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Receptor activity

Oxytocin and Vasopressin Receptors. The actions of oxytocin and vasopressin are mediated through their interactions with receptors. Different receptor types as well as different second messenger responses help explain their diverse activities in spite of the hormones stmctural similarities. Thus oxytocin has at least one separate receptor and vasopressin has been shown to have two principal receptor types, and V2. Subclasses of these receptors have been demonstrated, and species differences further compHcate experimental analysis. It is apparent that both oxytocin and receptors function through the GP/1 phosphoHpase C complex (75), while the V2 receptors activate cycHc AMP (76). [Pg.191]

NMD A receptors are selectively activated by A/-methyl-D-aspartate (NMD A) (182). NMD A receptor activation also requires glycine or other co-agonist occupation of an allosteric site. NMDAR-1, -2A, -2B, -2C, and -2D are the five NMD A receptor subunits known. Two forms of NMDAR-1 are generated by alternative splicing. NMDAR-1 proteins form homomeric ionotropic receptors in expression systems and may do so m situ in the CNS. Functional responses, however, are markedly augmented by co-expression of a NMDAR-2 and NMDAR-1 subunits. The kinetic and pharmacological properties of the NMD A receptor are influenced by the particular subunit composition. [Pg.551]

Leukotrienes and Prostanoids. Arachidonic acid (AA) (213) and its metabohtes are iavolved ia cellular regulatory processes ia all three principal chemical signaling systems endocrine (see Hormones), immune, and neuronal (62). FoUowiag receptor activation or iacreased iatraceUular... [Pg.555]

Pharmacodynamics is the study of dmg action primarily in terms of dmg stmcture, site of action, and the biochemical and physiological consequences of the dmg action. The availabiUty of a dmg at its site of action is deterrnined by several processes (Fig. 1), including absorption, metaboHsm, distribution, and excretion. These processes constitute the pharmacokinetic aspects of dmg action. The onset, intensity, and duration of dmg action are deterrnined by these factors as well as by the avadabihty of the dmg at its receptor site(s) and the events initiated by receptor activation (see Drug delivery). [Pg.267]

Figure 13.3 G protein-mediated activation of adenylate cyclase by hormone binding. Hormone binding on the extracellular side of a receptor such as the P adrenergic receptor activates a G protein on the cytoplasmic ATP side. The activated form of the G protein... Figure 13.3 G protein-mediated activation of adenylate cyclase by hormone binding. Hormone binding on the extracellular side of a receptor such as the P adrenergic receptor activates a G protein on the cytoplasmic ATP side. The activated form of the G protein...
Smooth muscle contractions are subject to the actions of hormones and related agents. As shown in Figure 17.32, binding of the hormone epinephrine to smooth muscle receptors activates an intracellular adenylyl cyclase reaction that produces cyclic AMP (cAMP). The cAMP serves to activate a protein kinase that phosphorylates the myosin light chain kinase. The phosphorylated MLCK has a lower affinity for the Ca -calmodulin complex and thus is physiologically inactive. Reversal of this inactivation occurs via myosin light chain kinase phosphatase. [Pg.560]

A classic example of where definitive experimental data necessitated refinement and extension of a model of drug-receptor interaction involved the discovery of constitutive receptor activity in GPCR systems. The state of the art model before this finding was the ternary complex model for GPCRs, a model that cannot accommodate ligand-independent (constitutive) receptor activity. [Pg.41]


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See also in sourсe #XX -- [ Pg.267 ]




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5-Receptor agonists pharmacological activity

5-Receptor antagonists pharmacological activity

Acetylcholine receptor activation cycle

Acetylcholine receptor-inducing activity

Acetylcholine receptor-inducing activity ARIA)

Acetylcholine receptors active site

Activation of receptors

Activation of the Cytoplasmic Apo-Receptor Complexes

Active conformation metabotropic glutamate receptors

Active receptor

Active receptor

Activity receptor profiling

Adenosine A3 receptor activation

Agonist receptor activation

Agonist receptor activity

Antiestrogens estrogen receptor activation mechanisms

Anxiolytics serotonin receptor-active

Apoptosis death receptor activation

Calcitonin receptors, osteoclast activity

Calcium NMDA receptor activation

Calcium channels receptor-mediated activation

Cannabinoid receptor constitutive activity

Cell surface receptors activation

Chemokine receptor activation

Chemokine receptor activation, molecular

Cholinergic receptors activation process

Cholinergic receptors activators

Cholinergic receptors structure-activity relationships

Constitutive activated receptor

Constitutive active receptor

Constitutive active/androstane receptor

Constitutive activity of receptors

Constitutive androstane receptor activation

Constitutive androstane receptor activators

Constitutively Active Receptors and Inverse Agonists

Constitutively Active Viral Chemokine Receptors Tools for Immune Subversion and Pathogenesis

Constitutively activating receptor

Constitutively active receptor CAR

Delta receptors activation

Electrochemical recognition of anionic guest species by redox-active receptor molecules

Electrochemical recognition of charged and neutral guest species by redox-active receptor

Electrochemical recognition of charged and neutral guest species by redox-active receptor molecules

ErbB receptors activating

Erythropoietin-receptor activators

Estrogen receptor binding activity

Estrogen receptors activity assessment

Estrogen-receptors activation mechanisms

Estrogen-receptors antiestrogen activity

Estrogenic receptor activity

Fenfluramine receptor activation

Formyl peptide receptor activation

Functional assays receptor activation

G-protein coupled receptors activation

G-protein receptors, activation

G-protein-coupled receptors active

GABAa receptors, activation

GABAa receptors, activation barbiturate binding site

GABAa receptors, activation benzodiazepine binding site

GABAa receptors, activation binding affinities

GABAa receptors, activation modulatory sites

GABAa receptors, activation structure

GABAa receptors, activation subtypes

Glutamate-activated receptors

H2-receptor activity

Herpesviruses Encode Constitutively Active Viral Chemokine Receptors

Hi-receptor activity

Histamine H3 receptor, activation

Histamine receptor antagonists) structure-activity relationship

Hormone independent gene activation by truncated receptors

Hormone-activated receptor tyrosine

Hormone-activated receptor tyrosine kinase

Insulin receptor activated

Insulin receptor tyrosyl kinase activity

Insulin receptor, activation

K-Receptor agonists pharmacological activity

K-Receptor antagonists pharmacological activity

Kappa receptors activation

Kappa-opioid receptor activation

Ligand-activated nuclear receptor

Ligands peroxisome proliferator-activated receptor

Lumophore-spacer-receptor systems with redox active guests

MSP Receptor Regulation or Activation

Mechanism of Thrombin Receptor Activation

Mitogen-activated protein kinase cell-surface receptors

Mitogen-activated protein kinase growth factor receptor signaling

Mouse vas deferens activity in receptor binding assa

Mu receptors activation

Muscarinic cholinergic receptors activation process

Muscarinic receptors activation

NMDA receptors activation

NMDA receptors physiological activity

Neuronal nicotinic acetylcholine receptors activation

Neuronal receptors activation

Nicotinic acetylcholine receptors activation mechanism

Nicotinic cholinergic receptors activation process

Nicotinic receptors activation

Novel Receptor Active Substances

Nuclear hormone receptor activator

Nuclear peroxisome proliferator activated receptor

Nuclear receptors, retinoid-induced gene activation

Opioid receptors activation

P-Opioid receptor activity in guinea-pig ileum

P-Receptor agonists pharmacological activity

P-Receptor antagonists pharmacological activity

PEROXISOME PROLIFERATED -ACTIVATED RECEPTORS (PPARS)

PPARy modulator proliferator-activated receptor

PPARy, Peroxisome proliferator activated receptor gamma

Partial agonism and the two-state model of receptor activation

Peroxisomal proliferator-activated receptors

Peroxisomal proliferator-activated receptors Subject

Peroxisome Proliferator-Activated Receptor y Coactivator-la

Peroxisome Proliferator-Activated Receptor y Ligands

Peroxisome Proliferator-Activated Receptor y-Agonists and Stroke

Peroxisome proliferation-activated receptor

Peroxisome proliferation-activated receptor PPAR)

Peroxisome proliferator activated receptor -a agonists

Peroxisome proliferator activated receptor binding protein

Peroxisome proliferator activated receptor interaction with genes

Peroxisome proliferator activated receptor species difference

Peroxisome proliferator activated receptor-y

Peroxisome proliferator activator receptor- (PPAR

Peroxisome proliferator activator receptor-a

Peroxisome proliferator-activated receptor 7 agonists

Peroxisome proliferator-activated receptor PPAR agonists)

Peroxisome proliferator-activated receptor PPAR)

Peroxisome proliferator-activated receptor PPAR) pathway

Peroxisome proliferator-activated receptor PPARa activation

Peroxisome proliferator-activated receptor PPARa)

Peroxisome proliferator-activated receptor PPARy)

Peroxisome proliferator-activated receptor PPARy) agonists

Peroxisome proliferator-activated receptor action mechanisms

Peroxisome proliferator-activated receptor activation

Peroxisome proliferator-activated receptor agonists thiazolidinediones

Peroxisome proliferator-activated receptor alpha

Peroxisome proliferator-activated receptor alpha activator

Peroxisome proliferator-activated receptor alpha gene

Peroxisome proliferator-activated receptor alpha protein

Peroxisome proliferator-activated receptor atherosclerosis

Peroxisome proliferator-activated receptor balance

Peroxisome proliferator-activated receptor beta

Peroxisome proliferator-activated receptor chemistry

Peroxisome proliferator-activated receptor effects

Peroxisome proliferator-activated receptor gamma

Peroxisome proliferator-activated receptor gene expression alterations

Peroxisome proliferator-activated receptor human response

Peroxisome proliferator-activated receptor inflammation

Peroxisome proliferator-activated receptor inhibition studies

Peroxisome proliferator-activated receptor insulin sensitivity improvement

Peroxisome proliferator-activated receptor insulin sensitization

Peroxisome proliferator-activated receptor isoforms

Peroxisome proliferator-activated receptor lipid oxidation products

Peroxisome proliferator-activated receptor mechanisms

Peroxisome proliferator-activated receptor modulator

Peroxisome proliferator-activated receptor oxidative stress

Peroxisome proliferator-activated receptor pioglitazone

Peroxisome proliferator-activated receptor polyunsaturated fatty acids

Peroxisome proliferator-activated receptor rosiglitazone

Peroxisome proliferator-activated receptor signaling

Peroxisome proliferator-activated receptor target gene identification

Peroxisome proliferator-activated receptor thiazolidinedione insulin sensitizers

Peroxisome proliferator-activated receptor tissue expression

Peroxisome proliferator-activated receptor transcriptional regulation

Peroxisome proliferator-activated receptor troglitazone

Peroxisome proliferator-activated receptor-alpha (PPAR

Peroxisome proliferator-activated receptor-y (PPAR

Peroxisome proliferator-activated receptor-y agonists

Peroxisome proliferator-activated receptors

Peroxisome proliferator-activated receptors PPARs), fatty acid ligands

Peroxisome proliferator-activated receptors dual agonists

Peroxisome proliferator-activated receptors functions

Peroxisome proliferator-activated receptors structure

Peroxisome proliferators activated receptor PPAR)

Peroxisome proliferators activator receptor

Peroxisome proliferators activator receptor PPAR) agonists

Peroxisome proliferators-activated receptor

Peroxisome-activator receptor-alpha

Peroxisome-activator receptor-alpha expression

Peroxisome-proliferator activated receptors PPARs)

Platelet activating factor receptor-mediated activities

Platelet activation receptors

Platelet-activating factor receptor

Platelet-activating factor receptor antagonists

Pregnane-activated receptor

Prolactin receptor activation

Proliferator-activated receptor

Proliferator-activated receptor PPAR)-gamma

Prostanoid receptors selective ligands and structure-activity relationships

Protease-activated receptor

Protease-activated receptor signaling

Protease-activated receptors reaction

Protein tyrosine phosphorylation receptor activation

Proteinase-activated receptors

Quantitative structure-activity relationship estrogen receptor binding affinity

Receptor Activation, Tyrosine Kinase Activity, and in Cultured Vascular Smooth Muscle Cells

Receptor activation

Receptor activation

Receptor activation mechanism

Receptor activation, molecular processes

Receptor activator of NF-kB

Receptor activator of NF-kB ligand

Receptor activator of nuclear factor

Receptor activator of nuclear factor-kB ligand

Receptor activities, regulation

Receptor activity dopamine

Receptor activity modifying proteins

Receptor activity modulating proteins

Receptor activity muscarinic

Receptor activity, conjugates

Receptor agonists/activators

Receptor binding assay activity

Receptor blocking activity

Receptor constitutively active

Receptor destroying activity

Receptor molecules, redox-active

Receptor molecules, redox-active electrochemical recognition

Receptor molecules, redox-active, electrochemical recognition of charged and

Receptor molecules, redox-active, electrochemical recognition of charged and neutral

Receptor molecules, redox-active, electrochemical recognition of charged and neutral guest

Receptor molecules, redox-active, electrochemical recognition of charged and neutral guest species

Receptor natural killer cells, activation

Receptor signaling complexes activated

Receptor tyrosine kinase Activation

Receptor tyrosine kinase activity, insulin

Receptor-independent activation

Receptors activated solely by synthetic

Receptors activated solely by synthetic ligands

Receptors antitumor activity

Receptors constitutive activity

Receptors intrinsic enzyme activity

Receptors membrane-bound, activation

Receptors redox-active

Receptors redox-active center

Receptors with Associated Tyrosine Kinase Activity

Receptors with Kinase Activity

Receptors with enzymatic activity

Receptors with guanylate cyclase activity

Receptors with intrinsic enzymatic activity

Receptors with protein kinase activity

Receptors with serine/threonine kinase activity

Receptors with tyrosine kinase activity

Receptors without enzymatic activity

Regulation of Receptor Activity

Selective drugs, activity toward receptors

Serotonin receptor activity

Serotonin receptor-active agents

Signal Transmission via Transmembrane Receptors with Tyrosine-specific Protein Kinase Activity

Smad anchor for receptor activation

Structural Determinants of Ligand Binding and Receptor Activation by CC Chemokines

Structure-activity relationships drug-receptor interactions

Structure-activity relationships of dopamine receptor agonists

Structure-activity relationships receptor mapping

T cell receptor activation

Test Systems Addressing 5-HT4 Receptor Agonist Activity

The Distinction between Agonist Binding and Receptor Activation

The Estrogen Receptors and Their Multiple Gene Activation Mechanisms

The Law of Mass Action, binding sites and receptors—understanding why specific, potent biological activity is a rare property for any one chemical to possess

The Peroxisome Proliferator Activated Receptor

The del Castillo-Katz Mechanism 1. Relationship between Agonist Concentration and Fraction of Receptors in an Active Form

Thrombin receptor activation

Thrombin receptor-activating peptide TRAP)

Thrombin receptor-activating peptides

Thromboxane receptor activation

Towards electrochemical recognition of neutral guest species by redox-active receptor molecules

Urokinase plasminogen activator receptor

Urokinase-type plasminogen activator receptor

Urokinase-type plasminogen activator receptor uPAR)

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