• neurotransmission
  • Reuptake inhibitors of neurotransmitters have a direct effect on extracellular concentrations of neurotransmitters in the synapses, and therefore influence neurotransmission. (axonmedchem.com)
  • This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. (wikipedia.org)
  • The idea that there must be specific transport proteins associated with the uptake of monoamines and acetylcholine into vesicles developed due to the discovery of specific inhibitors which interfered with monoamine neurotransmission and also depleted monoamines in neuroendocrine tissues. (wikipedia.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)
  • Tyramine can also be converted into octopamine by the dopamine-beta-hydroxylase (DBH) which itself acts as a false transmitter by displacing noradrenaline from its vesicle but not activating the postsynaptic alpha adrenoreceptor. (wikipedia.org)
  • extracellular
  • 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)
  • The major function of the plasma membrane dopamine transporter (DAT) is the rapid uptake of released DA into presynaptic nerve terminals leading to control of both the extracellular levels of DA and the intracellular stores of DA. (jneurosci.org)
  • These results suggest that considerable extracellular diffusion of dopamine in the prelimbic PFC may result, at least in part, from a paucity of DAT content in mesocortical dopamine axons, as well as a distribution of the DAT protein at a distance from synaptic release sites. (jneurosci.org)
  • The dopamine transporter (DAT) is a crucial protein in the regulation of dopamine transmission, serving to remove dopamine from the extracellular space after its release. (jneurosci.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)
  • terminals
  • 3 H]1-methyl-4-phenylpyridinium (MPP + ) was used to assess release from dopamine (DA) and norepinephrine nerve terminals, whereas [ 3 H]5-hydroxytryptamine (5-HT) was used to assess release from 5-HT nerve terminals. (aspetjournals.org)
  • VMAT2
  • 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)
  • 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)
  • 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)
  • neurotransmitters
  • The main function of these transporters is to help terminate the action of neurotransmitters released via exocytosis in response to nerve impulses. (aspetjournals.org)
  • There is growing evidence that a large number of well known exogenous chemicals work as substitute neurotransmitters, though the distinction between the classical model and the substitute neurotransmitter model only becomes apparent with neurotransmitters central to the signaling in the conscious brain, like dopamine and serotonin (as mentioned above). (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)
  • Rats
  • Systemic administration of relatively high doses of indirect- and direct-acting dopamine agonists can produce highly repetitive movements in laboratory rats, mice and cavies. (aspetjournals.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)