Pharmacology of receptors. Medical search. Frequent questions

Department of Pharmacology, Kagawa Univ. (bvsalud.org)

There was a close correlation between agonist the receptor occupation and the receptor activation. (acs.org)
The activation of heteromeric and homomeric nicotinic acetylcholine receptors was studied in Xenopus laevis oocytes to identify key structures of putative agonist molecules associated with the selective activation of homomeric α7 receptors. (aspetjournals.org)
A Biased Agonist at Immunometabolic Receptor GPR84 Causes Distinct Functional Effects in Macrophages. (ox.ac.uk)
Several screening tools for study of receptor mechanism with agonist and antagonist have been developed. (stmjournals.in)
In human airways, this neutrophil accumulation can be re-capitulated via intrabronchial exposure to lipopolysaccharide (LPS), a Toll-like receptor 4 (TLR4) agonist, that also causes a local increase in the neutrophil-mobilizing cytokine IL-26. (lu.se)

Thank you for sharing this Journal of Pharmacology and Experimental Therapeutics article. (aspetjournals.org)
A parallel approach may be applied to developing therapeutics targeting other peptide hormone G protein-coupled receptors. (nih.gov)
BERTRAND, D. Nicotinic acetylcholine receptors: from basic science to therapeutics. (bvsalud.org)

Our Purine Receptor review gives an overview of the subtypes and structures of the P2 receptor family, and the pharmacological ligands used to study them. (tocris.com)
Transmembrane guanylyl cyclases are homodimeric receptors activated by a diverse range of endogenous ligands. (guidetopharmacology.org)
Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, [6] making α3β4 a promising target for the development of novel antiaddictive agents. (wikipedia.org)
The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. (uos.ac.uk)
In this study we wanted to characterize the G protein activation properties of the two known cannabinoid receptors and GPR55 following stimulation with different cannabinoid ligands, using bioluminescence resonance energy transfer (BRET). (biomedcentral.com)
Violin JD, Lefkowitz RJ (2007) Beta-arrestin-biased ligands at seven-transmembrane receptors. (springer.com)
Increased understanding of cannabinoid receptor pharmacology and the discovery of endogenous ligands of these receptors has prompted debate and further research into the clinical utility of exogenous cannabinoid receptor agonists relative to the unwanted psychotropic effects of these agents. (nature.com)

The adenine receptor is a putative G-protein-coupled receptor thought to be involved in purinergic signalling. (tocris.com)
Anatomical profiling of G protein-coupled receptor expression. (guidetomalariapharmacology.org)
The chemerin receptor (CMKLR1) is a G protein-coupled receptor found on select immune, epithelial, and dorsal root ganglion/spinal cord neuronal cells. (nih.gov)
The protein encoded by this gene is an orphan G protein-coupled receptor whose ligand is unknown. (nih.gov)
G-protein-coupled receptor GPR161 is overexpressed in breast cancer and is a promoter of cell proliferation and invasion. (nih.gov)
The structural basis of G-protein-coupled receptor function and dysfunction in human diseases. (nih.gov)
False positive non-synonymous polymorphisms of G-protein coupled receptor genes. (nih.gov)
G-protein-coupled receptor signaling and neural tube closure defects. (nih.gov)
GPR84 is an orphan G-protein-coupled receptor that is expressed on immune cells and implicated in several inflammatory diseases. (ox.ac.uk)
GPR55 is an orphan G protein-coupled receptor which has been suggested to be a novel member of the cannabinoid receptor family. (biomedcentral.com)
Kim JY, Haastert PV, Devreotes PN (1996) Social senses: G-protein-coupled receptor signaling pathways in Dictyostelium discoideum . (springer.com)
Nordstrom KJ, Sallman Almen M, Edstam M et al (2011) Independent HHsearch, Needleman-Wunsch-based, and motif analyses reveal the overall hierarchy for most of the G protein-coupled receptor families. (springer.com)
PARs (protease-activated receptors) are a family of seven-transmembrane G-protein coupled receptor for proteases from circulation, inflammatory cells and endothelial tissues. (stmjournals.in)

Three of the five classes of Bn receptor antagonists that interacted with higher affinity with the fBB 4 -R functioned as fBB 4 -R antagonists and two as partial agonists. (acs.org)
Functional electrophysiological (TEVC) experiments indeed showed these compounds to be antagonists at cloned, homomeric KA receptors. (ku.dk)
The use of transgenic and gene knockout animals, gene manipulated cells, pharmacological LPA receptor agonists and antagonists have provided many insights into the biological significance of LPA and individual LPA receptors in the progression of atherosclerosis and vascular diseases. (edu.au)

British journal of pharmacology, 178 (S1). (uos.ac.uk)

It works by binding at motor nicotinic acetylcholine receptors and keeping myocytes in a depolarized state. (picmonic.com)
Myocytes still have succinylcholine actively bound to motor-nicotinic receptors and there is a constant depolarized state. (picmonic.com)
It binds to the nicotinic acetylcholine receptor and keeps the receiving nerve stuck in a depolarized state. (picmonic.com)
Succincylcholine exerts its action by binding to the motor nicotinic receptor, which typically only accepts endogenous acetylcholine. (picmonic.com)
This drug mimics acetylcholine at the nicotinic receptor, opening sodium channels and causing membrane depolarization. (picmonic.com)
The alpha-3 beta-4 nicotinic receptor , also known as the α3β4 receptor and the ganglion-type nicotinic receptor , [1] is a type of nicotinic acetylcholine receptor , consisting of α3 and β4 subunits . (wikipedia.org)
As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3) m (β4) n where m + n = 5]. (wikipedia.org)

1990) A family of AMPA-selective glutamate receptors. (guidetopharmacology.org)
Ionotropic glutamate receptors (iGluRs) are the primary mediators of fast excitatory neurotransmission in the mammalian CNS where they are involved in learning and memory formation. (ku.dk)

fBB 4 -R expression in cells widely used for other Bn receptor subtypes was unsuccessful as was expression in two frog cell lines. (acs.org)
Each ligand may interact with multiple receptor subtypes. (msdmanuals.com)
This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. (nih.gov)
Four subtypes (M1-M4) in muscarinic receptors (mACh-R) were discovered by the method of gene technology. (nii.ac.jp)

Reflecting the existing nomenclature of this family, a proposed classification of 'P0 receptor' has been suggested. (tocris.com)
However, the nomenclature of CCLR2 for this receptor and its classification as a member of the chemokine receptor family is provisional pending confirmation of chemokine binding. (guidetomalariapharmacology.org)
It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate. (uos.ac.uk)

DPhe 6 ,βAla 11 ,Phe 13 ,Nle 14 ]Bn(6−14) was found to have high affinity ( K i = 0.4 nM) for the fBB 4 receptor and 125 I-[DTyr 6 ,βala 11 ,Phe 13 ,Nle 14 ]Bn(6−14) to be an excellent ligand for this receptor. (acs.org)
A drug's ability to affect a given receptor is related to the drug's affinity (probability of the drug occupying a receptor at any given instant) and intrinsic efficacy (intrinsic activity-degree to which a ligand activates receptors and leads to cellular response). (msdmanuals.com)
The endogenous ligand for this receptor, acetylcholine, is removed from the receptor in second. (picmonic.com)
Beta-2 adrenergic receptors have also been found to couple with Gi, possibly providing a mechanism by which response to ligand is highly localized within cells. (wikipedia.org)
Here we report the pharmacology of a series of novel N1-substituted 2,3-quinoxalinediones, as well as the crystal structure of one compound (JP-10-7A) in the GluK1 ligand binding domain (GluK1-LBD) at 1.85 Å resolution. (ku.dk)

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. (uos.ac.uk)

Maintaining the second edition's focus on cell membrane receptors and the immediate signal transduction events at the membrane, this edition includes updated chapters on receptor structure and signal transduction by G-proteins and tyrosine kinases as well as enhancements to the quantitative treatment of drug-receptor interactions. (routledge.com)
The cell membrane receptors by which HDE initiates these responses have not been identified. (cdc.gov)

The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that binds epinephrine (adrenaline), a hormone and neurotransmitter whose signaling, via adenylate cyclase stimulation through trimeric Gs proteins, increases cAMP, and, via downstream L-type calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. (wikipedia.org)
It is possible that M2 and M2 come from dif-ferent modification of receptor proteins, such as phosphorylation, methylation, association with other protein or polymerization. (nii.ac.jp)
CB 1 and CB 2 cannabinoid receptors are G protein-coupled receptors which have been described to couple mainly to the G i/o subfamily of G proteins. (biomedcentral.com)
Sequence comparison does not support an evolutionary link between halobacterial retinal proteins including bacteriorhodopsin and eukaryotic G-protein-coupled receptors. (springer.com)

This third edition continues to combine current understanding of classical quantitative pharmacology and drug-receptor interactions with the basics of receptor structure and signal transduction mechanisms, providing an integrated analysis of the mechanisms of drug action at membrane receptors. (routledge.com)

Odorant receptors (ORs) belong to a large gene family of rhodopsin-like G protein-coupled receptors (GPCRs). (aspetjournals.org)
The product of this gene belongs to the family of G-protein coupled receptors. (nih.gov)
Genetic drift and selective forces have shaped the individual structure of a given receptor gene but also of the species-specific receptor repertoire - a process that is still ongoing. (springer.com)

Gyombolai, P., Turu, G. & Hunyady, L. Characterization of different G protein coupling properties of CB 1 and CB 2 cannabinoid receptors and GPR55 receptor using BRET. (biomedcentral.com)

Via six widely distributed G protein-coupled receptors (GPCRs), LPA elicits a plethora of biological responses, contributing to inflammation, thrombosis and atherosclerosis. (edu.au)

Catalytic receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, enzymes and transporters. (uos.ac.uk)

International Union of Basic and Clinical Pharmacology. (aspetjournals.org)

Based on structural comparisons of previously characterized selective and nonselective agonists, we hypothesize at least three chemical motifs exist that, when present in molecules containing an appropriate cationic center, could be associated with the selective activation of α7 receptors. (aspetjournals.org)
A few selective compounds that can discriminate between AMPA and kainate (KA) receptors are available. (ku.dk)
The structure and pharmacology will be valuable for design of new and more GluK3-selective quinoxalinedione analogues. (ku.dk)
This receptor is coupled to the stimulation of the phosphoinositide and adenylyl cyclase pathways and behaves as a selective purinoceptor. (nih.gov)
Non-selective receptor antagonist. (abcam.com)

The modal gating behavior of single sheep cardiac sarcoplasmic reticulum (SR) Ca2+-release/ryanodine receptor (RyR) channels was assessed. (ox.ac.uk)
An abnormal ryanodine receptor that controls calcium release causes a buildup of calcium in skeletal muscle, resulting in a massive metabolic reaction. (medscape.com)

Airway epithelial epidermal growth factor receptor mediates hogbarn dust-induced cytokine release but not Ca2+ response. (cdc.gov)
Because several other inhaled agents induce airway epithelial cell responses through epidermal growth factor receptor (EGFR) activation, we hypothesized that HDE would activate EGFRs and that EGFRs would be required for some of the responses to HDE. (cdc.gov)
Sigalling and trafficking of the cysteinyl leukotriene receptors in intestinal epithelial cells. (lu.se)

Sensory conflict theory (the most widely accepted explanation for motion sickness) proposes that the condition is caused by conflict between the visual, vestibular, and somatosensory systems, and involves complex neurophysiologic signaling between multiple nuclear regions, neurotransmitters, and receptors. (cdc.gov)

The rescue of the single lysine mutant P2X 2 subunit by wild-type P2X 3 (but not the converse) suggests that the heteromeric channel contains one P2X 2 and two P2X 3 subunits and that the receptor functions essentially normally as long as two subunits are not mutated. (aspetjournals.org)
The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries. (wikipedia.org)
Gα o with the C-terminal 5 amino acids replaced with those of Gα q , Gα s or Gα 12 , respectively) co-expressed with EYFP-tagged α 1 α 11 subunit and the receptor in CHO cells. (biomedcentral.com)

Few if any drugs are absolutely specific for one receptor or subtype, but most have relative selectivity. (msdmanuals.com)
Cardiac maCh-R (M2 subtype) are thought to consist of a single species of receptor protein. (nii.ac.jp)

XCR1 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. (guidetomalariapharmacology.org)

The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. (uos.ac.uk)
With the discovery of the protective arm of the renin-angiotensin system (RAS), interest has grown in protective RAS-related receptors such as the angiotensin AT(2)-receptor [AT(2)R] as potential new drug targets. (mdc-berlin.de)

selectivity relates largely to physicochemical binding of the drug to cellular receptors. (msdmanuals.com)
However, within the KA receptor family (GluK1-5) only compounds with selectivity towards GluK1 exist [1]. (ku.dk)
Thus, there is an unmet need for Tool compounds with selectivity towards the remaining KA receptor subunits. (ku.dk)

His research interests have included the role of bradykinin receptors in the human nasal airway, the control of microvascular circulation in human skin, and the mechanism of activation of dendritic cells. (routledge.com)
Interestingly, Beta-2 adrenergic receptor was observed to localize exclusively to the T-tubular network of adult cardiomyocytes, as opposed to Beta-1 adrenergic receptor, which is observed also on the outer plasma membrane of the cell Activation of the β2 adrenoreceptor with long-acting agents such as oral clenbuterol and intravenously-infused albuterol results in skeletomuscular hypertrophy and anabolism. (wikipedia.org)
Numerous studies documented for activation of PAR2 receptors through several proteases suggests its role in pain and inflammation. (stmjournals.in)

The purinergic receptor P2Y11 choreographs the polarization, mitochondrial metabolism, and migration of T lymphocytes. (nih.gov)

Chapter 1 PIXORIZE Pharmacology 2021: 1. (freemedtube.net)
PIXORIZE Pharmacology 2021: 6. (freemedtube.net)
PIXORIZE Pharmacology 2021: 8. (freemedtube.net)
PIXORIZE Pharmacology 2021: 17. (freemedtube.net)
PIXORIZE Pharmacology 2021: 18. (freemedtube.net)

Different receptors use inositol trisphosphate to mobilize Ca(2+) from different intracellular pools. (cam.ac.uk)
Publications] A. Mizushima: 'The H-L subgroup of guinea-pig cardiac M_2 receptors (M_2 ) regulates formation of inositol phosphates. (nii.ac.jp)
Most histamine H1 receptors operate through the inositol phosphate/diacylglycerol second messenger system. (bvsalud.org)

The Role of Inflammation, Hypoxia, and Opioid Receptor Expression in Pain Modulation in Patients Suffering from Obstructive Sleep Apnea. (iasp-pain.org)

The valuable source of large-scale genomic information initiated attempts to identify the origin(s) of G protein-coupled receptors (GPCR), count and categorize those genes, and follow their evolutionary history. (springer.com)
The chapter summarizes evolutionary processes working on GPCR genes and sheds light on their consequences at the levels of receptor structure and function. (springer.com)

We have studied systematically the distribution of receptors for substance P in the airway smooth muscle of the rabbit using both functional studies and light-microscopic autoradiography. (aspetjournals.org)

Roth Lab team and collaborators create molecules that selectively target the MT1 melatonin receptor to modulate the biological clocks in animal models of jet lag. (unc.edu)

Thank you for sharing this Molecular Pharmacology article. (aspetjournals.org)
Message Body (Your Name) thought you would be interested in this article in Molecular Pharmacology. (aspetjournals.org)
Overview of Pharmacodynamics Pharmacodynamics (sometimes described as what a drug does to the body) is the study of the biochemical, physiologic, and molecular effects of drugs on the body and involves receptor binding. (msdmanuals.com)
Physiologic functions (eg, contraction, secretion) are usually regulated by multiple receptor-mediated mechanisms, and several steps (eg, receptor-coupling, multiple intracellular 2nd messenger substances) may be interposed between the initial molecular drug-receptor interaction and ultimate tissue or organ response. (msdmanuals.com)
1 From the Molecular Pharmacology Research Center, and Molecular Cardiology Research Institute, Tufts Medical Center, Boston, Massachusetts 02111. (nih.gov)
Molecular Pharmacology of Synthetic Cannabinoids: Delineating CB1 Receptor-Mediated Cell Signaling. (musc.edu)

Comparative Effects of Direct Renin Inhibitor and Angiotensin Receptor Blocker on Albuminuria in Hypertensive Patients with Type 2 Diabetes. (bvsalud.org)
We compared the effect of aliskiren, a direct renin inhibitor (DRI), with that of angiotensin receptor blockers (ARBs) on albuminuria and urinary excretion of angiotensinogen , a marker of intrarenal renin-angiotensin system activity. (bvsalud.org)

These processes have left footprints in the genomic sequence that can be detected by bioinformatic methods and may help to interpret receptor function in the light of a given species in its environment. (springer.com)

Pain management in patients with OSA may create problems arousing from alterations in neuropeptide systems and overexpression of opioid receptors in hypoxia conditions, leading to intensification of side effects, e.g., respiratory depression and increased opioid sensitivity for analgesic effects. (iasp-pain.org)
opioid receptor agonists. (erowid.org)

2001) Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. (guidetopharmacology.org)

1. Hollmann M, O'Shea-Greenfield A, Rogers SW, Heinemann S. (1989) Cloning by functional expression of a member of the glutamate receptor family. (guidetopharmacology.org)

Among the many responses mediated by these receptors are smooth muscle contraction, increased vascular permeability, hormone release, and cerebral glyconeogenesis. (bvsalud.org)

Schioth HB, Fredriksson R (2005) The GRAFS classification system of G-protein coupled receptors in comparative perspective. (springer.com)

Markovian models of low and high activity levels of cardiac ryanodine receptors. (ox.ac.uk)
Publications] X.M. Zhou: 'The SH-H subgroup of cardiac M_2 receptors (M_2 ) inhibits adenulate cyclase activity. (nii.ac.jp)

His current major research interests are N-methyl-D-aspartate (NMDA) receptors in the stubstantia nigra in relation to cell death in Parkinson's disease and also ion transport and signaling in mast cells in relation to intracellular pH and volume regulation. (routledge.com)

In contrast, Beta-1 adrenergic receptors are coupled only to Gs, and stimulation of these results in a more diffuse cellular response. (wikipedia.org)
In cells expressing different receptors linked to Ins(1,4,5)P(3) formation, maximal stimulation of any one of them often releases all the Ins(1,4,5)P(3)-sensitive Ca(2+) stores, suggesting that Ins(1,4, 5)P(3) is used similarly by many receptors. (cam.ac.uk)

Multiple receptor antagonist. (abcam.com)

Department of Neuroscience and Pharmacology and Novo Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen, Copenhagen, Denmark (M.C.P., T.W.S. (aspetjournals.org)

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