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• W949761331 abstract "A fajdalom terapiajanak megoldasa surgető es relevans igeny. Korabban publikaltunk nehany az agyba limitaltan penetralo morfinant. Jelen munkaban kb. 30 uj szarmazekot vizsgaltunk. Periferias vs centralis analgetikus aktivitasuk 40-400, a rosszul penetralo opioid antagonistak gatoljak hatasukat, intrinsic efficacy-juk magas (periferias hatekonysag markere az altalunk kidolgozott modszer szerint ), gatlo hatasuk patkany DRG sejteken periferias tamadaspont mellett szol. Morfintolerans egerben spinalisan adva a DPDPE gatolja, mig TIPPszi potencirozza a DAMGO antinociceptiv hatasat. Patkanyon mind naiv mind tolerans allatban a hatas potencirozo. A prodynorfin genexpresszio es dinorfin szint a dependenciaert felelős agyi regiokban modosul periferias opioidok hatasara. A perinatalisan drog expozicionak kitett patkany anyak korai adoleszcens koru utodainak testsulya, adaptacios kepessege szignifikansan csokkent, erőltetett uszas teszten depressziot jeleztek, fizikalisan dependensekke, vulnerabilissa valtak. Az anyai viselkedes romlott. Konkluzio: uj morfinanok segitsegevel a C-6 szubsztitucio prominens szerepet demonstraltuk a periferias hatekonysag erősodeseben, a preemptiv analgeziaban, limitalt legzesdepresszio es pszichologiai dependencia mellett. Az eredmeny elmeleti jelentősege mellett gyakorlati fontossagu a klinikum szamara. Kimutattuk tovabba, hogy perinatalisan stimulans ill. opioid kabitoszerekkel kezelt patkanyok utodai vulnerabilissa valnak, az abuzus veszelye nő. | There is a permanent and relevant need to manage pain. Previously we published opioids with limited access to the brain. 30 new derivatives were studied in rodents and found to be more potent analgesics, than morphine (Mo). Their peripheral vs central activites were between 40-400, the analgesic action was inhibited by poorly penetrating antagonists contrast to Mo, they block DRG cells, their intrinsic efficacy (a good marker of peripheral activity), is much higher than Mo assessed by a method elaborated by us, suggesting a peripheral site of action. DPDP administered spinally to Mo tolerant mice inhibited, while TIPPsi potentiated DAMGO analgesia.. We observed potentiation both in naive and tolerant rat. Prodynorphin gene expression and dynorphin level in brain regions responsible for the development of dependence were modified by opioids. The body weight, the adaptive behaviour of early adolescent offspring of perinatally Mo and ecstasy exposed dams decreased, they show depression in swimming test, they became physically dependent, and vulnerable to addiction. The maternal behavior of dams was disturbed. Conclusion: new data on the mechanisms of preemptive analgesia were obtained by new C-6 substituted morphinans. Respiratory depression and psychological dependence were limited. This finding beside its basic importance has practical importance too.Furthermore the offspring of dams perinatally exposed to substances of drug abuse became vulnerable and prone to be addict.." @default.
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• W949761331 date "2011-01-01" @default.
• W949761331 modified "2023-09-27" @default.
• W949761331 title "Perifériás és centrális receptorok részvétele opioidok fájdalomcsillapító hatásában és mellékhatás spektrumában.Korai drog expozició (perinatális és adoleszcensz) hatásának vizsgálata patkányon = On the role of central and peripheral receptors in the antinociceptive action and side effects of opioids.The influence of early (perinatal and in adolescent age) drug exposition on antinociception" @default.
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