• rats
  • A series of phenolic hydroxy-2-aminotetralins with either a primary or a tertiary (N,N-di-n-propylated) amino group was investigated on electrically evoked acetylcholine release from striatal slices of reserpinized rats, a dopamine (DA) D2 receptor model. (aspetjournals.org)
  • N-methyl-D-aspartate receptor blockade differentially modifies regional cerebral metabolic responses to D1 and D2 dopamine agonists in rats with a unilateral 6-hydroxydopamine lesion. (semanticscholar.org)
  • The 2-deoxyglucose autoradiographic technique was used to examine the effect of N-methyl-D-aspartate receptor blockade on regional cerebral metabolic responses to D1 and D2 dopamine receptor stimulation in rats with a unilateral 6-hydroxydopamine lesion of the nigrostriatal pathway. (semanticscholar.org)
  • We have previously reported that two D1 dopamine agonists, SKF 82958 and SKF 77434, are readily self-administered by rats. (biomedsearch.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)
  • full agonists
  • It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies, but its high potency and long duration of action causes D1 receptor downregulation and tachyphylaxis, and unlike other D1 full agonists such as SKF-82,958, it does not produce place preference in animals. (wikipedia.org)
  • adrenergic
  • It also is an α2-adrenergic agonist. (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)
  • Rotigotine possesses the following in vitro receptor binding profile: All affinities listed were assayed using human materials except that for α2B-adrenergic which was done with NG 108-15 cells. (wikipedia.org)
  • Ligands
  • Takasu H, Gardella TJ, Luck MD, et al (1999) Amino-terminal modifications of human parathyroid hormone (PTH) selectively alter phospholipase C signaling via the type 1 PTH receptor: implications for design of signal-specific PTH ligands. (springer.com)
  • Unlike most other D2 receptor ligands, piquindone displays Na2+-dependent binding, a property it shares with tropapride, zetidoline, and metoclopramide. (wikipedia.org)
  • subtypes
  • Differences between the effects of the compounds at the two DA receptor subtypes concerned the N,N-dipropyl substitution which influenced the D2 activity much more pronouncedly, and an added 6-OH group (i.e., a catechol function), which seemed to be of foremost importance at the D1 site. (aspetjournals.org)
  • These results suggest two similar major binding sites for the DA receptor subtypes, but differences with respect to additional binding sites. (aspetjournals.org)
  • Dopamine receptor agonist, selective for subtypes D2 and D3. (wikipedia.org)
  • derivative
  • Piribedil (trade names Pronoran, Trivastal Retard, Trastal, Trivastan, Clarium and others) is an antiparkinsonian agent and piperazine derivative which acts as a D2 and D3 receptor agonist. (wikipedia.org)
  • 1996
  • Laugwitz KL, Allgeier A, Offermanns S, et al (1996) The human thyrotropin receptor: a heptahelical receptor capable of stimulating members of all four G protein families. (springer.com)
  • Sagan S, Chassaing G, Pradier L, et al (1996) Tachykinin peptides affect differently the second messenger pathways after binding to CHO-expressed human NK-1 receptors. (springer.com)
  • pharmacological
  • In recent years, biased agonists as well as pharmacological chaperones have demonstrated the potential to harness G protein-coupled receptor signaling and trafficking and have collectively opened new possibilities in G protein-coupled receptor drug discovery. (springer.com)
  • Combining pharmacological chaperoning and biased agonism properties into a unique given molecule would be of high therapeutic interest in many human diseases resulting from G protein-coupled receptor mutation and misfolding. (springer.com)
  • Cell-permeable pharmacological chaperones have been successfully challenged to restore plasma membrane localization of the receptor mutants and to rescue their function. (springer.com)
  • Because of its structural relationship to dopamine, DMDA has been the subject of a number of pharmacological investigations. (wikipedia.org)
  • mGlu
  • LY-404,039 has been shown to modulate glutamatergic activity in the limbic and forebrain areas, where group II mGlu receptors are most densely localized. (wikipedia.org)
  • 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)
  • neuronal
  • On the other hand, the preservation of D1-mediated rotational behavior and reduced lateral habenula glucose metabolism in the presence of MK-801 despite attenuation of the effects of the D1 agonist in entopeduncular nucleus and substantia nigra pars reticulata suggests that D1 receptor-regulated neuronal pathways exhibit varying degrees of sensitivity to N-methyl-D-aspartate receptor blockade. (semanticscholar.org)
  • prefrontal
  • In order to understand the effects of prefrontal DA release on neural activity, first let us consider DA receptors and the anatomy of DA-ergic terminals in PFC. (frontiersin.org)
  • Yet other definitions are based on its biochemical projections: the prefrontal cortex is that which receives dopamine (DA) through mesocortical projections. (springer.com)
  • caused by regional depletion of dopamine in prefrontal cortex of rhesus monkey. (springer.com)
  • 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)
  • functional
  • 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)
  • In functional studies however, rotigotine behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50). (wikipedia.org)
  • assay
  • In this assay, a drug was classed as "dopamine-like" if the vasoldilation it produced was not prevented by β-blocking drugs, and did not occur if the drug was injected into the femoral artery. (wikipedia.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)
  • In the dog, an i.v. dose of 16 μg/kg caused an ~ 80% decrease in heart rate in the same cardioaccelerator nerve assay, compared to an ~ 8% decrease produced by dopamine. (wikipedia.org)
  • intracellular
  • What intracellular enzyme is linked to the extracellular insulin receptor? (brainscape.com)
  • In most of the cases, it is associated with inactivating mutations of the renal arginine vasopressin V2 receptor leading to misfolding and intracellular retention of the receptor, causing the inability of patients to concentrate their urine in response to the antidiuretic hormone. (springer.com)
  • Inhibition
  • The concept underlying this putative therapy is the inhibition of the generation of the prolactin fragment by substrate depletion, i.e., the inhibition of pituitary prolactin secretion by activation of dopamine D2 receptors in lactotropes. (frontiersin.org)
  • treatment
  • Dopamine agonist treatment of anterograde amnesia from mediobasal forebrain injury. (springer.com)
  • These compounds, and particularly small-molecule-biased agonists which only trigger the V2-induced Gs protein-dependent signaling pathway, represent a potential therapeutic treatment of this X-linked genetic pathology. (springer.com)
  • Rotigotine (Neupro) is a dopamine agonist of the non-ergoline class of medications indicated for the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS). (wikipedia.org)
  • stimulation
  • These findings indicate that D1 and D2 receptor-associated brain mechanisms are differentially influenced by N-methyl-D-aspartate receptor stimulation. (semanticscholar.org)
  • D2-mediated behavioral and cerebral metabolic responses appear to require concurrent N-methyl-D-aspartate receptor stimulation. (semanticscholar.org)
  • LY-404,039 has been shown to act as a potent full agonist at group II mGluRs as demonstrated by its ability to inhibit cyclic adenosine monophosphate, cAMP, formation as a result of stimulation by forskolin. (wikipedia.org)
  • 2002
  • Holloway AC, Qian H, Pipolo L, et al (2002) Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors. (springer.com)
  • regulate
  • 1 Leptin has a variety of important central and peripheral actions to regulate energy balance and metabolism, fertility, and bone metabolism that are mediated by specific cell surface leptin receptors. (ahajournals.org)
  • anticholinergic
  • It also reduces motion sickness and has antiemetic (Histamine H1 receptors but it does not block the production of histamine) and anticholinergic properties. (wikipedia.org)
  • release
  • alcohol makes dopamine release, yes it does, you're loosened up but at the same time hyped up, usually on harder alcohol. (dr-bob.org)
  • but when it leaves the system, your sedated and GABA more in place, the dopamine release is the first couple hours, when it leaves the system your sedated. (dr-bob.org)