Abstract Xinguan No. 3 has been recommended for the treatment of coronavirus disease 2019 (COVID-19); however, its potential mechanisms are unclear. This study aims to explore against COVID-19 through network pharmacology and molecular docking. We first searched ingredients in three databases (Traditional Chinese Medicine Systems Pharmacology Database Analysis Platform, Traditional Medicines In...

Recently, a series of 5-HT7 receptor antagonists have been developed (24,29,36,68). Among them SB-258741, R-(+)-1-(toluene-3-sulfonyl)-2-[2-(4-methylpiperidin-1-yl)ethyl]-pyrrolidine, (compound "13" in 36,37) was one of the most potent and specific compounds. Due to a lack of specific ligands the pharmacology of 5-HT7 receptor antagonists is still relatively unexplored. It has been suggested, h...

Calcitonin-family receptors comprise calcitonin receptor-like receptor (CL) or calcitonin receptor and receptor activity-modifying protein (RAMP) pairings. Calcitonin gene-related peptide (CGRP) receptors are CL/RAMP1, whereas adrenomedullin (AM) receptors are CL/RAMP2 (AM1 receptor) or CL/RAMP3 (AM2 receptor). Amylin (Amy) receptors are RAMP hetero-oligomers with the calcitonin receptor (AMY1,...

Inotropes and vasopressors are biologically and clinically important compounds that originate from different pharmacological groups and act at some of the most fundamental receptor and signal transduction systems in the body. More than 20 such agents are in common clinical use, yet few reviews of their pharmacology exist outside of physiology and pharmacology textbooks. Despite widespread use i...

Published: Trends Pharmacol Sci. 2014 Oct;35(10):537-547. doi: 1 10.1016/j.tips.2014.08.002. 2 3 Trends in Pharmacological Science – accepted version 4 5 P2X7 receptor: an emerging target in CNS diseases 6 7 by Beata Sperlagh and Peter Illes 8 9 Department of Pharmacology, Institute of Experimental Medicine, Hungarian 10 Academy of Sciences, H-1450 Budapest, Hungary and Rudolf-Boehm-Institute 1...

Opioid receptors have been targeted for the treatment of pain and related disorders for thousands of years and remain the most widely used analgesics in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with opioid receptor like-1 (ORL1) being the least characterized. All four receptors are G-protein coupled and activate inhibit...

Opioids are a mainstay in acute pain management and produce their effects side (e.g., tolerance, opioid-use disorder immune suppression) by interaction with opioid receptors. I will discuss pharmacology some controversial areas of enquiry anaesthetic relevance. The main target is the µ (mu,MOP) receptor but other members family, δ (delta; DOP) κ (kappa; KOP) receptors also analgesic actions. Th...

Pannexin 1 (Panx1), an ortholog to invertebrate innexin gap junctions, has recently been proposed to be the pore induced by P2X(7) receptor (P2X(7)R) activation. We explored the pharmacological action of compounds known to block gap junctions on Panx1 channels activated by the P2X(7)R and the mechanisms involved in the interaction between these two proteins. Whole cell recordings revealed disti...

The sigma-1 receptor (S1R) is a 223 amino acid two transmembrane (TM) pass protein. It is a non-ATP-binding nonglycosylated ligand-regulated molecular chaperone of unknown three-dimensional structure. The S1R is resident to eukaryotic mitochondrial-associated endoplasmic reticulum and plasma membranes with broad functions that regulate cellular calcium homeostasis and reduce oxidative stress. S...

Lysophosphatidic acid (LPA) is a small ubiquitous lipid found in vertebrate and nonvertebrate organisms that mediates diverse biological actions and demonstrates medicinal relevance. LPA's functional roles are driven by extracellular signaling through at least six 7-transmembrane G protein-coupled receptors. These receptors are named LPA1-6 and signal through numerous effector pathways activate...