• 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)
  • gene
  • Rats with lesions of the nigrostriatal dopamine pathway caused by 6-hydroxydopamine (6-OHDA) serve as a model for Parkinson's disease and show alterations in gene expression in the two major output systems of the striatum to the globus pallidus and substantia nigra. (sciencemag.org)
  • These changes are taken as evidence of D 2 receptor-mediated suppression of neural activity and gene transcription. (jneurosci.org)
  • It is now known to be located in the coding region of the ANKK1 gene which controls the synthesis of dopamine in the brain. (wikipedia.org)
  • clarification needed] More recent studies show an interaction between friendships and the dopamine receptor (DRD4) gene that is associated with political ideology. (wikipedia.org)
  • The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. (wikipedia.org)
  • quinpirole
  • As it appears to improve mood, we examined its actions in rodent models of antidepressant properties, in comparison with the prototypical anti-Parkinson agent, apomorphine, the D2/D3 receptor agonist, quinpirole, and the antidepressants, imipramine and fluvoxamine. (biopsychiatry.com)
  • Paradoxically, neither the D 1 -like receptor agonist 6-chloro-2,3,4,5-tetrahydro-1-phenyl-1 H -3-benzazepine hydrobromide ( SKF81297 ) (1-10 μ m ) nor the D 2 -like agonist quinpirole (10 μ m ) produced a significant depolarization. (jneurosci.org)
  • Parkinson's
  • Severe movement disorders result from the loss of striatal dopamine in patients with Parkinson's disease. (sciencemag.org)
  • 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)
  • 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)
  • stimulation
  • This effect of NCS-1 was accompanied by an increase in D2 receptor-mediated cAMP inhibition after dopamine stimulation. (jneurosci.org)
  • 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)
  • Rather, D 2 receptor stimulation mobilizes intracellular Ca 2+ stores via G β γ activation of a phospholipase Cβ1 pathway, leading to a calcineurin-dependent reduction in L-type currents. (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)
  • From these and other related observations, the researchers concluded that DMDA was a potent inhibitor of the adrenergic system via stimulation of inhibitory putative (at that time) dopamine receptors on adrenergic nerve terminals. (wikipedia.org)
  • heteromers
  • 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)
  • 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)
  • 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)
  • rats
  • 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)
  • kinase
  • This G-protein coupled receptor is Gs/a coupled and indirectly activates cyclic AMP-dependent protein kinase, stimulating the neuron. (wikipedia.org)
  • Abundant extracellular adenosine can then bind to the A2A receptor resulting in a Gs-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e. (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)
  • regulate
  • In addition, A2A receptor can negatively regulate overreactive immune cells, thereby protecting tissues from collateral inflammatory damage. (wikipedia.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)
  • adrenergic
  • 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)
  • cortical
  • 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)
  • dihydrexidine
  • Dihydrexidine and adrogolide (ABT-431) (a prodrug of A-86929 with improved bioavailability) are the only selective, centrally active D1-like receptor agonists that have been studied clinically in humans. (wikipedia.org)