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Opioid receptor distribution in the claustrum-dorsal endopiriform complex [PDF]

open access: yesiScience
Summary: The claustrum and dorsal endopiriform form a subcortical structure reciprocally connected to the neocortex and enriched in opioid receptors. However, the precise cellular distribution of opioid receptors within this region remains unclear. Using
Matthew Bolger   +2 more
doaj   +2 more sources

Opioid Receptor-Mediated Regulation of Neurotransmission in the Brain

open access: yesFrontiers in Molecular Neuroscience, 2022
Opioids mediate their effects via opioid receptors: mu, delta, and kappa. At the neuronal level, opioid receptors are generally inhibitory, presynaptically reducing neurotransmitter release and postsynaptically hyperpolarizing neurons.
Kaitlin C. Reeves   +6 more
doaj   +1 more source

Expression and Localization of Opioid Receptors in Male Germ Cells and the Implication for Mouse Spermatogenesis. [PDF]

open access: yesPLoS ONE, 2016
The presence of endogenous opioid peptides in different testicular cell types has been extensively characterized and provides evidence for the participation of the opioid system in the regulation of testicular function.
Haizea Estomba   +6 more
doaj   +1 more source

The opioid receptor: emergence through millennia of pharmaceutical sciences

open access: yesFrontiers in Pain Research, 2023
Throughout history humanity has searched for an optimal approach to the use of opioids that maximizes analgesia while minimizing side effects. This review reflects upon the conceptualization of the opioid receptor and the critical role that the ...
Carolyn A. Fairbanks   +4 more
doaj   +1 more source

Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands

open access: yesFrontiers in Pharmacology, 2022
The present study investigated the in vitro pharmacology of the human kappa opioid receptor using multiple assays, including calcium mobilization in cells expressing chimeric G proteins, the dynamic mass redistribution (DMR) label-free assay, and a ...
Chiara Sturaro   +11 more
doaj   +1 more source

Design and development of novel, short, stable dynorphin-based opioid agonists for safer analgesic therapy

open access: yesFrontiers in Pharmacology, 2023
Kappa opioid receptors have exceptional potential as an analgesic target, seemingly devoid of many problematic Mu receptor side-effects. Kappa-selective, small molecule pharmaceutical agents have been developed, but centrally mediated side-effects limit ...
Rink-Jan Lohman   +4 more
doaj   +1 more source

Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

open access: yeseLife, 2021
Controlling receptor functional selectivity profiles for opioid receptors is a promising approach for discovering safer analgesics; however, the structural determinants conferring functional selectivity are not well understood.
Rajendra Uprety   +23 more
doaj   +1 more source

Models of neuroinflammation for the assessment of kappa-opioid receptor ligands

open access: yesФармация и фармакология (Пятигорск), 2023
The development of new drugs to combat neuroinflammation is highly relevant as it opens up possibilities for the treatment of a wide range of diseases, including Alzheimer’s disease, Parkinson’s disease, epilepsy, schizophrenia, depression, and others ...
K. Yu. Kalitin   +2 more
doaj   +1 more source

Mu Opioid Receptor Heterodimers Emerge as Novel Therapeutic Targets: Recent Progress and Future Perspective

open access: yesFrontiers in Pharmacology, 2020
Opioids are the most effective analgesics used in the clinical management of cancer pain or non-cancer pain. However, chronic opioids therapy can cause many side effects including respiratory depression, nausea, sedation, itch, constipation, analgesic ...
Li Zhang   +4 more
doaj   +1 more source

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