Khomula, Eugen V. published the artcilein vitro nociceptor neuroplasticity associated with in vivo opioid-induced hyperalgesia, HPLC of Formula: 330161-87-0, the publication is Journal of Neuroscience (2019), 39(36), 7061-7073, database is CAplus and MEDLINE.
Opioid-induced hyperalgesia (OIH) is a serious adverse event produced by opioid analgesics. Lack of an in-vitro model has hindered study of its underlying mechanisms. Recent evidence has implicated a role of nociceptors in OIH. To investigate the cellular and mol. mechanisms of OIH in nociceptors, in vitro, s.c. administration of an analgesic dose of fentanyl (30μg/kg, s.c.) was performed in vivo in male rats. Two days later, when fentanyl was administered intradermally (1μg, i.d.), in the vicinity of peripheral nociceptor terminals, it produced mech. hyperalgesia (OIH). Addnl., 2 d after systemic fentanyl, rats had also developed hyperalgesic priming (opioid-primed rats), long-lasting nociceptor neuroplasticity manifested as prolongation of prostaglandin E2 (PGE2) hyperalgesia. OIH was reversed, in vivo, by intrathecal administration of cordycepin, a protein translation inhibitor that reverses priming. When fentanyl (0.5 nm) was applied to dorsal root ganglion (DRG) neurons, cultured from opioid-primed rats, it induced a μ-opioid receptor (MOR)-dependent increase in [Ca2+]i in 26% of small-diameter neurons and significantly sensitized (decreased action potential rheobase) weakly IB4+ and IB4– neurons. This sensitizing effect of fentanyl was reversed in weakly IB4+ DRG neurons cultured from opioid-primed rats after in vivo treatment with cordycepin, to reverse of OIH. Thus, in vivo administration of fentanyl induces nociceptor neuroplasticity, which persists in culture, providing evidence for the role of nociceptor MOR-mediated calcium signaling and peripheral protein translation, in the weakly IB4-binding population of nociceptors, in OIH.
Journal of Neuroscience published new progress about 330161-87-0. 330161-87-0 belongs to indole-building-block, auxiliary class Protein Tyrosine Kinase/RTK,Src, name is SU6656, and the molecular formula is C19H21N3O3S, HPLC of Formula: 330161-87-0.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles