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| http://dx.doi.org/10.1038/npp.2010.119 | DOI Listing |
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Significant haematological alterations in clozapine-treated patients: prevalence and clinical correlation.
Acta Neuropsychiatr
November 2024
Department of Psychiatry, Firat University School of Medicine, Elazig, Turkey.
Objectives: Clozapine is an atypical antipsychotic crucial for treatment-resistant schizophrenia, characterised by its multi-receptor targeting, including serotonin (5-HT2A, 5-HT2C) and dopamine (D1, D2, D3, D4) receptors, among others. This broad mechanism is effective against positive symptoms of schizophrenia with a lower incidence of extrapyramidal side effects. However, clozapine poses significant haematological risks, notably agranulocytosis, necessitating stringent blood monitoring protocols.
View Article and Find Full Text PDFMescaline-induced behavioral alterations are mediated by 5-HT2A and 5-HT2C receptors in rats.
Pharmacol Biochem Behav
December 2024
Psychedelic Research Centre, National Institute of Mental Health, Topolová 748, Klecany 250 67, Czechia. Electronic address:
Rationale: Mescaline is a classical psychedelic compound with a phenylethylamine structure that primarily acts on serotonin 5-HT2A/C receptors, but also binds to 5-HT1A and 5-HT2B receptors. Despite being the first psychedelic ever isolated and synthesized, the precise role of different serotonin receptor subtypes in its behavioral pharmacology is not fully understood.
Objectives: In this study, we aimed to investigate how selective antagonists of 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT1A receptors affect the behavioral changes induced by subcutaneous administration of mescaline (at doses of 10, 20, and 100 mg/kg) in rats.
The effect of cancer-associated mutations on ligand binding and receptor function - A case for the 5-HT receptor.
Eur J Pharmacol
December 2024
Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, 2333 CC, Leiden, the Netherlands; Oncode Institute, 2333 CC, Leiden, the Netherlands. Electronic address:
The serotonin 5-HT receptor is a G protein-coupled receptor (GPCR) mainly expressed in the central nervous system. Besides regulating mood, appetite, and reproductive behavior, it has been identified as a potential target for cancer treatment. In this study, we aimed to investigate the effects of cancer patient-derived 5-HT receptor mutations on ligand binding and receptor functionality.
View Article and Find Full Text PDFActivation of ventral pallidum-projecting neurons in the nucleus accumbens via 5-HT receptor stimulation regulates motivation for wheel running in male mice.
Neuropharmacology
December 2024
Laboratory of Molecular Pharmacology, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, 920-1192, Japan. Electronic address:
Rodents have a strong motivation for wheel running; however, the neural mechanisms that regulate their motivation remain unknown. We investigated the possible involvement of serotonin (5-HT) systems in regulating motivation for wheel running in male mice. Systemic administration of a 5-HT receptor antagonist (WAY100635) increased the number of wheel rotations, whereas administration of a 5-HT or 5-HT receptor antagonist (volinanserin or SB242084, respectively) decreased it.
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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