CocaineTransporterAntagonistsNeuronsSelectiveStriatal dopamine releaseReceptorReuptakeNeuronal uptakeInhibitionMonoamine oxidase iReceptorsSerotonin and dopamineMetabolismMechanismVivoBehaviorExtracellularSynaptosomesMechanismsNeurotransmitterNucleus AccumbensPretreatmentTransportersSynapticMAOIsPerfusionCompoundsMDMADynamicsSpontaneousReleaseDoseIncreasesPsychiatric
Cocaine8
- Troparil is a few times more potent than cocaine as a dopamine reuptake inhibitor, but is less potent as a serotonin reuptake inhibitor, and has a duration spanning a few times longer, since the phenyl ring is directly connected to the tropane ring through a non-hydrolyzable carbon-carbon bond. (wikipedia.org)
- Dopamine and corticotropin-releasing factor synergistically alter basolateral amygdala-to-medial prefrontal cortex synaptic transmission: functional switch after chronic cocaine administration. (rush.edu)
- IRP and international researchers led by Amy Hauck Newman, Ph.D. , discovered that R-modafinil, like cocaine, inhibits dopamine uptake, but binds to the dopamine transporter in a unique fashion that may not result in the same addictive response as cocaine. (nih.gov)
- Behavioral responses to a D1 dopamine agonist in weanling rats treated neonatally with cocaine and delta9-tetrahydrocannabinol. (umassmed.edu)
- Excited Delirium typically accompanies the use of stimulants, most commonly but not limited to cocaine and methamphetamines, as these drugs block the re-uptake of dopamine, resulting in elevation of dopamine levels in the brain. (spiritofautism.org)
- Our current research is focused on understanding neurochemical, behavioral and molecular differences among typical and atypical blockers of the membrane dopamine transporter that can lead to pharmacotherapeutics for the treatment of cocaine and other psychostimulant use disorders. (nih.gov)
- Many psychostimulants, like cocaine, inhibit the dopamine transporter (DAT), which is largely thought to account for actions related to their misuse and dependence. (nih.gov)
- Cocaine-like, typical DAT inhibitors preferentially bind DAT in an outward-facing conformation, while atypical DAT inhibitors, like modafinil, prefer a more inward-facing DAT conformation. (nih.gov)
Transporter13
- This, in addition to the fact that perfusion of the probe with a low Ca(2+) medium inhibited the MDMA-induced increase in extracellular dopamine, indicates that the neurotransmitter may be released by a Ca(2+) -dependent mechanism not related to the dopamine transporter. (erowid.org)
- The data also indicate that the free radical formation is probably not associated with the MDMA-induced dopamine release and that MDMA does not induce dopamine release via an action at the dopamine transporter. (erowid.org)
- In low micromolar concentrations, BPB, U-73122 and nordihydroguaiaretic acid, but not aspirin and indomethacin, inhibited uptake of [3H]DA into striatal synaptosomes and binding of [3H]mazindol to the DA transporter. (aspetjournals.org)
- To test this hypothesis, we administered systemic injections of saline or GBR-12909, a selective dopamine transporter (DAT) inhibitor, to monkeys and assessed their novelty seeking behavior during a probabilistic decision making task. (nih.gov)
- Troparil is used in scientific research into the dopamine reuptake transporter. (wikipedia.org)
- Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4′-halophenyl)nortropanes: Candidate Radioligands for In Vivo Imaging of the Brain Dopamine Transporter with Positron Emission Tomography. (acs.org)
- Development of 3-Phenyltropane Analogues with High Affinity for the Dopamine and Serotonin Transporters and Low Affinity for the Norepinephrine Transporter. (acs.org)
- We also confirmed that the release induced by these compounds was prevented by selective transporter inhibitors (indalpine or nomifensine). (erowid.org)
- The inhibitory effect of methiothepin was not due to its effects as a transporter inhibitor or Ca(2+)-channel blocker and is unlikely to be due to its antagonist properties on 5-HT1/2, dopamine or any other extracellular receptor. (erowid.org)
- Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1, 2, 3, 6-tetrahydro-pyridin-4-yl)-1H-indoles. (google.nl)
- This drug blocks the dopamine transporter and the norepinephrine transporter , leading to elevated dopamine and norepinephrine ranges with the inhibition of their reuptake. (girlscoutstotem.org)
- Theorized that action may be related to mediation through the reversible inhibition of vesicular monoamine transporter 2 (VMAT2), a transporter that decreases uptake of monoamines (eg, dopamine, serotonin, norepinephrine, histamine) into synaptic vesicles and depletes monoamine stores from nerve terminals. (medscape.com)
- Depletes neurotransmitter stores of dopamine, serotonin, and noradrenaline within nerve cells in the brain, thereby altering transmission of electric signals from the brain that control movement by reversibly inhibiting vesicular monoamine transporter 2 (VMAT2). (medscape.com)
Antagonists3
- Glutamate antagonists selective for hyperpolarizing bipolar cells, such as 2,3-piperidine dicarboxylic acid (PDA), caused dose- and calcium-dependent release of dopamine from the retina. (tmc.edu)
- In our body, Adrenergic Agents include: adrenergic agonists and antagonists and agents that affect the synthesis, storage, uptake, metabolism, or release of adrenergic transmitters. (wellnessadvocate.com)
- therefore, an adequate trial with this medication is reasonable before using dopamine antagonists. (medscape.com)
Neurons3
- The idea that dopamine modulates novelty seeking is supported by evidence that novel stimuli excite dopamine neurons and activate brain regions receiving dopaminergic input. (nih.gov)
- Progressive loss of nigrostriatal dopamine (DA) neurons is the neuropathological hallmark of Parkinson's disease (PD). (jneurosci.org)
- Intrastriatal transplantation of foetal midbrain dopamine (DA) neurons ameliorates the fundamental symptoms of dopaminergic denervation in clinical and experimental parkinsonism despite providing only restricted reinnervation. (ox.ac.uk)
Selective5
- Selective serotonin reuptake inhibitors (SSRIs) are some of the most commonly prescribed antidepressants available. (moviecultists.com)
- Prozac is the brand name of the drug fluoxetine , a selective serotonin reuptake inhibitor (SSRI). (moviecultists.com)
- Selective YAP/TAZ inhibition in fibroblasts via dopamine receptor D1 agonism reverses fibrosis. (harvard.edu)
- GBR 12935 dihydrochloride is a potent and selective inhibitor of dopamine uptake. (lancrix.com)
- In a study utilizing purified synaptosomes from rat brain, Tianeptine was reported to enhance serotonin uptake in selective brain regions. (multinpharma.com)
Striatal dopamine release2
- MDMA (30 mg/kg, i.p.), given three times at 3-h intervals, produced a rapid increase in striatal dopamine release measured by in vivo microdialysis (maximum increase to 380 +/- 64% of baseline). (erowid.org)
- Inhibitors of arachidonic acid metabolism: effects on rat striatal dopamine release and uptake. (aspetjournals.org)
Receptor6
- The purpose of this study was to investigate the possibility that arachidonic acid metabolites mediate D-2 dopamine (DA) receptor inhibition of striatal DA release. (aspetjournals.org)
- Pharmacologic neuroimaging of the ontogeny of dopamine receptor function. (harvard.edu)
- p-OHA-induced PPI disruptions were also improved by a serotonin (5-HT)2A receptor antagonist, a 5-HT synthesis inhibitor or a 5-HT neurotoxin. (bvsalud.org)
- Treatment with the dopamine receptor agonist, apomorphine, or the dopamine-releasing drug, amphetamine, produced significant disruption of PPI in control mice but not in ACE knockout mice. (unboundmedicine.com)
- The role of other dopamine-receptor subtypes is currently unclear. (medscape.com)
- It binds to receptor sites on motor nerve terminals, and after uptake it inhibits the release of acetylcholine, blocking transmission of impulses in neuromuscular tissue. (medscape.com)
Reuptake6
- These data demonstrate that dopamine enhances novelty-driven value and imply that excessive novelty seeking-characteristic of impulsivity and behavioral addictions-might be caused by increases in dopamine, stemming from less reuptake. (nih.gov)
- Troparil is a phenyltropane-based dopamine reuptake inhibitor (DRI) that is derived from methylecgonidine. (wikipedia.org)
- Objective: Solriamfetol (formerly JZP-110), a dopamine/norepinephrine reuptake inhibitor, is approved in the US to improve wakefulness in adults with excessive daytime sleepiness associated with narcolepsy (75-150 mg/d) or obstructive sleep apnea (37.5-150 mg/d). (elsevierpure.com)
- They may also have a weak effect on norepinephrine and dopamine neuronal reuptake. (medscape.com)
- Sertraline selectively inhibits presynaptic serotonin reuptake with minimal or no effect on the reuptake of norepinephrine or dopamine. (medscape.com)
- TCAs are potent inhibitors of serotonin and norepinephrine reuptake. (genelabs.com)
Neuronal uptake2
- SSRIs inhibit central nervous system (CNS) neuronal uptake of serotonin (5HT). (medscape.com)
- The active ingredient is "Bupropion" a weak inhibitor of the neuronal uptake of dopamine, serotonin and norepinephrine. (thegreenieonthelake.com)
Inhibition1
- However, the results also suggest that certain inhibitors of arachidonic acid metabolism are relatively potent DA uptake blockers/releasers and that this action is unrelated to their inhibition of enzymes in the arachidonic acid cascade. (aspetjournals.org)
Monoamine oxidase i2
- Lexapro is not considered a monoamine oxidase inhibitor (MAOI). (moviecultists.com)
- Amoxapine is not a monoamine oxidase inhibitor. (genelabs.com)
Receptors3
- In our body, Dopamine Agents (Dopaminergic Agents) , as a neurotransmitter (or a neurotransmitter agent) , are exogenous neurotransmitter substances used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of the dopaminergic neurons. (wellnessadvocate.com)
- In animals, amoxapine reduced the uptake of nor-epinephirine and serotonin and blocked the response of dopamine receptors to dopamine. (genelabs.com)
- In order for a dopamine agonist to offer clinical benefit, it must stimulate D2 receptors. (medscape.com)
Serotonin and dopamine3
- The two most commonly identified culprits are serotonin and dopamine. (madinamerica.com)
- An enzyme called monoamine oxidase is involved in removing the neurotransmitters norepinephrine, serotonin and dopamine from the brain . (moviecultists.com)
- MAOIs work by slowing down the breakdown of serotonin and dopamine, another chemical in your brain. (moviecultists.com)
Metabolism1
- by preventing peripheral metabolism, it increases the concentration of dopamine in the central nervous system (CNS). (medscape.com)
Mechanism2
- The mechanism underlying 5-hydroxytryptamine (5-HT) and/or dopamine release induced by (+)-amphetamine ((+)-Amph), 3,4-methylendioxymethamphetamine (MDMA), p-chloroamphetamine (pCA) and (+)-fenfluramine ((+)-Fen) was investigated in rat brain superfused synaptosomes preloaded with the 3H neurotransmitters. (erowid.org)
- It is a weak dopamine uptake inhibitor, though the exact mechanism for its stimulating effects remains unknown. (girlscoutstotem.org)
Vivo1
- sc-201146) uptake in vitro and in vivo. (multinpharma.com)
Behavior3
- In addition, dopamine is shown to drive exploratory behavior in novel environments. (nih.gov)
- According to the JEMS website, elevated levels of dopamine cause agitation, paranoia and violent behavior. (spiritofautism.org)
- We are currently characterizing the effects of modafinil, its enantiomers and several newly synthetized structural analogs of modafinil, alone and in combination with addictive psychostimulants on dopamine dynamics, via neuro-electrochemistry procedures, and on reward-related behavior in rodents. (nih.gov)
Extracellular2
- Lack of extracellular Ca2+ did not alter uptake mechanisms nor did it modify the carrier-dependent dopamine-induced [3H]-dopamine release. (erowid.org)
- First, during repeated depolarization at a physiological firing frequency, when net extracellular concentrations reflect DA release versus uptake, ambient levels of extracellular DA within the graft are restored to normal. (ox.ac.uk)
Synaptosomes1
- The Ca(2+)-dependent release is mediated by Ca(2+)-influx (mainly through P-type Ca(2+)-channels), possibly triggered by the drug interacting with an unknown intracellular target, affected by methiothepin, common to both 5-HT and dopamine synaptosomes. (erowid.org)
Mechanisms1
- The present study examined the mechanisms by which 3,4- methylenedioxymethamphetamine (MDMA) produces long-term neurotoxicity of striatal dopamine neurones in mice and the protective action of the dopamine uptake inhibitor GBR 12909. (erowid.org)
Neurotransmitter1
- Apparently, so the story goes, depression is caused by an imbalance of the neurotransmitter serotonin and schizophrenia is caused by an imbalance of dopamine. (madinamerica.com)
Nucleus Accumbens1
- In this work, we employ fast scan cyclic voltammetry (FSCV) to probe nucleus accumbens shell (NAS) dopamine (DA) dynamics in C57BL/6 male and female mice. (nih.gov)
Pretreatment2
- This effect was prevented by a pretreatment with a dopamine (DA) uptake inhibitor. (bvsalud.org)
- Pretreatment with the ACE inhibitor, captopril, which itself did not affect PPI, caused a reduction in the effect of apomorphine on PPI, similar to that seen in the ACE knockout mice. (unboundmedicine.com)
Transporters1
- 3H-radiolabelled forms of troparil have been used in humans and animals to map the distribution of dopamine transporters in the brain. (wikipedia.org)
Synaptic1
- This ends in increased dopamine ranges on the synaptic cleft, and hence the consequences of dopamine turn out to be amplified. (girlscoutstotem.org)
MAOIs5
- Monoamine oxidase inhibitors (MAOIs) are a separate class from other antidepressants , treating different forms of depression and other nervous system disorders such as panic disorder, social phobia, and depression with atypical features. (moviecultists.com)
- Although SSRIs are the current frontline treatment for depression, MAOIs (monoamine oxidase inhibitors) were the first antidepressants developed. (moviecultists.com)
- Monoamine oxidase inhibitors (MAOIs) are an extremely strong class of antidepressants that treat depression by preventing the breakdown of the brain chemicals serotonin, dopamine, and norepinephrine. (moviecultists.com)
- SSRIs are second-generation antidepressants, which means they are newer than first-generation medications such as monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants (TCAs). (moviecultists.com)
- Monoamine Oxidase Inhibitors (MAOIs): Do not use MAOIs intended to treat psychiatric disorders with bupropion hydrochloride extended-release tablets (XL) or within 14 days of stopping treatment with bupropion hydrochloride extended-release tablets (XL). (nih.gov)
Perfusion1
Compounds2
- 3. [3H]-5HT and/or [3H]-dopamine release induced by all these compounds was partially (31-80%), but significantly Ca(2+)-dependent. (erowid.org)
- Monoamine oxidase (MAO) inhibitors are a class of one such naturally occurring compounds that have been clinically developed as an antidepressant and as a treatment for social anxiety and Parkinson's disease (Youdim et al. (moviecultists.com)
MDMA2
- This increase was enhanced to 576 +/- 109% of baseline by GBR 12909 (10 mg/kg, i.p.) administered 30 min before each dose of MDMA, supporting the contention that MDMA enters the terminal by diffusion and not via the dopamine uptake site. (erowid.org)
- These data suggest that MDMA-induced toxicity of dopamine neurones in mice results from free radical formation which in turn induces an oxidative stress process. (erowid.org)
Dynamics1
Spontaneous2
- U-73122 (10 microM), another phospholipase A2 inhibitor, decreased evoked overflow of DA, did not affect the action of N-0437 but also increased spontaneous outflow of DA. (aspetjournals.org)
- In slices prelabeled with [3H]DA, exposure to BPB, U-73122 and nordihydroguaiaretic acid (a lipoxygenase inhibitor) significantly increased spontaneous outflow of tritium whereas the cyclooxygenase inhibitors aspirin and indomethacin did not. (aspetjournals.org)
Release6
- 4. Methiothepin inhibited the Ca(2+)-dependent component of (+)-Amph-induced [3H]-dopamine release with high potency (70 nM), as previously found with (+)-Fen-induced [3H]-5-HT release. (erowid.org)
- The retinal circuitry underlying the release of dopamine was examined in the turtle, Pseudemys scripta elegans, using neurochemical release studies, anatomical techniques, and biochemistry. (tmc.edu)
- This indicated that dopamine release was tonically inhibited by GABA. (tmc.edu)
- This indicated that depolarizing bipolar cells were not involved in retinal circuitry underlying the release of dopamine in the turtle retina. (tmc.edu)
- The cells capable of the release of dopamine were identified using both uptake autoradiography and immunocytochemical localization with dopamine antisera. (tmc.edu)
- This drug is an acetylcholine release inhibitor and neuromuscular blocking agent. (medscape.com)
Dose1
- Patients with dopamine-responsive dystonia (DRD) typically experience marked, long-term benefit with low-dose levodopa. (medscape.com)
Increases2
Psychiatric1
- This is amplified if the person already has a pre-existing psychiatric condition that is treated with dopamine re-uptake inhibitors. (spiritofautism.org)