Электронный архив

Distinct activity of endocannabinoid-hydrolyzing enzymes MAGL and FAAH in key regions of peripheral and central nervous system implicated in migraine

Показать сокращенную информацию

dc.contributor.author Della Pietra A.
dc.contributor.author Giniatullin R.
dc.contributor.author Savinainen J.R.
dc.date.accessioned 2022-02-09T20:38:34Z
dc.date.available 2022-02-09T20:38:34Z
dc.date.issued 2021
dc.identifier.issn 1661-6596
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/169518
dc.description.abstract In migraine pain, cannabis has a promising analgesic action, which, however, is associated with side psychotropic effects. To overcome these adverse effects of exogenous cannabinoids, we propose migraine pain relief via activation of the endogenous cannabinoid system (ECS) by inhibiting enzymes degrading endocannabinoids. To provide a functional platform for such purpose in the peripheral and central parts of the rat nociceptive system relevant to migraine, we measured by activity-based protein profiling (ABPP) the activity of the main endocannabinoid-hydrolases, monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH). We found that in trigeminal ganglia, the MAGL activity was nine-fold higher than that of FAAH. MAGL activity exceeded FAAH activity also in DRG, spinal cord and brainstem. However, activities of MAGL and FAAH were comparably high in the cerebellum and cerebral cortex implicated in migraine aura. MAGL and FAAH activities were identified and blocked by the selective and potent inhibitors JJKK- 048/KML29 and JZP327A, respectively. The high MAGL activity in trigeminal ganglia implicated in the generation of nociceptive signals suggests this part of ECS as a priority target for blocking peripheral mechanisms of migraine pain. In the CNS, both MAGL and FAAH represent potential targets for attenuation of migraine-related enhanced cortical excitability and pain transmission.
dc.relation.ispartofseries International Journal of Molecular Sciences
dc.subject Analgesia
dc.subject Endocannabinoid
dc.subject Migraine
dc.subject Pain
dc.subject Serine hydrolases
dc.title Distinct activity of endocannabinoid-hydrolyzing enzymes MAGL and FAAH in key regions of peripheral and central nervous system implicated in migraine
dc.type Article
dc.relation.ispartofseries-issue 3
dc.relation.ispartofseries-volume 22
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 1
dc.source.id SCOPUS16616596-2021-22-3-SID85099963455


Файлы в этом документе

Данный элемент включен в следующие коллекции

  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

Показать сокращенную информацию

Поиск в электронном архиве


Расширенный поиск

Просмотр

Моя учетная запись

Статистика