Pharmacology of opioids
... Naturally occurring opioid compounds are found in plants (e.g. morphine) and produced in the body (endogenous opioids), where they are widely distributed throughout the central nervous system (CNS). These endogenous compounds are peptides that have variable potency and are preferentially bound by di ...
... Naturally occurring opioid compounds are found in plants (e.g. morphine) and produced in the body (endogenous opioids), where they are widely distributed throughout the central nervous system (CNS). These endogenous compounds are peptides that have variable potency and are preferentially bound by di ...
Effect of novel adenosine A3 receptor antagonist
... Sheep is a species that shows 85% overall identity of the adenosine A3 receptor with its human ortholog. In this study we demonstrate a role for the adenosine A3 receptor in ovine allergic airway responses. In isolated tracheal preparations taken from sheep naturally sensitive to Ascaris suum, antig ...
... Sheep is a species that shows 85% overall identity of the adenosine A3 receptor with its human ortholog. In this study we demonstrate a role for the adenosine A3 receptor in ovine allergic airway responses. In isolated tracheal preparations taken from sheep naturally sensitive to Ascaris suum, antig ...
Leuprorelin rescues polyglutamine
... Leuprorelin-treated AR-97Q mice showed a decrease in body weight and deterioration in the rotarod task at an age of 8–9 weeks (Figs. 1e,f and 3a), when serum testosterone initially increased through the agonistic effect of leuprorelin (Fig. 1a). This change was transient and was followed by sustaine ...
... Leuprorelin-treated AR-97Q mice showed a decrease in body weight and deterioration in the rotarod task at an age of 8–9 weeks (Figs. 1e,f and 3a), when serum testosterone initially increased through the agonistic effect of leuprorelin (Fig. 1a). This change was transient and was followed by sustaine ...
Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine
... The effect of ParaA on nAChR on Xenopus oocytes injected with T. marmorata ␣12 ␥␦ nAChR-rich membranes was investigated. The oocytes responded to the ACh application with stable currents from the second day after the injection forward. Each oocyte was first tested with ACh to ascertain consistent re ...
... The effect of ParaA on nAChR on Xenopus oocytes injected with T. marmorata ␣12 ␥␦ nAChR-rich membranes was investigated. The oocytes responded to the ACh application with stable currents from the second day after the injection forward. Each oocyte was first tested with ACh to ascertain consistent re ...
Characterising nicotinic acetylcholine receptors in the plant parasitic
... within a short time period while the environmental conditions are optimal. Therefore, locomotion is an essential component of its invasion strategy. It belongs to the phylum Nematoda, which also includes the free-living model genetic nematode C. elegans. We explored the idea that the neurobiological ...
... within a short time period while the environmental conditions are optimal. Therefore, locomotion is an essential component of its invasion strategy. It belongs to the phylum Nematoda, which also includes the free-living model genetic nematode C. elegans. We explored the idea that the neurobiological ...
Glyceraldehyde-3-Phosphate Dehydrogenase Is a GABAA Receptor
... glyceraldehyde-3-phosphate dehydrogenase (GAPDH). Molecular constructs demonstrated that GAPDH directly phosphorylates the long intracellular loop of GABAA receptor ␣1 subunit at identified serine and threonine residues. GAPDH and the ␣1 subunit were found to be colocalized at the neuronal plasma me ...
... glyceraldehyde-3-phosphate dehydrogenase (GAPDH). Molecular constructs demonstrated that GAPDH directly phosphorylates the long intracellular loop of GABAA receptor ␣1 subunit at identified serine and threonine residues. GAPDH and the ␣1 subunit were found to be colocalized at the neuronal plasma me ...
Pre- or postsynaptic distribution of distinct endocannabinoid
... the reduction of further neurotransmitter release from the axon terminals (Wilson & Nicoll, 2002). Variations of this basic functional logic are responsible for various forms of short-term and longterm synaptic plasticity mediated by 2-AG (Chevaleyre et al, 2006), which can be the mechanisms underly ...
... the reduction of further neurotransmitter release from the axon terminals (Wilson & Nicoll, 2002). Variations of this basic functional logic are responsible for various forms of short-term and longterm synaptic plasticity mediated by 2-AG (Chevaleyre et al, 2006), which can be the mechanisms underly ...
Potent Neuropeptide Y Y, Receptor Antagonist, 1229U91: Blockade
... via Y, receptors. However, because of the lack of potent and selective antagonists for Y, receptors, it has not been clarified whether Y, receptors regulate physiological feeding behavior. Recently, nonpeptide Y, antagonists, BIBP3226 and SR120819A, have been reported with K, values of 7.2 and 21 nM ...
... via Y, receptors. However, because of the lack of potent and selective antagonists for Y, receptors, it has not been clarified whether Y, receptors regulate physiological feeding behavior. Recently, nonpeptide Y, antagonists, BIBP3226 and SR120819A, have been reported with K, values of 7.2 and 21 nM ...
... This study demonstrates that the TP receptor antagonist, BAY u 3405, produces only partial protection against PGD2-induced airway narrowing at 90 min after ingestion. The magnitude of protection was similar when 20, 50 or 100 mg doses were used, despite increasing plasma concentrations of BAY u 3405 ...
Allosteric Binding Sites on Muscarinic Acetylcholine Receptors
... the affinity of the endogenous ligand for the orthosteric site (such allosteric agents are also referred to as allosteric enhancers or inhibitors, respectively) and/or for exogenously applied orthosteric ligands. During the past decade, considerable efforts have been focused on developing novel ther ...
... the affinity of the endogenous ligand for the orthosteric site (such allosteric agents are also referred to as allosteric enhancers or inhibitors, respectively) and/or for exogenously applied orthosteric ligands. During the past decade, considerable efforts have been focused on developing novel ther ...
Could membrane lipids influence the receptor tyrosine kinase
... by Guan and co-workers (31). They used a UDP-Gal/ /UDP-GalNAc 4-epimerase deficient variant of Chinese Hamster Ovary cell line (IdlD4) transfected with EGFR gene (IdlD4/EGFR). The IdlD4 cell line is incapable of synthesizing galactose containing glycans, including gangliosides and glycoproteins, unl ...
... by Guan and co-workers (31). They used a UDP-Gal/ /UDP-GalNAc 4-epimerase deficient variant of Chinese Hamster Ovary cell line (IdlD4) transfected with EGFR gene (IdlD4/EGFR). The IdlD4 cell line is incapable of synthesizing galactose containing glycans, including gangliosides and glycoproteins, unl ...
Ca Channels As Integrators of G Protein
... proteins (Hanlon et al., 1999). Heterologous expression experiments have shown that in the absence of channel -subunit, the ␣1-subunit is retained in the endoplasmic reticulum (Bichet et al., 2000). Under basal conditions (in the absence of transmitter), coexpression of the ␣1-subunit with a -subu ...
... proteins (Hanlon et al., 1999). Heterologous expression experiments have shown that in the absence of channel -subunit, the ␣1-subunit is retained in the endoplasmic reticulum (Bichet et al., 2000). Under basal conditions (in the absence of transmitter), coexpression of the ␣1-subunit with a -subu ...
Multidimensional scaling reveals the main evolutionary pathways of class A G-protein-coupled receptors.
... widespread in the animal kingdom and are usually assumed to be G-protein-coupled receptors (GPCRs) by similarity with their vertebrate counterparts. Because they transduce signals from a wide variety of chemical or physical stimuli, these receptors are involved in the perception by the cell of its e ...
... widespread in the animal kingdom and are usually assumed to be G-protein-coupled receptors (GPCRs) by similarity with their vertebrate counterparts. Because they transduce signals from a wide variety of chemical or physical stimuli, these receptors are involved in the perception by the cell of its e ...
Expression of ml-m4 Muscarinic Acetylcholine Receptor Proteins in
... systems may contribute to memory loss and other cognitive deficits in Alzheimer’s disease (Coyle et al., 1983). Indeed, the potential for cholinergic replacement therapies in dementia (McKinney and Coyle, 1991; Davis et al., 1992) has provided a great incentive for improved understanding of the role ...
... systems may contribute to memory loss and other cognitive deficits in Alzheimer’s disease (Coyle et al., 1983). Indeed, the potential for cholinergic replacement therapies in dementia (McKinney and Coyle, 1991; Davis et al., 1992) has provided a great incentive for improved understanding of the role ...
Lipid and Lipoprotein Population Distributions - Lectures For UG-5
... Primarily LDL elevations Synthesis may be normal but decrease or lack LDL receptors due to mutation in LDL receptor gene. Therefore LDL builds-up in serum Since cells cannot acquire from LDL therefore increase internal synthesis of cholesterol. ...
... Primarily LDL elevations Synthesis may be normal but decrease or lack LDL receptors due to mutation in LDL receptor gene. Therefore LDL builds-up in serum Since cells cannot acquire from LDL therefore increase internal synthesis of cholesterol. ...
Localization of Glycine Neurotransmitter Transporter (GLYT2
... To see some of the rostral staining the sections were developed longer, even if the staining in the spinal cord reached a saturated level . Therefore, GLYT2 appeared to be more abundant in midbrain and diencephalon from the immunostaining results in comparison with western blot (Fig. 1) . The specif ...
... To see some of the rostral staining the sections were developed longer, even if the staining in the spinal cord reached a saturated level . Therefore, GLYT2 appeared to be more abundant in midbrain and diencephalon from the immunostaining results in comparison with western blot (Fig. 1) . The specif ...
Anticoagulants, Thrombolytics Agents and Antiplatelet Drugs
... 1. Schafer AI. Am J Med 1996; 101: 199–209. ...
... 1. Schafer AI. Am J Med 1996; 101: 199–209. ...
Localization of Leptin Binding Domain in the Leptin Receptor
... Sequence analysis of OB-Rb indicated that it is a member of the class I cytokine receptor family; this family includes GH-R, EPO-R, interleukin-6 receptor, and GCSF-R. The extracellular region of these receptors are characterized by the presence of multiple domains, including CK, C2, and F3 (Fig. 1) ...
... Sequence analysis of OB-Rb indicated that it is a member of the class I cytokine receptor family; this family includes GH-R, EPO-R, interleukin-6 receptor, and GCSF-R. The extracellular region of these receptors are characterized by the presence of multiple domains, including CK, C2, and F3 (Fig. 1) ...
Supplementary Files
... Ionotropic glutamate receptors are ligand-gated ion channels. They are divided into different receptor types based on their pharmacological properties. The key receptor sub-groups are GluA (AMPA, 2-amino-3-3- hydroxy-5-methyl-isoxazol-4-yl propanoic acid), GluD (δ), GluK (kainate), and the GluN (NMD ...
... Ionotropic glutamate receptors are ligand-gated ion channels. They are divided into different receptor types based on their pharmacological properties. The key receptor sub-groups are GluA (AMPA, 2-amino-3-3- hydroxy-5-methyl-isoxazol-4-yl propanoic acid), GluD (δ), GluK (kainate), and the GluN (NMD ...
Informatics approaches to understanding TGFb pathway regulation
... distinct points in the pathway. Inhibitory Smads (I-Smads) antagonize signaling near the top of the pathway by blocking interactions between type I receptors and R-Smads and also by preventing R-Smad–Co-Smad complex formation (Miyazono, 2008). Members of the Sno/Corl/Dac family of nuclear corepresso ...
... distinct points in the pathway. Inhibitory Smads (I-Smads) antagonize signaling near the top of the pathway by blocking interactions between type I receptors and R-Smads and also by preventing R-Smad–Co-Smad complex formation (Miyazono, 2008). Members of the Sno/Corl/Dac family of nuclear corepresso ...
19 Sensation of Smell-14322012-09
... the mucous layer overlying the receptors. Diffusion through the layer brings the odorants into contact with the olfactory cilia, where they bind with receptors (odorant-binding proteins). This leads to an activation of a second messenger system which depolarises the the receptive cell and initiates ...
... the mucous layer overlying the receptors. Diffusion through the layer brings the odorants into contact with the olfactory cilia, where they bind with receptors (odorant-binding proteins). This leads to an activation of a second messenger system which depolarises the the receptive cell and initiates ...
Histamine receptor antagonists
... Prostaglandins, histamine, and serotonin belong to a group of compounds called autacoids. These heterogeneous substances have widely differing structures and pharmacologic activities. They all have the common feature of being formed by the tissues on which they act; thus, they function as local horm ...
... Prostaglandins, histamine, and serotonin belong to a group of compounds called autacoids. These heterogeneous substances have widely differing structures and pharmacologic activities. They all have the common feature of being formed by the tissues on which they act; thus, they function as local horm ...
as a PDF
... been found after long-term treatment with various antidepressants 3°. These findings have led to the suggestion that an excess of 5-HT at some receptors, probably the 5-HT 2 type, could be involved in depressive illness. The 5-HT1A agonist 8-OH-DPAT has been found to selectively reduce brain 5-HT sy ...
... been found after long-term treatment with various antidepressants 3°. These findings have led to the suggestion that an excess of 5-HT at some receptors, probably the 5-HT 2 type, could be involved in depressive illness. The 5-HT1A agonist 8-OH-DPAT has been found to selectively reduce brain 5-HT sy ...
Opioid Receptor Imaging with Positron Emission Tomography and
... mu receptors remain unoccupied and thus available for action by the endogenous opioid ligands in critical brain regions. These unoccupied receptors are also available for action by exogenous opioid ligands commonly used for the relief of pain. The half-life of methadone in the racemic (d,l or S,R) f ...
... mu receptors remain unoccupied and thus available for action by the endogenous opioid ligands in critical brain regions. These unoccupied receptors are also available for action by exogenous opioid ligands commonly used for the relief of pain. The half-life of methadone in the racemic (d,l or S,R) f ...
Antipsychotic drugs reverse the AMPA receptor-stimulated release
... At the end of the experiments, rats were killed by an overdose of anesthetic. The placement of the dialysis probes was examined by perfusion of fast green dye and visual inspection of the probe track after cutting the brain at the appropriate levels. In experiments involving the local application of ...
... At the end of the experiments, rats were killed by an overdose of anesthetic. The placement of the dialysis probes was examined by perfusion of fast green dye and visual inspection of the probe track after cutting the brain at the appropriate levels. In experiments involving the local application of ...
NMDA receptor
The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel protein found in nerve cells. It is activated when glutamate and glycine (or D-serine) bind to it, and when activated it allows positively charged ions to flow through the cell membrane. The NMDA receptor is very important for controlling synaptic plasticity and memory function.The NMDAR is a specific type of ionotropic glutamate receptor. The NMDA receptor is named this because the agonist molecule N-methyl-D-aspartate (NMDA) binds selectively to it, and not to other glutamate receptors. Activation of NMDA receptors results in the opening of an ion channel that is nonselective to cations with a reversal potential near 0 mV. A property of the NMDA receptor is its voltage-dependent activation, a result of ion channel block by extracellular Mg2+ & Zn2+ ions. This allows the flow of Na+ and small amounts of Ca2+ ions into the cell and K+ out of the cell to be voltage-dependent.Calcium flux through NMDARs is thought to be critical in synaptic plasticity, a cellular mechanism for learning and memory. The NMDA receptor is distinct in two ways: first, it is both ligand-gated and voltage-dependent; second, it requires co-activation by two ligands: glutamate and either D-serine or glycine.The activity of the NMDA receptor is affected by many psychoactive drugs such as phencyclidine (PCP), alcohol (ethanol) and dextromethorphan (DXM). The anaesthetic effects of the drugs ketamine and nitrous oxide are partially because of their effects on NMDA receptor activity.