Pharmacological activation of mediodorsal thalamic GABA-A receptors modulates morphine/cetirizine-induced changes in the prefrontal cortical GFAP expression in a …

N Asgharpour-Masouleh, A Rezayof… - Behavioural Brain …, 2023 - Elsevier
The present study investigated the involvement of mediodorsal thalamic (MD) GABA-A
receptors in cetirizine/morphine-induced anti-allodynia using a rat model of neuropathic …

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

DM Riddy, AE Cook, DM Shackleford, TL Pierce… - …, 2019 - Elsevier
The histamine H 3 receptor is a G protein-coupled receptor (GPCR) drug target that is highly
expressed in the CNS, where it acts as both an auto-and hetero-receptor to regulate …

Cold‐evoked potentials in clinical practice: A head‐to‐head contrast with laser‐evoked responses

C Perchet, K Hagiwara, C Salameh… - … Journal of Pain, 2023 - Wiley Online Library
Background Innocuous cooling of the skin activates cold‐specific Aδ fibres, and hence, the
recording of cold‐evoked potentials (CEPs) may improve the objective assessment of …

TREK1 channel activation as a new analgesic strategy devoid of opioid adverse effects

J Busserolles, I Ben Soussia, L Pouchol… - British Journal of …, 2020 - Wiley Online Library
Background and Purpose Opioids are effective painkillers. However, their risk–benefit ratio
is dampened by numerous adverse effects and opioid misuse has led to a public health …

Microinjection of histamine and its H3 receptor agonist and antagonist into the agranular insular cortex influence sensory and affective components of neuropathic …

S Salimi, E Tamaddonfard - European journal of pharmacology, 2019 - Elsevier
Many areas of the brain along with neurotransmitters involve in processing of nociceptive,
emotional and cognitive dimensions of neuropathic pain. Brian neuronal histamine through …

[HTML][HTML] Sleep, narcolepsy, and sodium oxybate

M Mamelak - Current Neuropharmacology, 2022 - ncbi.nlm.nih.gov
Sodium oxybate (SO) has been in use for many decades to treat narcolepsy with cataplexy.
It functions as a weak GABAB agonist but also as an energy source for the brain as a result …

Efficacy of the multi-target compound E153 in relieving pain and pruritus of different origins

S Mogilski, M Kubacka, A Świerczek, E Wyska… - Pharmaceuticals, 2023 - mdpi.com
Itch and pain are closely related but distinct sensations that share largely overlapping
mediators and receptors. We hypothesized that the novel, multi-target compound E153 has …

Dual-targeting approach on histamine H3 and sigma-1 receptor ligands as promising pharmacological tools in the treatment of CNS-linked disorders

K Szczepańska, KJ Kuder… - Current Medicinal …, 2021 - ingentaconnect.com
With the recent market approval of Pitolisant (Wakix®), the interest in clinical application for
novel multifunctional histamine H3 receptor antagonists has clearly increased. Several …

Synthesis and evaluation of histamine H3 receptor ligand based on lactam scaffold as agents for treating neuropathic pain

F Dou, X Cao, P Jing, C Wu, Y Zhang, Y Chen… - Bioorganic & Medicinal …, 2019 - Elsevier
The synthesis and H 3 receptor ligand of a new series of lactam derivatives are reported.
The new compounds were evaluated in vitro in H 3 and H 1 receptor-binding assays. The …

Targeting neuropathic pain: pathobiology, current treatment and peptidomimetics as a new therapeutic opportunity

MC Caroleo, A Brizzi, M De Rosa… - Current Medicinal …, 2020 - ingentaconnect.com
There is a huge need for pharmaceutical agents for the treatment of chronic Neuropathic
Pain (NP), a complex condition where patients can suffer from either hyperalgesia or …