Sigma receptors [σ Rs]: biology in normal and diseased states

CG Rousseaux, SF Greene - Journal of Receptors and Signal …, 2016 - Taylor & Francis
This review compares the biological and physiological function of Sigma receptors [σRs] and
their potential therapeutic roles. Sigma receptors are widespread in the central nervous …

Novel approaches, drug candidates, and targets in pain drug discovery

S Obeng, T Hiranita, F León, LR McMahon… - Journal of medicinal …, 2021 - ACS Publications
Because of the problems associated with opioids, drug discovery efforts have been
employed to develop opioids with reduced side effects using approaches such as biased …

Small molecules selectively targeting sigma-1 receptor for the treatment of neurological diseases

N Ye, W Qin, S Tian, Q Xu, EA Wold… - Journal of medicinal …, 2020 - ACS Publications
The sigma-1 (σ1) receptor, an enigmatic protein originally classified as an opioid receptor
subtype, is now understood to possess unique structural and functional features of its own …

[HTML][HTML] Sigma-1 receptor: A drug target for the modulation of neuroimmune and neuroglial interactions during chronic pain

MC Ruiz-Cantero, R González-Cano, MÁ Tejada… - Pharmacological …, 2021 - Elsevier
Immune and glial cells play a pivotal role in chronic pain. Therefore, it is possible that the
pharmacological modulation of neurotransmission from an exclusively neuronal perspective …

The state-of-the-art pharmacotherapeutic options for the treatment of chronic non-cancer pain

RS D'Souza, B Langford, RE Wilson… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction Pharmacotherapeutic options continue to expand for the treatment of chronic
non-cancer pain. There has been an increasing emphasis on multimodal analgesia. This …

[HTML][HTML] Endocannabinoid control of glutamate NMDA receptors: the therapeutic potential and consequences of dysfunction

M Rodríguez-Muñoz, P Sánchez-Blázquez, M Merlos… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Glutamate is probably the most important excitatory neurotransmitter in the brain. The
glutamate N-methyl-D-aspartate receptor (NMDAR) is a calcium-gated channel that …

Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one …

S Intagliata, A Sharma, TI King, C Mesangeau… - The AAPS Journal, 2020 - Springer
The sigma-2 receptor has been cloned and identified as Tmem97, which is a
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …

Involvement of the opioidergic mechanism in the analgesic potential of a novel indazolone derivative: efficacy in the management of pain, neuropathy, and …

Q Ullah, Z Ali, U Rashid, G Ali, N Ahmad, R Khan… - ACS …, 2023 - ACS Publications
Indazolones possess interesting pharmacological activities. The search for indazole and
indazolone-containing nuclei as drugs is an important research area of medicinal chemistry …

The σ1 receptor engages the redox-regulated HINT1 protein to bring opioid analgesia under NMDA receptor negative control

M Rodríguez-Muñoz, P Sánchez-Blázquez… - Antioxidants & redox …, 2015 - liebertpub.com
Aims: The in vivo pharmacology of the sigma 1 receptor (σ1R) is certainly complex; however,
σ1R antagonists are of therapeutic interest, because they enhance mu-opioid receptor …

Molecular interplay between the sigma-1 receptor, steroids, and ion channels

SL Morales-Lázaro, R González-Ramírez… - Frontiers in …, 2019 - frontiersin.org
Cell excitability is tightly regulated by the activity of ion channels that allow for the passage
of ions across cell membranes. Ion channel activity is controlled by different mechanisms …