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  • 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)
  • 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
  • Bromocriptine (originally marketed as Parlodel, subsequently under many names) is an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes. (wikipedia.org)
  • 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)
  • 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)
  • antiparkinsonian
  • 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)
  • Ligands
  • Unlike most other D2 receptor ligands, piquindone displays Na2+-dependent binding, a property it shares with tropapride, zetidoline, and metoclopramide. (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)
  • bromocriptine
  • Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine). (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • acute
  • In sharp contrast to the observations in the Str, in the NAc, acute administration of cocaine or D1 agonist significantly increased P-CREB and P-ERK2 in PSAL mice, a response that was not evident in PCOC mice. (frontiersin.org)
  • knockout
  • For example, low-density lipoprotein-receptor knockout mice lacking leptin (LDLR −/− ob/ob ) develop more atherosclerotic lesions than LDLR −/− control mice. (ahajournals.org)