augstās intensitātes stimuli (Tail-flick, Hot-plate), un pastāvīgo (hronisko) sāpju testi, kad dzīvniekiem ar inducētiem perifēriem bojājumiem vai iekaisumiem tiek vērotas izmaiņas uzvedībā (formalīna tests). Šajā bakalaura darbā 3 jauniem 1,4-dihidropiridīnu atvasinājumiem: oksidētajam difluronam, D3-72, V-1-53-2, kas sintezēti Latvijas Organiskās sintēzes institūtā ESF projekta “Neiroimūnās regulācijas iespējas neirodeģeneratīvo slimību ārstēšanā ar jauna tipa priviliģētām struktūrām” Nr.2009/0217/1DP/1.1.1.2.0/09/APIA/VIAA/031 ietvaros, pārbaudīta iespējamā analgētiskā darbība ar Tail-Flick metodi pelēm. Analgēziju izraisa oksidētais diflurons devā 10mg/kg pēc 120 minūtēm, bet D3-72 devā 0,1 mg/kg pēc 90 min un devā 1 mg/kg pēc 120 un 180 minūtēm. Savukārt savienojums V-1-53-2 neietekmē sāpju jūtību pelēm Tail- Flick testā. Atslēgvārdi: sāpes, analgēzija, Tail-flick tests, oksidētais diflurons, D3-72, V-1-53-2.
Analgesics are compounds used to reduce pain. Depending on pain intensity and location a variety of analgesic agents are used: opioids, NSAIDs, non - opioid analgesics (flupirtin, paracetamol).Before the pharmacological agents are used on humans, they are tested on animals to ensure their safety, efficacy, mode of action, side effects and other characteristics. Experimental pain tests are divided into two categories: acute pain tests, when used high-intensity stimuli (tail-Flick, Hot-plate), and permanent (chronic) pain tests, the animals induced by peripheral injury or inflammation is a change in behavior (formalin test). In this thesis 3 new 1,4-dihydropyridine derivatives: oxidized difluron, D3-72, V-1-53-2, which were synthesized by Latvian Institute of Organic Chemistry in ESF project "Neuroimmune management options for the treatment of neurodegenerative diseases with a new type of privileged structures" Nr. 2009/0217/1DP/1.1.1.2.0/09/APIA/VIAA/031 context, antinociceptive actions were measured using Tail-flick test. Analgesia was induced by difluron at dose 10 mg/ kg after 120 minutes, by D3-72 at dose 0.1 mg/kg at 90 min and at dose of 1 mg/kg at 120 and 180 minutes. Compound V-1-53-2 does not affect pain sensitivity of mice in the Tail-flick test. Key words: pain, analgesia, Tail-Flick test, oxidized difluron, D3-72, V-1-53-2
Analgesics are compounds used to reduce pain. Depending on pain intensity and location a variety of analgesic agents are used: opioids, NSAIDs, non - opioid analgesics (flupirtin, paracetamol).Before the pharmacological agents are used on humans, they are tested on animals to ensure their safety, efficacy, mode of action, side effects and other characteristics. Experimental pain tests are divided into two categories: acute pain tests, when used high-intensity stimuli (tail-Flick, Hot-plate), and permanent (chronic) pain tests, the animals induced by peripheral injury or inflammation is a change in behavior (formalin test). In this thesis 3 new 1,4-dihydropyridine derivatives: oxidized difluron, D3-72, V-1-53-2, which were synthesized by Latvian Institute of Organic Chemistry in ESF project "Neuroimmune management options for the treatment of neurodegenerative diseases with a new type of privileged structures" Nr. 2009/0217/1DP/1.1.1.2.0/09/APIA/VIAA/031 context, antinociceptive actions were measured using Tail-flick test. Analgesia was induced by difluron at dose 10 mg/ kg after 120 minutes, by D3-72 at dose 0.1 mg/kg at 90 min and at dose of 1 mg/kg at 120 and 180 minutes. Compound V-1-53-2 does not affect pain sensitivity of mice in the Tail-flick test. Key words: pain, analgesia, Tail-Flick test, oxidized difluron, D3-72, V-1-53-2
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