Valnoctamide: The effect on relieving of neuropathic pain and possible mechanisms

Pain condition and sex differences in the descending noradrenergic system following lateral hypothalamic stimulation

“…An unexpected finding was that female CCI rats had essentially no response to α 2 -adrenoceptor blockade, indicating that antinociception mediated by α 2 -adrenoceptors did not occur in these nerve-injured females. While α 2 -adrenoceptor-mediated antinociception was seen in female rats following crush injury (Obradovic et al, 2015), it was not found following CCI in female Wistar rats (Samur et al, 2018), a model similar to that of the present study. Some have suggested that estrogen attenuates the antinociceptive effects of α 2 -adrenoceptors in acute and inflammatory pain models (Nag and Mokha, 2016) and it is reasonable to assume such may be the case in CCI females.…”

“…Female CCI rats did not show α 2 -adrenoceptor-mediated antinociception at any carbachol dose (Fig. 3) and others have seen similar results following CCI (Samur et al, 2018). The clinical implications of this study are that deep brain LH stimulation, as well as the use of SNRIs, may be useful to relieve neuropathic pain, that sex and dose differences may occur, and in particular, females may not respond as well as males, in part because of the pronounced pronociceptive effect of α 1 –adrenoceptors and the absence of α 2 –mediated antinociception.…”

Chirality as an Important Factor for the Development of New Antiepileptic Drugs

“…The higher clearance observed for compound (2 R ,3 S )‐SPD and (2 S ,3 R )‐SPD may potentially provide lower plasma concentrations and consequently weaker anticonvulsant activity than that of the racemic‐SPD and its two other stereoisomers. However, the in vivo data do not confirm this relationship . VCD also has a stereoselective pharmacokinetic profile, that is, (2 S ,3 S )‐VCD revealed the lowest clearance and consequently higher plasma exposure than that of all other stereoisomers.…”

Cross-Talk of Toll-Like Receptor 5 and Mu-Opioid Receptor Attenuates Chronic Constriction Injury-Induced Mechanical Hyperalgesia through a Protein Kinase C Alpha-Dependent Signaling

“…Mechanical hyperalgesia is evaluated by the noxious pinprick stimulation (A von Frey-type 0.5 mm filament) with Dynamic Plantar Aesthesiometer (Code: 37450, Ugo Basile, Comerio-Varese, Italy) [56]. Minimal force (g) is automatically measure as the time elapsed from the onset of rounded tip stimulation to the withdrawal of hindpaw.…”