Results 1 to 10 of about 18,176 (269)

Ligand and G-protein selectivity in the κ-opioid receptor. [PDF]

Nature, 2023
AbstractThe κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders1. However, the development of KOR analgesics has been hindered by the associated hallucinogenic side effects2.
Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T.   +13 more
europepmc   +7 more sources

The atomistic level structure for the activated human κ-opioid receptor bound to the full Gi protein and the MP1104 agonist. [PDF]

Proc Natl Acad Sci U S A, 2020
The kappa opioid receptor (κOR) is an important target for pain therapeutics to reduce depression and other harmful side effects of existing medications. The analgesic activity is mediated by κOR signaling through the adenylyl cyclase-inhibitory family of Gi protein. Here, we report the three-dimensional (3D) structure for the active state of human κOR
Mafi A, Kim SK, Goddard WA.
europepmc   +11 more sources

Nalfurafine Hydrochloride, a κ-Opioid Receptor Agonist, Induces Melanophagy via PKA Inhibition in B16F1 Cells [PDF]

Cells, 2022
Selective autophagy controls cellular homeostasis by degrading unnecessary or damaged cellular components. Melanosomes are specialized organelles that regulate the biogenesis, storage, and transport of melanin in melanocytes.
Ha Jung Lee, Seong Hyun Kim, Yong Hwan Kim, So Hyun Kim, Gyeong Seok Oh, Ji-Eun Bae, Joon Bum Kim, Na Yeon Park, Kyuhee Park, Eunbyul Yeom, Kwiwan Jeong, Pansoo Kim, Doo Sin Jo, Dong-Hyung Cho   +13 more
doaj   +2 more sources

Enantiomerically Pure Quinoline-Based κ-Opioid Receptor Agonists: Chemoenzymatic Synthesis and Pharmacological Evaluation. [PDF]

ChemMedChem, 2020
AbstractRacemic K‐opioid receptor (KOR) agonist 2‐(3,4‐dichlorophenyl)‐1‐[(4aRS,8SR,8aSR)‐8‐(pyrrolidin‐1‐yl)‐3,4,4a,5,6,7,8,8a‐octahydroquinolin‐1(2H)‐yl]ethan‐1‐one ((±)‐4) was prepared in a diastereoselective synthesis. The first key step of the synthesis was the diastereoselective hydrogenation of the silyl ether of 1,2,3,4‐tetrahydroquinoin‐8‐ol ((
Martin B, Schepmann D, Bernal FA, Schmidt TJ, Che T, Loser K, Wünsch B.   +6 more
europepmc   +5 more sources

The κ-opioid receptor-induced autophagy is implicated in stress-driven synaptic alterations [PDF]

Frontiers in Molecular Neuroscience, 2022
Recent evidence has shown that G protein-coupled receptors (GPCRs) are direct sensors of the autophagic machinery and opioid receptors regulate neuronal plasticity and neurotransmission with an as yet unclarified mechanism.
Christos Karoussiotis, Aggeliki Sotiriou, Alexia Polissidis, Alexandra Symeonof, Danae Papavranoussi-Daponte, Vassiliki Nikoletopoulou, Zafiroula Georgoussi   +6 more
doaj   +2 more sources

Effects of the novel selective κ-opioid receptor agonist NP-5497-KA on morphine-induced reward-related behaviors [PDF]

Scientific Reports, 2023
Opioid addiction and the opioid overdose epidemic are becoming more serious, and the development of therapeutic agents is essential for the pharmacological treatment of substance use disorders.
Soichiro Ide, Toshitake Hirai, Takafumi Muto, Tomio Yamakawa, Kazutaka Ikeda   +4 more
doaj   +2 more sources

Central δ/κ opioid receptor signaling pathways mediate chronic and/or acute suckling-induced LH suppression in rats during late lactation [PDF]

The Journal of Reproduction and Development
In mammals, secretion of tonic (pulsatile) gonadotropin-releasing hormone (GnRH)/luteinizing hormone (LH) is often suppressed during lactation. Suppression of GnRH/LH pulses in lactating dams is assumed to be caused by suckling stimuli and a chronic ...
Yoshihisa UENOYAMA, Miku NONOGAKI, Hitomi TSUCHIDA, Marina TAKIZAWA, Sena MATSUZAKI, Naoko INOUE, Hiroko TSUKAMURA   +6 more
doaj   +2 more sources

Decoding the κ Opioid Receptor (KOR): Advancements in Structural Understanding and Implications for Opioid Analgesic Development [PDF]

Molecules
The opioid crisis in the United States is a significant public health issue, with a nearly threefold increase in opioid-related fatalities between 1999 and 2014. In response to this crisis, society has made numerous efforts to mitigate its impact. Recent
Zoe Li, Ruili Huang, Menghang Xia, Nancy Chang, Wenjing Guo, Jie Liu, Fan Dong, Bailang Liu, Ann Varghese, Aasma Aslam, Tucker A. Patterson, Huixiao Hong   +11 more
doaj   +2 more sources

Central nicotine induces browning through hypothalamic κ opioid receptor [PDF]

Nature Communications, 2019
Nicotine reduces food intake and increases energy expenditure in brown adipose tissue. Here the authors show that nicotine also induces white adipose tissue browning via central kappa opioid receptor action.
Patricia Seoane-Collazo, Laura Liñares-Pose, Eva Rial-Pensado, Amparo Romero-Picó, José María Moreno-Navarrete, Noelia Martínez-Sánchez, Pablo Garrido-Gil, Ramón Iglesias-Rey, Donald A. Morgan, Naoki Tomasini, Samuel Andrew Malone, Ana Senra, Cintia Folgueira, Gema Medina-Gomez, Tomás Sobrino, José L. Labandeira-García, Rubén Nogueiras, Ana I. Domingos, José-Manuel Fernández-Real, Kamal Rahmouni, Carlos Diéguez, Miguel López   +21 more
doaj   +2 more sources

8-epi-Salvinorin B: crystal structure and affinity at the κ opioid receptor [PDF]

Beilstein Journal of Organic Chemistry, 2007
There have been many reports of epimerization of salvinorins at C-8 under basic conditions, but little evidence has been presented to establish the structure of these compounds.
Thomas A. Munro, Katharine K. Duncan, Richard J. Staples, Wei Xu, Lee-Yuan Liu-Chen, Cécile Béguin, William A. Carlezon Jr., Bruce M. Cohen   +7 more
doaj   +2 more sources