• analogs
  • Affinity of the analogs for the [³H]DTBZ binding site did not correlate with inhibitory potency in the [³H]DA uptake assay. (sigmaaldrich.com)
  • All of the analogs, except for the N -methyl-substituted compounds, showed increased inhibitory potency against 3 H-(−)-2-β-carbomethoxy-3-β-(4-fluorophenyl)tropane 1,5-naphthalenedisulfonate ([ 3 H]WIN 35,428) ([ 3 H]WIN) binding to the dopamine transporter, compared with TMP. (aspetjournals.org)
  • neuronal
  • Objectives The purpose of this study was to elucidate whether the neuronal noradrenaline reuptake transporter (uptake 1 ) undergoes age-dependent regulation in the human heart. (onlinejacc.org)
  • However, in the synaptic cleft, action of noradrenaline at the receptors is terminated by reuptake into sympathetic nerve terminals through the neuronal uptake 1 transporter (10,11) . (onlinejacc.org)
  • In fact, there is indirect evidence that, with aging, neuronal uptake of noradrenaline declines (6,12) . (onlinejacc.org)
  • However, direct measurements of neuronal uptake 1 sites and neuronal uptake 1 activity in aging human hearts are missing. (onlinejacc.org)
  • We have recently shown that, in rat cardiac membranes, ( 3 H)-nisoxetine binding and, in rat cardiac tissue slices, assessment of ( 3 H)-noradrenaline accumulation can be used to identify sites that have characteristics of the cardiac neuronal uptake 1 transporter (13) . (onlinejacc.org)
  • drugs
  • Drugs that block dopamine uptake often function as positive reinforcers but can differ along the dimension of strength or effectiveness as a positive reinforcer. (aspetjournals.org)
  • This common stereotypic effect engendered by the indirect-acting dopamine agonists is consistent with the common spectrum of other behavioral effects generally observed with these drugs. (aspetjournals.org)
  • Many DRIs such as cocaine are drugs of abuse due to the rewarding effects evoked by elevated synaptic concentrations of dopamine in the brain. (wikipedia.org)
  • Unlike other similar drugs, GYKI-52895 is a selective dopamine reuptake inhibitor, which presumably would produce stimulant effects in vivo. (wikipedia.org)
  • Monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants (TCAs) were the first drugs to be developed for the treatment of depression, dating back to the early 1950s. (wikipedia.org)
  • Because monoamine oxidase inhibitors can have serious pharmacodynamic interactions with other drugs and with foodstuffs that contain tyramine, relatively few patients are treated with this class of antidepressant, which can be especially effective in many patients. (aspetjournals.org)
  • serotonin and norepinephrine
  • Consistent with the in vitro data and behavioral effects, peripheral administration of PRC200-SS (5 and 10 mg/kg i.p.) significantly increased extracellular levels of serotonin and norepinephrine in the medial prefrontal cortex, and of serotonin and dopamine in the core of nucleus accumbens, with reduction of levels of 3,4-dihydroxyphenylacetic acid, homovanillic acid, and 5-hydroxyindoleacetic acid compared with levels for saline control. (aspetjournals.org)
  • noradrenaline
  • To test this hypothesis, BTS 74 398 was administered in combination with selective dopamine, 5-HT, and noradrenaline receptor antagonists. (aspetjournals.org)
  • The interaction among noradrenaline, 5-HT, and dopamine in the control of motor behavior is complex. (aspetjournals.org)
  • Methods We determined uptake 1 density (by [ 3 H]-nisoxetine binding to membranes) and activity (by accumulation of [ 3 H]-noradrenaline into tissue slices) in the right atria (RA) of 42 patients (age range 3 months to 76 years) undergoing open-heart surgery without apparent heart failure. (onlinejacc.org)
  • Thus, an age-dependent reduction in activity of this transporter would also lead to prolonged action of noradrenaline at beta-adrenoceptors and could thus contribute to cardiac beta-adrenoceptor desensitization with aging. (onlinejacc.org)
  • Dopamine is a biological precursor to noradrenaline. (wikipedia.org)
  • nucleus accumbens
  • In vivo microdialysis experiments compared the effects of the full substrates [(±)-1-(2-naphthyl)propan-2-amine (PAL-287) and ( S )- N -methyl-1-(2-naphthyl)propan-2-amine (PAL-1046)], to that of a partial DAT/5-HT transporter substrate [( S )- N -ethyl-1-(2-naphthyl)propan-2-amine (PAL-1045)] on extracellular DA and 5-HT in the nucleus accumbens of the rat. (aspetjournals.org)
  • vivo
  • These results add to a small but growing literature that demonstrates differences in the in vitro and in vivo pharmacological effects of indirect dopamine agonists. (aspetjournals.org)
  • Furthermore, the process of aggregate formation is ultimately associated with degeneration Inhibitors,research,lifescience,medical of mammalian cells.8 Analysis of in vitro and in vivo model systems support the hypothesis that glutamine repeat disorders, like Alzheimer's disease and Parkinson's disease, are caused by an aggregation-based pathogenetic mechanism. (thrombininhibitors.com)
  • VMAT2
  • It has been found that these inhibitors are less effective at inhibiting VMAT1 than VMAT2, and the inhibitory effects of the tetrabenazines on VMAT1 is negligible. (wikipedia.org)
  • Introduction of aromatic substituents in lobelane maintained analog affinity for the [³H]DTBZ binding site on VMAT2 and inhibitory potency in the [³H]DA uptake assay assessing VMAT2 function. (sigmaaldrich.com)
  • VMAT2 is believed to possess at least two distinct binding sites, which are characterized by tetrabenazine (TBZ) and reserpine binding to the transporter. (wikipedia.org)
  • If VMAT2 function is inhibited or compromised, monoamine neurotransmitters such as dopamine cannot be released into the synapse via typical release mechanisms (i.e., exocytosis resulting from action potentials). (wikipedia.org)
  • assays
  • Biogenic amine transporter release assays were carried out in rat brain synaptosomes and followed published procedures. (aspetjournals.org)
  • The in vitro release assays demonstrated that partial substrate activity occurs at all three transporters. (aspetjournals.org)
  • it produces the same effects as SoRI-20040 and SoRI-9804 in uptake assays and binding assays, inhibiting the re-uptake of dopamine, but does not modulate d-amphetamine-induced DA release by inhibiting that as well, like 'agonists' of the series do. (wikipedia.org)
  • Subsequently, human VMATs were cloned using human cDNA libraries with the rat homologs as probes, and heterologous-cell amine uptake assays were performed to verify transport properties. (wikipedia.org)
  • pharmacological effects
  • The ability of agonists of γ-aminobutyric acid A (GABA A ) receptors to enhance stereotyped gnawing was used as a method for dissociating the pharmacological effects of indirect-acting dopamine agonists. (aspetjournals.org)
  • GYKI-52,466, another 2,3-benzodiazepine with other than GABAergic function Tifluadom Lufuradom Benzodiazepine Substituted methylenedioxyphenethylamine Horváth K, Szabó H, Pátfalusi M, Berzsenyi P, Andrási F. Pharmacological Effects of GYKI 52895, a New Selective Dopamine Uptake Inhibitor. (wikipedia.org)