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The opioid receptors play a pivotal role in the treatment of several neuropsychiatric and neurological disorders. (L.) Kurtz is a very important medicinal plant with several therapeutic applications. It is a main constituent of the Ayurvedic formulation 'Dashmool' used for multifaceted disorders by the Indians. However, the constituents of this plant in neurological conditions have not been well studied. Here, we performed activity-guided isolation of compounds for opioid receptor modulator activity. In the study, we found that the isolated compound baicalein () has shown the most potent and competitive antagonistic activity at 20 mg/kg dose experiments. The acute dose of (20 mg/kg) and pan opioid receptor antagonist naloxone (20 mg/kg) block the morphine-induced antinociception and the paw withdrawal latency decreases up to 8.3 s and 9.6 s, respectively. The studies also support our data that compound binds with MOR and KOR.
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http://dx.doi.org/10.1080/14786419.2024.2396452 | DOI Listing |
Cardiol Rev
September 2025
From the Department of General Medicine, J.S.S. Medical College, JSS Academy of Higher Education and Research, Mysuru, India.
Heart failure with preserved ejection fraction (HFpEF) accounts for nearly half of all heart failure cases and is increasing in prevalence due to aging populations and comorbidities such as hypertension and diabetes. While echocardiography remains the diagnostic cornerstone, many patients with preserved ejection fraction present with nonspecific symptoms and ambiguous diastolic indices, leading to diagnostic uncertainty and therapeutic delay. Arterial stiffness-quantified by pulse wave velocity, augmentation index, and cardio-ankle vascular index)-is emerging as a key contributor to HFpEF pathophysiology.
View Article and Find Full Text PDFTransl Vis Sci Technol
September 2025
Wilmer Eye Institute, School of Medicine, Johns Hopkins University, Baltimore, MD, USA.
Purpose: The purinergic receptor P2X4 is critical to transduction of ocular pain. The aim of this study was to investigate the therapeutic potential of the P2X4 receptor antagonist BAY-776 in alleviating chronic ocular pain.
Methods: Chronic ocular pain was induced in male rats (8-9 weeks old; n = 12 per group) via double lacrimal gland removal (DLGR).
J Biochem Mol Toxicol
September 2025
Department of Rehabilitation Medicine, Hebei Engineering University Affiliated Hospital, Handan, Hebei, China.
Blood-Brain Barrier (BBB) dysfunction acts as a key mediator of ischemic brain injury, contributing to brain edema, inflammatory cell infiltration, and neuronal damage. The integrity of the BBB is largely maintained by tight junction proteins, such as Claudin-5, and its disruption exacerbates neurological deficits. Neurokinin B (NKB), a neuropeptide that belongs to the tachykinin family, has been implicated in various physiological processes, including neuroinflammation and vascular function.
View Article and Find Full Text PDFDrug Dev Res
September 2025
R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, India.
Non-small cell lung cancer (NSCLC) remains a leading cause of cancer-related mortality, with "epidermal growth factor receptor (EGFR)" mutations playing a pivotal role in tumor progression and carcinogenesis. "Third-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs)," such as Osimertinib, have significantly improved treatment outcomes by overcoming resistance mechanisms like the T790M mutation. However, Osimertinib's clinical application is limited by cardiotoxicity concerns, necessitating safer alternatives.
View Article and Find Full Text PDFDrug Dev Res
September 2025
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, India.
The epidermal growth factor receptor (EGFR) is a common diver gene for lung cancer (NSCLC), which leads to an increasing death rate worldwide. This study reports the design, synthesis, and biological evaluation of triazole-clubbed pyrimidine derivatives (RDa-RDm) as potential anticancer agents. Thirteen compounds were synthesized and screened against the A549 lung cancer cell line.
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