Increased numbers of platelet high affinity alpha 2-adrenoceptors binding sites have been reported in depressed patients using the agonist radioligand [3H]clonidine, whereas no differences from controls have been found using antagonist radioligands. We have measured platelet high affinity alpha 2-adrenoceptors in 13 depressed patients and 14 well-matched controls using a new selective agonist radioligand, [3H]UK-14,304. Unlike previous studies using [3H]clonidine, we find no differences in Bmax or KD of the high affinity alpha 2-adrenoceptor binding sites between the 2 groups.

Download full-text PDF

Source
http://dx.doi.org/10.1016/0014-2999(86)90067-1DOI Listing

Publication Analysis

Top Keywords

high affinity
16
platelet high
12
binding sites
12
depressed patients
12
affinity alpha
12
alpha 2-adrenoceptors
8
agonist radioligand
8
affinity
4
affinity adrenoceptor
4
adrenoceptor binding
4

Similar Publications

Radioactive iodine, a key waste product of nuclear energy, has been a significant concern among nuclear materials because of its high volatility and its ability to easily enter the human metabolism. Porous materials containing a large number of N-heterocyclic units such as carbazole in the skeletons use as effective adsorbents showing high iodine capture capacities. Herein, a new carbazole-bismaleimide-based hyper-cross-linked porous organic polymer (CzBMI-POP) was successfully prepared from a new tetra-armed carbazole-maleimide monomer (Bis-Cz(BMI)), which contains biscarbazole units and maleimide side groups.

View Article and Find Full Text PDF

The Ca/calmodulin-dependent protein kinase II α (CaMKIIα) plays a crucial role in regulating neuronal signaling and higher brain functions, being involved in various brain diseases. Utilization of small molecules targeting the CaMKIIα hub domain has proved to be a promising strategy for specific CaMKIIα modulation and future therapy. Through an structure-based virtual screening campaign, we herein identified 2-arylthiazole-4-carboxylic acids as a new class of high-affinity CaMKIIα hub ligands.

View Article and Find Full Text PDF

Antigen receptor ITAMs provide tonic signaling by acting as guanine nucleotide exchange factors to directly activate R-RAS2.

Sci Signal

January 2025

Centro de Biología Molecular Severo Ochoa, Consejo Superior de Investigaciones Científicas, Universidad Autónoma de Madrid, 28049 Madrid, Spain.

The small GTPase R-RAS2 regulates homeostatic proliferation and survival of T and B lymphocytes and, when present in high amounts, drives the development of B cell chronic lymphocytic leukemia. In normal and leukemic lymphocytes, R-RAS2 constitutively binds to antigen receptors through their immunoreceptor tyrosine-based activation motifs (ITAMs) and promotes tonic activation of the phosphatidylinositol 3-kinase (PI3K) signaling pathway. Here, we examined the molecular mechanisms underlying this direct interaction and its consequences for R-RAS2 activity.

View Article and Find Full Text PDF

It has been well accumulated that G-quadruplex (G4-DNA) has great anticancer relevance, and various heterocyclic moieties have been synthesized and examined as potent G4-DNA binders with promising anticancer activity. Here, we have synthesized a series of naphthalimide-triazole-coumarin conjugates by substituting various amines and further examine their anticancer activity against 60 human cancer cell lines at 10 μM. One and five dose concentration results reveal low values of MG-MID GI for compounds including (3.

View Article and Find Full Text PDF

Nanobodies or variable antigen-binding domains (VH) derived from heavy chain-only antibodies (HcAb) occurring in the Camelidae family offer certain superior physicochemical characteristics like enhanced stability, solubility, and low immunogenicity compared to conventional antibodies. Their efficient antigen-binding capabilities make them a preferred choice for next-generation small biologics. In the present work, we design an anti-SARS-CoV-2 bi-paratopic nanobody drug conjugate by screening a nanobody database.

View Article and Find Full Text PDF

Want 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!