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  • affinity
  • K.A. Neve, R.A. Henningsen, J.M. Kinzie, T. de Paulis, D.E. Schmidt, R.M. Kessler and A. Janowsky: Sodium-dependent isomerization of dopamine D-2 receptors characterized using [125I]epidepride, a high-affinity substituted benzamide ligand, J Pharm Exp Ther 252: 1108-1116 (1990). (springer.com)
  • C.A. Mathis, J.E. Bishop, J.M. Gerdes, B. Faggin, and R. Mailman: Synthesis of aryl-substituted 5-[18F]fluoroalkylbenzamides: High affinity ligands for dopamine D-2 studies. (springer.com)
  • Research suggests that it does not have any appreciable affinity for other metabotropic glutamate receptors, ionotropic NMDA receptors, or kainate receptors, nor does it appear to have any affinity for adrenergic, benzodiazepine/GABAergic, histaminergic or muscarinic receptors. (wikipedia.org)
  • Because many receptors are essentially enzymes, the field of pharmakinetics utilizes the Michaelis-Menten equation to describe drug affinity (dissociation constant Kd) and total binding (Bmax). (wikipedia.org)
  • Moreover, itopride has no affinity for the 5-HT4 receptors, unlike other benzamides such as cisapride and mosapride, which are 5-HT4 agonists. (wikipedia.org)
  • The affinity of cisapride for 5-HT4 receptors in the heart has been implicated in the undesirable cardiac effects of cisapride itself. (wikipedia.org)
  • functional
  • Identifying the currents and receptor mechanisms involved in depolarization of layer I interneurons is essential for understanding the functional role of these cells and their modulation by dopamine. (jneurosci.org)
  • The functional activity of LY-404,039 on mGluR receptors has been further demonstrated by investigating the drug's ability to suppress electrically stimulated excitatory postsynaptic potentials, or EPSPs. (wikipedia.org)
  • The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. (wikipedia.org)
  • Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
  • Parkinson's
  • The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, drug addiction and Parkinson's disease. (wikipedia.org)
  • Itopride may not be indicated for those suffering from Parkinson's disease or other conditions involving dopamine regulation issues. (wikipedia.org)
  • 2001
  • The desensitization of activated GPCRs is mediated by the phosphorylation of serine and threonine residues within the intracellular domains of receptors ( Ferguson, 2001 ). (jneurosci.org)
  • Although originally thought to mediate agonist-dependent (homologous) and agonist-independent (heterologous) forms of receptor desensitization, both GRKs and second messenger kinases are now believed to contribute to both forms of receptor desensitization in a more complex manner ( Ferguson, 2001 ). (jneurosci.org)
  • blockade
  • Using a whole-brain searchlight decoding approach we show that D2-receptor blockade enhances decoding of reward signals in the medial orbitofrontal cortex. (jneurosci.org)
  • These results suggest that D2-receptor blockade enhances content-specific representations in frontal cortex, presumably by a dopamine-mediated increase in pattern separation. (jneurosci.org)
  • Accordingly, blockade of D2-receptor activation should in turn enhance prefrontal representations by inhibiting potentially interfering concurrent representations ( Seamans and Yang, 2004 ). (jneurosci.org)
  • GPCRs
  • G protein-coupled receptors (GPCRs) are the largest receptor family and transmit the physiological effects of numerous biologically active molecules. (pnas.org)
  • The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). (wikipedia.org)
  • increases
  • Using whole-cell recording techniques in neocortical brain slices, we have examined how dopamine increases excitability of layer I interneurons in postnatal day 7-11 rats. (jneurosci.org)
  • It increases the release of dopamine as well as its metabolites DOPAC and HVA in the prefrontal cortex in a manner similar to the atypical antipsychotic clozapine. (wikipedia.org)
  • Dopamine increases the motivation for food cravings and appetite mediation. (wikipedia.org)
  • The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
  • rats
  • The discriminative stimulus effect of LSD in rats occurs in two phases, and these studies provide evidence that the later temporal phase is mediated by D 2 dopamine receptor stimulation. (springer.com)
  • By comparison, N-methyldopamine also had no effect in caudectomized mice at ≤ 150 mg/kg, and only a weak effect in nigral-lesioned rats at 25 mg/kg, although it was as effective as dopamine in stimulating cAMP in the adenylate cyclase assay. (wikipedia.org)
  • stimulation
  • This effect of NCS-1 was accompanied by an increase in D2 receptor-mediated cAMP inhibition after dopamine stimulation. (jneurosci.org)
  • In an assay based on the increase in heart rate (positive chronotropic response) produced by electrical stimulation of the post-ganglionic fibers of cat cardioaccelerator nerve, an i.v. dose of ~ 15 μg/kg DMDA caused a 50% reduction of the response, compared to an approximately 10% decrease produced by the same dose of dopamine. (wikipedia.org)
  • basal
  • The decrease in phospho-AKT levels, suggesting an increase in D2 dopamine receptor activity in basal conditions, was associated with an increase of AKT/PP2A complex, as revealed by co-immunoprecipitation experiments. (nih.gov)
  • regulate
  • In addition, A2A receptor can negatively regulate overreactive immune cells, thereby protecting tissues from collateral inflammatory damage. (wikipedia.org)
  • Moreover
  • Moreover, consistent with the cortical distribution of D2 receptors, post hoc analyses showed enhanced decoding of motor signals in motor cortex, but not of visual signals in visual cortex. (jneurosci.org)
  • mGluR2
  • The specific binding of LY-404,039 to human cloned mGlu receptors has been found to be highest for mGluR2 (Ki = 149 ± 11 nM) and relatively high for mGluR3 (Ki = 92 ± 14 nM). (wikipedia.org)
  • prolactin
  • Typically, itopride is indicated in the treatment of GI symptoms caused by reduced GI motility: dyspepsia of a non-ulcer/dysmotility type (gastric "fullness", discomfort, and possible pain) gastroparesis (delayed gastric emptying) anorexia heartburn regurgitation bloating nausea and vomiting other possible gastric, prolactin, or dopamine related conditions Itopride is typically taken three times a day. (wikipedia.org)
  • synaptic
  • The long form (D2Lh) has the "canonical" sequence and functions as a classic post-synaptic receptor. (wikipedia.org)
  • The short form (D2Sh) is pre-synaptic and functions as an autoreceptor that regulates the levels of dopamine in the synaptic cleft. (wikipedia.org)
  • protein-coupled receptor
  • His initial research as an assistant professor focused on structural neurobiology and immunology, combining chemistry, structural biology and protein chemistry with a specific biological interest in understanding how the G protein-coupled receptor (GPCR) superfamily works. (wikipedia.org)
  • ventral striatum
  • The four key structures are the midbrain dopamine system, the striatum (putamen, caudate nucleus, and ventral striatum), the amygdala (in the medial temporal lobe), and the orbitofrontal cortex (the cortex above the eyes). (dana.org)
  • blockade
  • Blockade of post-synaptic α2 receptors causes only minor corpus cavernosum smooth muscle relaxation, due to the fact that the majority of adrenoceptors in the corpus cavernosum are of the α1 type. (wikipedia.org)
  • novel
  • To investigate this hypothesis, we first assessed whether D2 dopaminergic modulation in mice affects novel object preference, a hippocampus-dependent task. (ufrn.br)
  • Subsequent novel human receptor structures include: 2012: The first structure of a lipid-activated GPCR, the sphingolipid, the human kappa-opioid receptor and the human nociceptin/orphanin FQ peptide. (wikipedia.org)
  • efficacy
  • Dopamine hyperactivity has been linked with alcohol withdrawal syndrome (AWS), suggesting that tiapride's antidopaminergic effects are the most likely mechanism for its clinical efficacy, although others believe some other mechanism might be involved. (wikipedia.org)
  • drug
  • Biased agonism of the AT1 receptor - Perspectives in drug discovery? (ece2013.org)
  • The sugar transporter receptor, i.e., "transceptor" GLUT2, may constitute a drug target to treat eating disorders and associated metabolic diseases, particularly by modulating its receptor function without affecting vital sugar provision by its transporter function. (physiology.org)
  • Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. (wikipedia.org)
  • effects
  • Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well. (wikipedia.org)
  • function
  • GLUT2 is a sugar transporter sustaining energy production in the cell, but it can also function as a receptor for extracellular glucose. (physiology.org)
  • However, the contribution of the receptor function over the transporter function of GLUT2 in the control of food intake remains to be determined. (physiology.org)
  • We define the function of rewards by their influence on the body, not by specific sensory receptors or by any external measure. (dana.org)
  • Disamping persiapan akademik, buy provigil in canada exercise reinstatement lexapro gum receptor fluid disease concern response kini ujian much presence function weight livingyou lexapro. (meta-u.com)