WHO classified neurological disorders to be among 6.3% of the global disease burden. Among the most central aspects of CNS drug development is the ability of novel molecules to cross the blood-brain barrier (BBB) to reach the target site over a desired time period for therapeutic action. Based on various aspects, brain pharmacokinetics is considered to be one of the foremost perspectives for the higher attrition rate of CNS biologics. Although drug traits are important, the BBB and blood-cerebrospinal fluid barrier together with transporters become the mechanistic approach behind CNS drug delivery. The present review emphasizes neuropharmacokinetic parameters, their importance, an assessment approach and the vast effect of transporters to brain drug distribution for CNS drug discovery.
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http://dx.doi.org/10.1016/j.drudis.2019.02.007 | DOI Listing |
J Neuroimaging
January 2025
Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seongnam-si, Republic of Korea.
Background And Purpose: We investigated the relationship between serotonergic and dopaminergic specific binding transporter ratios (SBRs) over 4 years in Parkinson's disease (PD) patients. We assessed serotonergic innervation's potential compensatory role for dopaminergic denervation, association with PD symptoms, and involvement in the development of levodopa-induced dyskinesia (LID).
Methods: SBRs of the midbrain and striatum were evaluated from [I-123] N-ω-fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl)nortropane SPECT images at baseline and after 4 years.
Discov Oncol
January 2025
Department of Neurosurgery, Changde Hospital, Xiangya School of Medicine, Central South University (The First People's Hospital of Changde City), Changde, 415003, Hunan, China.
Purpose: Glioma is the most prevalent tumor of the central nervous system. The poor clinical outcomes and limited therapeutic efficacy underscore the urgent need for early diagnosis and an optimized prognostic approach for glioma. Therefore, the aim of this study was to identify sensitive biomarkers for glioma.
View Article and Find Full Text PDFNeurochem Res
January 2025
Department of Biochemistry and Molecular Biology, Federal University of Santa Maria (UFSM), Santa Maria, RS, Brazil.
Purinergic signaling plays a major role in aging and neurodegenerative diseases, which are associated with memory decline. Blackcurrant (BC), an anthocyanin-rich berry, is renowned for its antioxidant and neuroprotective activities. However, evidence on the effects of BC on purinergic signaling is lacking.
View Article and Find Full Text PDFGut Microbes
December 2025
Department of Molecular, Cellular, & Biomedical Sciences, University of New Hampshire, Durham, NH, USA.
The therapeutic benefits of opioids are compromised by the development of analgesic tolerance, which necessitates higher dosing for pain management thereby increasing the liability for drug dependence and addiction. Rodent models indicate opposing roles of the gut microbiota in tolerance: morphine-induced gut dysbiosis exacerbates tolerance, whereas probiotics ameliorate tolerance. Not all individuals develop tolerance, which could be influenced by differences in microbiota, and yet no study design has capitalized upon this natural variation.
View Article and Find Full Text PDFJ Oral Facial Pain Headache
September 2024
Department of Radiology, International School of Medicine, Istanbul Medipol University, 34200 Istanbul, Turkey.
Myofascial pain is one of the common symptoms in patients with temporomandibular joint disorders (TMD). Occlusal splint (OS) and masticatory muscle trigger point (TP) local injections are primary treatment options. We aimed to investigate the effects of these treatments using clinical and elastography measures.
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