A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for the compounds at 5-HT(2) receptor subtypes are reported. The analogue which showed the highest 5-HT(2C) binding affinity (27, 1.6nM) was found to be successful in reducing food intake in rats.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2005.10.029 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
GW117 induces anxiolytic effects by improving hippocampal functions.
Pharmacol Biochem Behav
November 2024
Department of Pharmacology, School of Basic Medical Sciences, Capital Medical University, Beijing 100069, China.
GW117 functions as both an MT1/MT2 receptor agonist and a 5-HT2C receptor antagonist. This study aimed to investigate the anxiolytic effects of GW117 through behavioral assessments, including the open field test and novelty-suppressed feeding test (NSFT) within a chronic unpredictable mild stress (CUMS) model. GW117 was administered via oral gavage for 21 days to evaluate its sustained anxiolytic effects, with behavioral tests including the NSFT, the Vogel-conflict test, and the O-maze test.
View Article and Find Full Text PDFBmal1 haploinsufficiency impairs fear memory and modulates neuroinflammation via the 5-HT2C receptor.
Front Pharmacol
November 2024
Department of Infectious Diseases and Shenzhen Key Laboratory for Endogenous Infections, The 6th Affiliated Hospital of Shenzhen University Health Science Center, Shenzhen, China.
Background: BMAL1, a key regulator of circadian rhythms, plays a multifaceted role in brain function. However, the complex interplay between BMAL1, memory, neuroinflammation, and neurotransmitter regulation remains poorly understood. To investigate these interactions, we conducted a study using BMAL1-haplodeficient mice (BMAL1).
View Article and Find Full Text PDFSignificant 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 PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!