PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 24081522-1 2014 The human noradrenaline transporter (NET) and 5-hydroxytryptamine (5-HT) transporter (SERT) are inhibited by antidepressants and psychoactive drugs such as cocaine. Cocaine 156-163 solute carrier family 6 member 2 Homo sapiens 10-35 23583454-4 2013 3,4-Methylenedioxypyrovalerone and naphyrone had high affinity for radioligand binding sites on recombinant human dopamine (hDAT), serotonin (hSERT) and norepinephrine (hNET) transporters, potently inhibited [3H]neurotransmitter uptake, and, like cocaine, did not induce transporter-mediated release. Cocaine 247-254 solute carrier family 6 member 2 Homo sapiens 169-173 21420984-0 2011 Interaction of tyrosine 151 in norepinephrine transporter with the 2beta group of cocaine analog RTI-113. Cocaine 82-89 solute carrier family 6 member 2 Homo sapiens 31-57 21420984-1 2011 Cocaine binds and inhibits dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 55-81 21498515-0 2011 Cocaine up-regulation of the norepinephrine transporter requires threonine 30 phosphorylation by p38 mitogen-activated protein kinase. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 29-55 21498515-12 2011 Mutational analysis of serine and threonine residues revealed that substitution of threonine 30, located at the amino terminus of hNET with alanine (T30A-hNET), abolished cocaine-induced up-regulation of NET function, surface expression, and phosphorylation. Cocaine 171-178 solute carrier family 6 member 2 Homo sapiens 130-134 21498515-12 2011 Mutational analysis of serine and threonine residues revealed that substitution of threonine 30, located at the amino terminus of hNET with alanine (T30A-hNET), abolished cocaine-induced up-regulation of NET function, surface expression, and phosphorylation. Cocaine 171-178 solute carrier family 6 member 2 Homo sapiens 154-158 21498515-12 2011 Mutational analysis of serine and threonine residues revealed that substitution of threonine 30, located at the amino terminus of hNET with alanine (T30A-hNET), abolished cocaine-induced up-regulation of NET function, surface expression, and phosphorylation. Cocaine 171-178 solute carrier family 6 member 2 Homo sapiens 131-134 21498515-14 2011 These studies identify a novel molecular mechanism that cocaine-activated p38 MAPK-mediated phosphorylation of NET-T30 dictates surface NET availability, and hence, NE transport. Cocaine 56-63 solute carrier family 6 member 2 Homo sapiens 111-114 21498515-14 2011 These studies identify a novel molecular mechanism that cocaine-activated p38 MAPK-mediated phosphorylation of NET-T30 dictates surface NET availability, and hence, NE transport. Cocaine 56-63 solute carrier family 6 member 2 Homo sapiens 136-139 21498515-2 2011 Cocaine binds NET and modulates NE transport. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 14-17 21498515-6 2011 Acute intra-peritoneal injections of cocaine (20 mg/kg body weight) to rats resulted in increased NE uptake by prefrontal cortex (PFC) synaptosomes with a parallel increase in the surface expression of endogenous NET. Cocaine 37-44 solute carrier family 6 member 2 Homo sapiens 213-216 21498515-8 2011 In vitro cocaine (30-50 muM) treatment of rat PFC synaptosomes increased native NET function, surface expression, and phosphorylation in a manner sensitive to p38 MAPK inhibition by PD169316. Cocaine 9-16 solute carrier family 6 member 2 Homo sapiens 80-83 21498515-9 2011 We next examined cocaine-elicited effects on wild-type human NET (hNET) expressed heterologously in human placental trophoblast cells to gain more insights into the mechanisms involved. Cocaine 17-24 solute carrier family 6 member 2 Homo sapiens 61-64 21498515-9 2011 We next examined cocaine-elicited effects on wild-type human NET (hNET) expressed heterologously in human placental trophoblast cells to gain more insights into the mechanisms involved. Cocaine 17-24 solute carrier family 6 member 2 Homo sapiens 66-70 21498515-10 2011 Cocaine treatment of hNET expressing human placental trophoblast cells up-regulated the function, surface expression, and phosphorylation of hNET in a PD169316-sensitive manner. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 21-25 21498515-10 2011 Cocaine treatment of hNET expressing human placental trophoblast cells up-regulated the function, surface expression, and phosphorylation of hNET in a PD169316-sensitive manner. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 141-145 21498515-11 2011 In addition, cocaine inhibited constitutive endocytosis of hNET. Cocaine 13-20 solute carrier family 6 member 2 Homo sapiens 59-63 20932493-8 2011 The serotonin transporter and the norepinephrine transporter are expressed on the maternal-facing side of the syncytiotrophoblast, thus exposed to the inhibitory actions of cocaine and amphetamines if present in maternal blood. Cocaine 173-180 solute carrier family 6 member 2 Homo sapiens 34-60 21149640-1 2011 The human dopamine and norepinephrine transporters (hDAT and hNET, respectively) control neurotransmitter levels within the synaptic cleft and are the site of action for amphetamine (AMPH) and cocaine. Cocaine 193-200 solute carrier family 6 member 2 Homo sapiens 61-65 20352074-6 2010 The compound displaced binding of radiolabeled cocaine analogs at all three MATs, usually with nanomolar K(i) values and within two fold of cocaine"s affinity at the norepinephrine transporter. Cocaine 47-54 solute carrier family 6 member 2 Homo sapiens 166-192 20352074-6 2010 The compound displaced binding of radiolabeled cocaine analogs at all three MATs, usually with nanomolar K(i) values and within two fold of cocaine"s affinity at the norepinephrine transporter. Cocaine 140-147 solute carrier family 6 member 2 Homo sapiens 166-192 19728366-0 2010 PET imaging of the effects of age and cocaine on the norepinephrine transporter in the human brain using (S,S)-[(11)C]O-methylreboxetine and HRRT. Cocaine 38-45 solute carrier family 6 member 2 Homo sapiens 53-79 15757904-1 2005 The human norepinephrine (NE) transporter (hNET) attenuates neuronal signaling by rapid NE clearance from the synaptic cleft, and NET is a target for cocaine and amphetamines as well as therapeutics for depression, obsessive-compulsive disorder, and post-traumatic stress disorder. Cocaine 150-157 solute carrier family 6 member 2 Homo sapiens 43-47 17141753-10 2007 The hN120C mutant caused an 11-fold increase in the binding affinity of cocaine, compared to the wild-type hNET, while hQ118C, hY119C, hR121C and hE122C showed smaller increases. Cocaine 72-79 solute carrier family 6 member 2 Homo sapiens 107-111 16515684-14 2006 CONCLUSION: The current and previous studies support the following conclusions: 1) cocaine blocks all 3 monoamine transporters at similar concentrations; 2) methylphenidate inhibits DAT and NET well but a 1000-fold higher concentration of the drug is required to inhibit SERT; 3) Amphetamine and methamphetamine are most potent at NET, while being 5- to 9-fold less potent at DAT, and 200- to 500-fold less potent at SERT; 4) MDMA has moderately higher apparent affinity for SERT and NET than for DAT. Cocaine 83-90 solute carrier family 6 member 2 Homo sapiens 331-334 16289633-1 2006 The norepinephrine (NE) transporter (NET) mediates the removal of NE from synaptic spaces and is a major target for antidepressants, amphetamine and cocaine. Cocaine 149-156 solute carrier family 6 member 2 Homo sapiens 37-40 16092934-10 2005 The results suggest that this region of hNET is important for interactions with antidepressants and cocaine, but it is probably not involved in substrate translocation mechanisms. Cocaine 100-107 solute carrier family 6 member 2 Homo sapiens 40-44 16515684-14 2006 CONCLUSION: The current and previous studies support the following conclusions: 1) cocaine blocks all 3 monoamine transporters at similar concentrations; 2) methylphenidate inhibits DAT and NET well but a 1000-fold higher concentration of the drug is required to inhibit SERT; 3) Amphetamine and methamphetamine are most potent at NET, while being 5- to 9-fold less potent at DAT, and 200- to 500-fold less potent at SERT; 4) MDMA has moderately higher apparent affinity for SERT and NET than for DAT. Cocaine 83-90 solute carrier family 6 member 2 Homo sapiens 190-193 16515684-14 2006 CONCLUSION: The current and previous studies support the following conclusions: 1) cocaine blocks all 3 monoamine transporters at similar concentrations; 2) methylphenidate inhibits DAT and NET well but a 1000-fold higher concentration of the drug is required to inhibit SERT; 3) Amphetamine and methamphetamine are most potent at NET, while being 5- to 9-fold less potent at DAT, and 200- to 500-fold less potent at SERT; 4) MDMA has moderately higher apparent affinity for SERT and NET than for DAT. Cocaine 83-90 solute carrier family 6 member 2 Homo sapiens 331-334 15757904-1 2005 The human norepinephrine (NE) transporter (hNET) attenuates neuronal signaling by rapid NE clearance from the synaptic cleft, and NET is a target for cocaine and amphetamines as well as therapeutics for depression, obsessive-compulsive disorder, and post-traumatic stress disorder. Cocaine 150-157 solute carrier family 6 member 2 Homo sapiens 44-47 15763139-2 2005 The cocaine and tricyclic antidepressant-sensitive NET belongs to a family of sodium and chloride coupled transporters that include the monoamines dopamine and serotonin and the amino acids GABA and glycine. Cocaine 4-11 solute carrier family 6 member 2 Homo sapiens 51-54 15763139-8 2005 Chronic exposure to cocaine upregulated NET protein expression and [3H]nisoxetine binding sites in the insular cortex from brains of cocaine addicts. Cocaine 20-27 solute carrier family 6 member 2 Homo sapiens 40-43 15763140-1 2005 Binding assays for the norepinephrine (NE) transporter (NET) with [3H]nisoxetine have generally yielded weak potencies for compounds related to cocaine and 1-(2-(di(4-fluorophenyl)-methoxy)-ethyl)-4-(3-phenylpropyl)piperazine (GBR 12909), as compared with their functional activity in inhibiting NE uptake. Cocaine 144-151 solute carrier family 6 member 2 Homo sapiens 56-59 12837768-0 2003 chi-Conopeptide MrIA partially overlaps desipramine and cocaine binding sites on the human norepinephrine transporter. Cocaine 56-63 solute carrier family 6 member 2 Homo sapiens 91-117 12499385-7 2003 We show that ASP(+) (4-(4-(dimethylamino)styrl)-N-methylpyridinium) has micromolar potency for the human norepinephrine transporter, that ASP(+) accumulation is Na(+)-, Cl(-)-, cocaine-, and desipramine-sensitive and temperature-dependent, and that ASP(+) competes with norepinephrine uptake. Cocaine 177-184 solute carrier family 6 member 2 Homo sapiens 105-131 11875370-3 2002 Compared to the wild-type hNET, the Ala(457)Pro variant exhibited a five-fold higher affinity for cocaine, but a two-fold lower affinity for the NET inhibitor nisoxetine, and an unchanged affinity for the antidepressant desipramine. Cocaine 98-105 solute carrier family 6 member 2 Homo sapiens 27-30 11396611-9 2001 Using these methods, Na-dependent, NE+-induced hNET currents that are blocked by cocaine and antidepressants, channel modes of NE+ conduction, voltage-dependent uptake coupled to NE+-induced ion channel activity, PKC (phosphokinase C) regulation of NE+ uptake, and transporter modulation by [Ca2+]i have all been discovered. Cocaine 81-88 solute carrier family 6 member 2 Homo sapiens 47-51 11223167-7 2001 Also discovered was a novel exon 5 splice variant of NET that displayed very low levels of transport and did not bind cocaine. Cocaine 118-125 solute carrier family 6 member 2 Homo sapiens 53-56 11082428-10 2000 Cocaine and amphetamine have distinctly different effects on NET expression after continuous exposure. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 61-64 11082428-0 2000 Regulation of the human norepinephrine transporter by cocaine and amphetamine. Cocaine 54-61 solute carrier family 6 member 2 Homo sapiens 24-50 9852563-0 1998 Cocaine acts as an apparent competitive inhibitor at the outward-facing conformation of the human norepinephrine transporter: kinetic analysis of inward and outward transport. Cocaine 0-7 solute carrier family 6 member 2 Homo sapiens 98-124 9074537-10 1997 CONCLUSION: PET imaging with 11C-hydroxyephedrine permits quantitative assessment of cardiac norepinephrine transporter function in active chronic cocaine users. Cocaine 147-154 solute carrier family 6 member 2 Homo sapiens 93-119 9681456-0 1998 Voltammetric studies on mechanisms of dopamine efflux in the presence of substrates and cocaine from cells expressing human norepinephrine transporter. Cocaine 88-95 solute carrier family 6 member 2 Homo sapiens 124-150 9092590-12 1997 fET-mediated transport of catecholamines is sensitive to cocaine and tricyclic antidepressants, with antagonist potencies significantly correlated with hNET inhibitor sensitivity. Cocaine 57-64 solute carrier family 6 member 2 Homo sapiens 152-156 9030630-1 1997 The norepinephrine transporter (NET) is a site of action for tricyclic antidepressant drugs and for drugs of abuse such as amphetamine and cocaine. Cocaine 139-146 solute carrier family 6 member 2 Homo sapiens 4-30 9030630-1 1997 The norepinephrine transporter (NET) is a site of action for tricyclic antidepressant drugs and for drugs of abuse such as amphetamine and cocaine. Cocaine 139-146 solute carrier family 6 member 2 Homo sapiens 32-35 7500004-1 1995 Transport of norepinephrine (NE+) by cocaine- and antidepressant-sensitive transporters in presynaptic terminals is predicted to involve the cotransport of Na+ and Cl-, resulting in a net movement of charge per transport cycle. Cocaine 37-44 solute carrier family 6 member 2 Homo sapiens 184-187 8710929-6 1996 These events are stimulated by NE and by guanethidine, an hNET substrate, and they are blocked by cocaine and the antidepressant desipramine. Cocaine 98-105 solute carrier family 6 member 2 Homo sapiens 58-62 8700133-1 1996 The role of N-glycosylation in the expression, stability, and ligand recognition by the cocaine- and antidepressant-sensitive human norepinephrine transporter (hNET) was assessed in stably and transiently transfected cell lines. Cocaine 88-95 solute carrier family 6 member 2 Homo sapiens 132-158 8700133-1 1996 The role of N-glycosylation in the expression, stability, and ligand recognition by the cocaine- and antidepressant-sensitive human norepinephrine transporter (hNET) was assessed in stably and transiently transfected cell lines. Cocaine 88-95 solute carrier family 6 member 2 Homo sapiens 160-164 8218295-0 1993 Sodium- and chloride-dependent, cocaine-sensitive, high-affinity binding of nisoxetine to the human placental norepinephrine transporter. Cocaine 32-39 solute carrier family 6 member 2 Homo sapiens 110-136 7886020-2 1994 Currently available models describing the pathogenesis of these effects focus on the involvement of cocaine target systems, primarily the noradrenaline transporter, in the mother and the fetus. Cocaine 100-107 solute carrier family 6 member 2 Homo sapiens 138-163 7823027-7 1994 Electrophysiological recording of human NETs and SERTs stably expressed in HEK-293 cells reveals that both transporters move charge across the plasma membrane following the addition of substrates; these currents can be blocked by NET-and SERT-selective antagonists as well as by cocaine. Cocaine 279-286 solute carrier family 6 member 2 Homo sapiens 40-43