Synthesis and Pharmacological Evaluation of Fluorinated Quinoxaline‐Based κ‐Opioid Receptor (KOR) Agonists Designed for PET Studies
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DOI: 10.1002/cmdc.202000502
Abstract: κ‐Opioid receptors (KORs) play a predominant role in pain alleviation, itching skin diseases, depression and neurodegenerative disorders such as multiple sclerosis. Therefore, imaging of KOR by a fluorinated PET tracer was envisaged. Two strategies were… read more here.
Keywords: kor; pharmacological evaluation; evaluation fluorinated; fluorinated quinoxaline ... See more keywords
Biosensors Monitor Ligand-Selective Effects at Kappa Opioid Receptors.
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DOI: 10.1007/164_2020_427
Abstract: The kappa opioid receptor (KOR) has emerged as a promising therapeutic target for pain and itch treatment. There is growing interest in biased agonists that preferentially activate select signaling pathways downstream of KOR activation on… read more here.
Keywords: kor; biosensors monitor; selective effects; receptor ... See more keywords
Opioid receptors mRNAs expression and opioids agonist-dependent G-protein activation in the rat brain following neuropathy
Sign Up to like & getrecommendations! Published in 2020 at "Progress in Neuro-Psychopharmacology and Biological Psychiatry"
DOI: 10.1016/j.pnpbp.2019.109857
Abstract: Potent opioid-based therapies are often unsuccessful in promoting satisfactory analgesia in neuropathic pain. Moreover, the side-effects associated with opioid therapy are still manifested in neuropathy-like diseases, including tolerance, abuse, addiction and hyperalgesia, although the mechanisms… read more here.
Keywords: kor; dor; opioid receptors; mrnas expression ... See more keywords
Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the κ-Opioid Receptor for the Treatment of Chronic Abdominal Pain
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DOI: 10.1021/acs.jmedchem.1c00158
Abstract: The rising opioid crisis has become a worldwide societal and public health burden, resulting from the abuse of prescription opioids. Targeting the κ-opioid receptor (KOR) in the periphery has emerged as a powerful approach to… read more here.
Keywords: peptide; opioid receptor; kor; chronic abdominal ... See more keywords
Comparison of Pharmacological Properties between the Kappa Opioid Receptor Agonist Nalfurafine and 42B, Its 3-Dehydroxy Analogue: Disconnect between in Vitro Agonist Bias and in Vivo Pharmacological Effects.
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DOI: 10.1021/acschemneuro.0c00407
Abstract: Nalfurafine, a moderately selective kappa opioid receptor (KOR) agonist, is used in Japan for treatment of itch without causing dysphoria or psychotomimesis. Here we characterized pharmacology of compound 42B, a 3-dehydroxy analog of nalfurafine and… read more here.
Keywords: opioid receptor; kor; agonist; nalfurafine 42b ... See more keywords
Role of RGS12 in the differential regulation of kappa opioid receptor-dependent signaling and behavior
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DOI: 10.1038/s41386-019-0423-7
Abstract: Kappa opioid receptor (KOR) agonists show promise in ameliorating disorders, such as addiction and chronic pain, but are limited by dysphoric and aversive side effects. Clinically beneficial effects of KOR agonists (e.g., analgesia) are predominantly… read more here.
Keywords: protein; opioid receptor; kor; arrestin signaling ... See more keywords
Conditional deletion of KOR (Oprk1) in kisspeptin cells does not alter LH pulses, puberty, or fertility in mice.
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DOI: 10.1210/endocr/bqac175
Abstract: Classic pharmacological studies suggested that endogenous dynorphin-KOR signaling is important for reproductive neuroendocrine regulation. With the seminal discovery of an interconnected network of hypothalamic arcuate neurons co-expressing kisspeptin, neurokinin B, and dynorphin ("KNDy neurons"), the… read more here.
Keywords: kisspeptin cells; hypothesis; kisspeptin; kndy neurons ... See more keywords
Agonists Specific for κ-Opioid Receptor Induces Apoptosis of HCC Cells Through Enhanced Endoplasmic Reticulum Stress
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DOI: 10.3389/fonc.2022.844214
Abstract: Cancer pain is an important factor affecting life quality of patients especially in the advanced stage and relieving pain is one of fundamental strategies for cancer treatment. Opioids such as morphine are the most widely… read more here.
Keywords: hcc cells; hcc; malignant phenotypes; mor ... See more keywords