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External Validation of the Population Pharmacokinetic Models of Amisulpride and Remedial Strategies for Delayed or Missed Doses.
Drug Des Devel Ther
January 2025
Department of Pharmacy, Xi'an Mental Health Center, Xi'an, Shaanxi, 710100, People's Republic of China.
Objective: This study aimed to evaluate the predictive performance of published amisulpride population pharmacokinetic (PopPK) models in schizophrenia patients with an external data set and establish remedial dosing regimens for nonadherent amisulpride-treated patients.
Methods: A systematic search was conducted on PubMed, Embase, and Web of Science to identify PopPK models for evaluation. The evaluation process involved analyzing 390 serum concentration samples obtained from 361 Chinese adult inpatients diagnosed with schizophrenia.
Spontaneous formation of small and ultrasmall unilamellar vesicles in mixtures of drug surfactant and phospholipid: Effect of chemical structure of phospholipid tails on vesicle size.
J Colloid Interface Sci
December 2024
Department of Medicinal Chemistry, Uppsala University, P.O. Box 547, 751 23, Uppsala, Sweden. Electronic address:
We have investigated the effect of length and chemical structure of phospholipid tails on the spontaneous formation of unilamellar liposomal vesicles in binary solute mixtures of cationic drug surfactant and zwitterionic phosphatidylcholine phospholipids. Binary drug surfactant-phospholipid mixtures with four different phospholipids with identical headgroups (two saturated phospholipids 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC, 14:0) and 1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC, 16:0), and two unsaturated lipids 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC, 18:1) and 1,2-Dierucoyl-sn-Glycero-3-Phosphatidylcholine (DEPC, 22:1)) combined with two different tricyclic antidepressant drugs (amitriptyline hydrochloride (AMT) and doxepin hydrochloride (DXP)) have been investigated with small-angle neutron scattering (SANS) and cryo-transmission electron microscopy (cryo-TEM). We observe a conspicuous impact of phospholipid tail structure on both micelle-to-vesicle transition point and vesicle size.
View Article and Find Full Text PDFAmphetamine Derivatives as Potent Central Nervous System Multitarget SERT/NET/H Agents: Synthesis and Biological Evaluation.
Molecules
November 2024
School of Pharmacy, Nanjing Tech University, 30th South Puzhu Road, Nanjing 211816, China.
In this research, a variety of novel amphetamine derivatives were synthesized and assessed for their potential as multifaceted antidepressant agents. Among these compounds, compound demonstrated potent inhibitory effects on both serotonin and noradrenaline transporters (SERT/NET) and high affinity for histamine H receptor (HR), and displayed low affinity for off-target receptors (H1, α1) and hERG channels, which can reduce the prolongation of the QT interval. Molecular docking studies offered a rational binding model of compound when it forms a complex with SERT, NET, and the histamine H receptor.
View Article and Find Full Text PDFNeurotrophin receptors of the Trk family are involved in the regulation of brain development and neuroplasticity, and therefore can serve as targets for anti-cancer and stroke-recovery drugs, antidepressants, and many others. The structures of Trk protein domains in various states upon activation need to be elucidated to allow rational drug design. However, little is known about the conformations of the transmembrane and juxtamembrane domains of Trk receptors.
View Article and Find Full Text PDFDesign, synthesis and biological evaluation of arylpropylamine derivatives as potential multi-target antidepressants.
Bioorg Med Chem
November 2024
School of Pharmacy, Nanjing Tech University, 30th South Puzhu Road, Nanjing 211816, China. Electronic address:
Article Synopsis
- This study focuses on a new series of arylpropylamine compounds designed as potential multi-target antidepressants, with a highlight on compound (R)-13j.
- Compound (R)-13j showed strong inhibition of serotonin and noradrenaline transporters while having low affinity for certain receptors, potentially minimizing side effects.
- In animal tests, (R)-13j significantly reduced signs of depression compared to duloxetine, demonstrating a favorable safety and effectiveness profile, suggesting it could be a promising new treatment for depression.
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