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Effects of 5-HT1A Receptor Antagonist and 5-HT2A Receptor Agonist on Morphine Withdrawal
AbstractChronic administration of morphine causes physical dependence, possibly through serotonin 5‑HT 1A receptor (5-HT 1A R) and 5-HT 2A receptor (5-HT
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The classical D1 dopamine receptor antagonist SCH23390 is a functional sigma-1 receptor allosteric modulator
SCH23390 is a widely used D 1 dopamine receptor (D 1 R) antagonist that also elicits some D 1 R-independent effects. We previously found that the...
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Preparation and preliminary evaluation of a tritium-labeled allosteric P2X4 receptor antagonist
P2X4 receptors are ATP-gated cation channels that were proposed as novel drug targets due to their role in inflammation and neuropathic pain. Only...
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DT-0111: a novel P2X3 receptor antagonist
Extracellular adenosine 5’-triphosphate (ATP) acts as an autocrine and paracrine agent, the actions of which on affected cells are mediated by P2...
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DP2 receptor activity sensor suited for antagonist screening and measurement of receptor dynamics in real-time
The DP2 receptor is a G-protein coupled receptor involved in allergic inflammation and is the target of recently developed antagonists already being...
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Mendelian randomization uncovers a protective effect of interleukin-1 receptor antagonist on kidney function
Interleukins (ILs), key cytokine family of inflammatory response, are closely associated with kidney function. However, the causal effect of various...
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A potent new-scaffold androgen receptor antagonist discovered on the basis of a MIEC-SVM model
Prostate cancer (PCa) is the second most prevalent malignancy among men worldwide. The aberrant activation of androgen receptor (AR) signaling has...
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Interleukin-1 Receptor Antagonist as Therapy for Traumatic Brain Injury
Traumatic brain injury is a common type of acquired brain injury of varying severity carrying potentially deleterious consequences for the afflicted...
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Structure-based drug discovery of a corticotropin-releasing hormone receptor 1 antagonist using an X-ray free-electron laser
Thus far, attempts to develop drugs that target corticotropin-releasing hormone receptor 1 (CRF 1 R), a drug target in stress-related therapy, have...
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CYX-5, a G-protein biassed MOP receptor agonist, DOP receptor antagonist and KOP receptor agonist, evokes constipation but not respiratory depression relative to morphine in rats
BackgroundStrong opioid analgesics such as morphine alleviate moderate to severe acute nociceptive pain (e.g. post-surgical or post-trauma pain) as...
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Combining a noble gas with radiotherapy: glutamate receptor antagonist xenon may act as a radiosensitizer in glioblastoma
BackgroundIonotropic glutamate receptors α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor (AMPAR) and N-methyl-D-aspartate receptor...
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GM-1020: a novel, orally bioavailable NMDA receptor antagonist with rapid and robust antidepressant-like effects at well-tolerated doses in rodents
The NMDA receptor (NMDAR) antagonist ketamine has shown great potential as a rapid-acting antidepressant; however, its use is limited by poor oral...
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Effect of Gonadotropin-Releasing Hormone Antagonist on the Expression Patterns of Insulin-Like Growth Factor 1, Androgen Receptor, and Luteinizing Hormone Receptor in an Experimental Rat Model of Functional Ovarian Cysts
We studied the expression of insulin-like growth factor 1 (IGF-1), androgen receptor (AR) and luteinizing hormone receptor (LHR) in the ovaries under...
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Therapeutic potential of the topical recombinant human interleukin-1 receptor antagonist in guinea pigs with allergic rhinitis
BackgroundRecombinant human Interleukin receptor antagonist (rhIL-Ra) can bind to the IL-1 receptor on the cell membrane and reversibly blocks the...
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Haloperidol, a Sigma-1 Receptor Antagonist, Inhibits Ca2+ Responses in Rat Peritoneal Macrophages
AbstractSigma-1 receptors are ubiquitous multifunctional ligand-regulated molecular chaperons in the membrane of the endoplasmic reticulum, having a...
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The kisspeptin-1 receptor antagonist peptide-234 aggravates uremic cardiomyopathy in a rat model
Uremic cardiomyopathy is characterized by diastolic dysfunction, left ventricular hypertrophy (LVH), and fibrosis. Dysregulation of the kisspeptin...
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The role of a novel mineralocorticoid receptor antagonist, finerenone, in chronic kidney disease: mechanisms and clinical advances
BackgroundChronic kidney disease (CKD) poses a significant health risk in contemporary society. Current CKD treatments primarily involve...
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The non-steroidal mineralocorticoid receptor antagonist finerenone and heart failure with preserved ejection fraction
Finerenone is a novel non-steroidal mineralocorticoid receptor (MR) antagonist (MRA) with high binding affinity, high MR selectivity and a short...
