Beta-carbolines and indoloquinolizidines occur in plants, and some of the former compounds also in mammalian tissues. Many beta-carbolines cause tremor or convulsions, and they are among the most potent known endogenous compounds to bind to benzodiazepine, tryptamine and serotonin binding sites. In this study seven indoloquinolizidines which are formal derivatives of 1,2-disubstituted 1,2,3,4-tetrahydro-beta-carbolines were assayed for their affinity for benzodiazepine, tryptamine and serotonin binding sites in rat brain in vitro. Three of them exhibited significant affinity for tryptamine receptors: Ki values ranged from 0.97 microM upwards. The affinity spectra towards different receptors greatly varied from compound to compound showing selectivity to one or several of the binding sites now studied. These derivatives of beta-carbolines may be useful tools when assessing the physiological functions of the tryptamine and other binding sites.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/0028-3908(86)90019-5 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Genetic predisposition to Behcet's disease mediated by a IL10RA enhancer polymorphism.
Heliyon
January 2025
The First Affiliated Hospital of Chongqing Medical University, Chongqing Branch (Municipality Division) of National Clinical Research Center for Ocular Diseases, Chongqing, PR China.
Background: Several studies suggested the genetic association between IL10RA variants and susceptibility to Behcet's disease (BD). However, the precise mechanism of the association is still unknown. The purpose of this study was to investigate the mechanism underlying the genetic associations between IL10RA polymorphisms and the risk of BD.
View Article and Find Full Text PDFProbing the Signal Transduction Mechanism of the Light-Activated Adenylate Cyclase OaPAC Using Unnatural Amino Acid Mutagenesis.
ACS Chem Biol
January 2025
Department of Chemistry, Stony Brook University, Stony Brook, New York 11794-3400, United States.
OaPAC, the photoactivated adenylyl cyclase from , is composed of a blue light using FAD (BLUF) domain fused to an adenylate cyclase (AC) domain. Since both the BLUF and AC domains are part of the same protein, OaPAC is a model for understanding how the ultrafast modulation of the chromophore binding pocket caused by photoexcitation results in the activation of the output domain on the μs-s time scale. In the present work, we use unnatural amino acid mutagenesis to identify specific sites in the protein that are involved in transducing the signal from the FAD binding site to the ATP binding site.
View Article and Find Full Text PDFEster-Bearing Calix[]phenoxazines: Side Chain Enhanced Recognition and Redox-Responsive Reversible Host-Guest System.
J Org Chem
January 2025
School of Pharmaceutical and Chemical Engineering & Institute for Advanced Studies, Taizhou University, 1139 Shifu Avenue, Taizhou 318000, Zhejiang,China.
We report an enhanced recognition and redox-responsive reversible host-guest system based on ester-bearing calix[]phenoxazines. The carbonyl groups, oriented toward the cavity, act as the extra binding sites to enhance the binding affinity, which is confirmed by NMR and FTIR experiments and single-crystal structure analysis. Due to the oxidizable nature of calix[]phenoxazine, a redox-controlled reversible response is established.
View Article and Find Full Text PDFSynthesis, Molecular Docking, Antimicrobial, and Antioxidant Evaluation of Novel Dithiazole and Thiazole Derivatives.
Curr Org Synth
January 2025
Microbial Genetics Department, Biotechnology Research Institute, National Research Centre, Giza, Egyp.
Introduction: An efficient procedure was reported for the synthesis of novel hybrid dithiazoles 7 and thiazoles 15, in good yields, by applying hydrazonyl chlorides 4 with thiocarbohydrazone derivatives 3 and 12.
Methods: The thiazole derivatives were evaluated for their antimicrobial and antioxidant activities.
Results: According to the results, thiazoles revealed marked potency as antimicrobial and antioxidant agents.
Evaluating the potential of Kalanchoe pinnata, Piper amalago amalago, and other botanicals as economical insecticidal synergists against Anopheles gambiae.
Malar J
January 2025
Caribbean Centre for Research in Biosciences, Natural Products Institute, University of the West Indies, Kingston, Jamaica.
Background: Synergists reduce insecticide metabolism in mosquitoes by competing with insecticides for the active sites of metabolic enzymes, such as cytochrome P450s (CYPs). This increases the availability of the insecticide at its specific target site. The combination of both insecticides and synergists increases the toxicity of the mixture.
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!