• One of the more notable drugs in the stimulant class is amphetamine, which acts as a dopamine and norepinephrine analog, reuptake inhibitor, as well as an agent that increases the amount of global catecholamine signaling throughout the nervous system by reversing transporters in the synapses. (wikipedia.org)
  • Drugs such as cocaine and methylphenidate act as reuptake inhibitors of norepinephrine, as do some antidepressants, such as those in the SNRI class. (wikipedia.org)
  • Adrenergic uptake inhibitors are drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. (mcw.edu)
  • Both stereoisomers of MDMA, MDA and MBDB were potent inhibitors of [3H]serotonin uptake into hippocampal synaptosomes, but only S-(+)-amphetamine produced an appreciable inhibition of [3H]serotonin uptake. (erowid.org)
  • Other antidepressants that inhibit serotonin uptake would also be expected to interact, such as serotonin-norepinephrine reuptake inhibitors and certain tricyclic antidepressants (eg, clomipramine, imipramine). (pharmacytimes.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)
  • Comparative safety of adding serotonin and norepinephrine reuptake inhibitors (SNRIs) versus nonsteroidal anti-inflammatory drugs (NSAIDs) to short-acting opioids for non-malignant pain in nursing homes. (medscape.com)
  • Pharmacological activity of the species derived from this irreversible norepinephrine uptake inhibitor. (aspetjournals.org)
  • The aziridinium ion was as potent as xylamine as an irreversible uptake inhibitor, and the effects of both compounds were sodium-dependent. (aspetjournals.org)
  • The dimer was a weak competitive inhibitor of norepinephrine uptake, with an IC50 of about 10 microM. (aspetjournals.org)
  • Pretreatment with the selective 5-HT uptake inhibitor fluoxetine, at a concentration which had no effect on baseline firing (20 microM), blocked the inhibitory effect of (+)-MDMA and PCA on dorsal raphe neurons. (erowid.org)
  • The selective norepinephrine uptake inhibitor desipramine (20 microM) was ineffective. (erowid.org)
  • Prozac is an SSRI, or a selective serotonin re-uptake inhibitor. (escapistmagazine.com)
  • H(2)(15)O]-Positron Emission Tomography (PET) was used to examine regional cerebral blood flow (rCBF) after administration of a single oral dose of the serotonin realeaser and uptake inhibitor MDMA (1.7 mg/kg) or placebo to 16 MDMA-naïve subjects. (researchgate.net)
  • The antidepressant mirtazapine is not considered an inhibitor of serotonin uptake (although it may cause release of serotonin), but in 1 study mirtazapine was associated with an increased risk of bleeding in patients taking warfarin. (pharmacytimes.com)
  • The level of neuronal uptake of norepinephrine in the pig pineal was 3.5+/-0.9 pmol/h/mg of wet tissue and represented about 77% of the total tissue radioactivity. (nel.edu)
  • Decreased adrenergic neuronal uptake activity in experimental right heart failure. (jci.org)
  • Despite its selective uptake by neuroendocrine tumors, mIBG accumulates in several normal tissues and leads to tissue-specific radiation toxicities. (aspetjournals.org)
  • Most of these are SSRIs (selective serotonin re-uptake inhibiters) given for depression and include Prozac, Zoloft, Paxil, Celexa and Lexapro. (edocr.com)
  • In contrast to the 5-fold stereoselectivity observed with amphetamine, only the S-(+) enantiomer of MDMA and 3,4-methylenedioxyamphetamine (MDA) inhibited [3H]dopamine uptake into striatal synaptosomes. (erowid.org)
  • Neither stereoisomer of the alpha-ethyl homolog of MDMA, N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), inhibited [3H]dopamine uptake. (erowid.org)
  • The rank order of affinities of MDMA at various brain receptors and uptake sites are as follows: 5-HT uptake greater than alpha 2-adrenoceptors = 5-HT2 serotonin = M-1 muscarinic = H-1 histamine greater than norepinephrine uptake = M-2 muscarinic = alpha 1-adrenoceptors = beta-adrenoceptors greater than or equal to dopamine uptake = 5-HT1 serotonin much greater than D-2 dopamine greater than D-1 dopamine. (erowid.org)
  • On the other side of the synapse are transporters, which re-uptake the dopamine so that it doesn't continue to just sit around the synapse, stimulating neurons endlessly. (escapistmagazine.com)
  • Emerging evidences suggest that the polyspecific organic cation transporters play important roles in systemic disposition and tissue-specific uptake of mIBG. (aspetjournals.org)
  • Norepinephrine transporter, organic cation transporters, and multidrug and toxin extrusion proteins play differential roles in tumor targeting, systemic elimination, and accumulation in normal tissues. (aspetjournals.org)
  • Development of 3-Phenyltropane Analogues with High Affinity for the Dopamine and Serotonin Transporters and Low Affinity for the Norepinephrine Transporter. (acs.org)
  • Effects of synthetic cathinones on inhibition of uptake (upper panels) and stimulation of release (lower panels) at dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters in rat brain synaptosomes. (aspetjournals.org)
  • However, recent evidence suggests that excessive adrenergic stimulation may not produce myocardial beta-receptor downregulation unless there is an additional defect in the local norepinephrine (NE) uptake mechanism. (jci.org)
  • desflurane increases toxicity of norepinephrine by Mechanism: unknown. (medscape.com)
  • Although the mechanism has not been established, it has been proposed that the ability of SSRIs to inhibit the uptake of serotonin into platelets inhibits the ability of platelets to aggregate. (pharmacytimes.com)
  • Both amphetamine and cocaine increase norepinephrine (NE) via stimulation of release and inhibition of reuptake, respectively. (nih.gov)
  • Since the pharmacology of MDMA is largely uncharacterized, the stereochemical profiles of MDMA and some of its homologs were derived on inhibition of synaptosomal uptake of [3H]monoamines and compared to those of amphetamine and the hallucinogenic phenylisopropylamine 2,5-dimethoxy-4-methylamphetamine (DOM). (erowid.org)
  • The two stereoisomers of amphetamine and the MDMA-related compounds were equipotent in inhibiting [3H]norepinephrine uptake into hypothalamic synaptosomes. (erowid.org)
  • Theoretically, SSRIs and other drugs that inhibit serotonin uptake would increase the risk of bleeding when combined with other anticoagulants, but little information is available. (pharmacytimes.com)
  • While the conversion of tyrosine to dopamine occurs predominantly in the cytoplasm, the conversion of dopamine to norepinephrine by dopamine β-monooxygenase occurs predominantly inside neurotransmitter vesicles. (wikipedia.org)
  • Norepinephrine is synthesized from tyrosine as a precursor, and packed into synaptic vesicles. (wikidoc.org)
  • Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. (wikipedia.org)
  • The name "noradrenaline" (from Latin ad, "near", and ren, "kidney") is more commonly used in the United Kingdom, whereas "norepinephrine" (from Ancient Greek ἐπῐ́ (epí), "upon", and νεφρός (nephrós), "kidney") is usually preferred in the United States. (wikipedia.org)
  • Norepinephrine ( INN ) (abbreviated norepi or NE ) or noradrenaline ( BAN ) (abbreviated NA or NAd ) is a catecholamine with multiple roles including as a hormone and a neurotransmitter . (wikidoc.org)
  • In the rest of the body, norepinephrine increases heart rate and blood pressure, triggers the release of glucose from energy stores, increases blood flow to skeletal muscle, reduces blood flow to the gastrointestinal system, and inhibits voiding of the bladder and gastrointestinal motility. (wikipedia.org)
  • Xylamine (N-2'-chloroethyl-N-ethyl-2-methylbenzylamine), a nitrogen mustard that irreversibly inhibits norepinephrine uptake, cyclizes in solution to form an aziridinium ion. (aspetjournals.org)
  • Neither stereoisomer of DOM inhibited synaptosomal uptake of any [3H]monoamine. (erowid.org)
  • The natural stereoisomer is L -(−)-( R )-norepinephrine. (wikidoc.org)
  • MDMA exhibited negligible affinities (greater than 500 microM) at opioid (mu, delta and kappa), central-type benzodiazepine, and corticotropin-releasing factor receptors, and at choline uptake sites and calcium channels. (erowid.org)
  • It performs its action by being released into the synaptic cleft, where it acts on adrenergic receptors, followed by the signal termination, either by degradation of norepinephrine, or by uptake by surrounding cells. (wikidoc.org)
  • Maternal odor learning occurs using a simple learning circuit including robust olfactory bulb norepinephrine (NE), release from the locus ceruleus (LC), and amygdala suppression by low corticosterone (CORT). (diva-portal.org)
  • Norepinephrine can also suppress neuroinflammation when released diffusely in the brain from the locus ceruleus . (wikidoc.org)
  • mIBG enters cancer cells through the norepinephrine transporter (NET) where the radioactive decay of 131 I causes DNA damage, cell death, and tumor necrosis. (aspetjournals.org)
  • In particular, human organic cation transporter 2 (hOCT2) and multidrug and toxin extrusion proteins 1 and 2-K (hMATE1/2-K) likely mediate renal secretion of mIBG, whereas hOCT1 and hOCT3 may contribute to mIBG uptake into normal tissues such as the liver, salivary glands, and heart. (aspetjournals.org)
  • Transporter-mediated uptake has been exploited successfully in nuclear medicine to deliver several radiopharmaceuticals for cancer imaging and treatment ( Zhang and Wang, 2020 ). (aspetjournals.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)
  • Norepinephrine release is lowest during sleep, rises during wakefulness, and reaches much higher levels during situations of stress or danger, in the so-called fight-or-flight response. (wikipedia.org)
  • Norepinephrine attenuates hypoxia-inhibited thyrotropin-releasing hormone release in median eminence and paraventricular nucleus of rat hypothalamus. (nel.edu)
  • Uptake and depolarization-evoked release of (3)H-norepinephrine were investigated in vitro using pieces of the pig pineals. (nel.edu)
  • Specific antagonists and agonists of alpha(2)-adrenoceptors were employed for the characterization of alpha(2)-adrenoceptors involved in the autoregulation of depolarization-evoked release of norepinephrine in the pig pineal. (nel.edu)
  • Regardless of how and where it is released, norepinephrine acts on target cells by binding to and activating adrenergic receptors located on the cell surface. (wikipedia.org)
  • 80% V̇ o 2max ) causes a seven- to eightfold increase in glucose production ( R a ) and a fourfold increase in glucose uptake ( R d ), resulting in hyperglycemia, whereas moderate exercise (ME) causes both to double. (diabetesjournals.org)
  • Norepinephrine is released when a host of physiological changes are activated by a stressful event. (wikidoc.org)
  • These results demonstrate that the aziridinium ion is responsible for xylamine's uptake blocking activity and that the other xylamine derivatives do not influence this action. (aspetjournals.org)
  • The aziridinium ion, its hydrolysis product, and the dimer were synthesized to evaluate directly their effects on norepinephrine uptake in rabbit thoracic aorta. (aspetjournals.org)
  • This study presented the effects of hypoxia on TRH secretion in rat hypothalamus, and the norepinephrine (NE) involvement in the modulation of TRH secretion during acute hypoxia exposure. (nel.edu)
  • Norepinephrine" is also the international nonproprietary name given to the drug. (wikipedia.org)
  • Hence, a major goal in cancer drug development and therapy is to increase tumor-specific drug uptake while reducing uptake into normal tissues to minimize toxicities. (aspetjournals.org)
  • Norepinephrine uptake dependent upon apparent Mg++-ATPase activity and proton transport in storage vesicles in axoplasm. (nih.gov)
  • To investigate the association between beta-adrenoceptor regulation and NE uptake activity, we carried out studies in 30 dogs with right heart failure (RHF) produced by tricuspid avulsion and progressive pulmonary artery constriction and 23 sham-operated control dogs. (jci.org)
  • Compared with sham-operated dogs, RHF dogs showed a 26% decrease in beta-adrenoceptor density, a 51% reduction in NE uptake activity, and a 57% decrease in NE uptake-1 carrier density in their right ventricles. (jci.org)
  • In addition, right ventricle beta-receptor density correlated significantly with NE uptake activity and NE uptake-1 carrier density. (jci.org)