PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 7681602-2 1993 The brain 5HT transporter appears to be a principal site of action of therapeutic antidepressants and may mediate behavioral and/or toxic effects of cocaine and amphetamines. Cocaine 149-156 solute carrier family 6 member 4 Homo sapiens 10-25 34798166-0 2022 Methylation of the serotonin transporter gene moderates the depressive subjective effect of cocaine. Cocaine 92-99 solute carrier family 6 member 4 Homo sapiens 19-40 8450469-8 1993 These findings suggest that, although seizure initiation may depend primarily on affinity of cocaine and related compounds for binding sites associated with the serotonin transporter, the seizure-inducing properties of cocaine may ultimately depend on a final summation of its effects not only on serotonergic systems, but on muscarinic and sigma neuronal systems as well. Cocaine 93-100 solute carrier family 6 member 4 Homo sapiens 161-182 1896028-0 1991 Binding of the cocaine analog 2 beta-[3H] carboxymethoxy-3 beta-(4-fluorophenyl)tropane to the serotonin transporter. Cocaine 15-22 solute carrier family 6 member 4 Homo sapiens 95-116 1896028-7 1991 These results suggest that [3H]CFT and cocaine bind to the serotonin transporter at a site close to but distinct from the antidepressant binding site. Cocaine 39-46 solute carrier family 6 member 4 Homo sapiens 59-80 2308472-7 1990 In general, our results indicate that unique structural requirements exist for each transporter site, but that cocaine binding at norepinephrine and dopamine transporters can be described by more similar structure-activity relationships than those found for the serotonin transporter. Cocaine 111-118 solute carrier family 6 member 4 Homo sapiens 262-283 34798166-1 2022 Genetic variation in the serotonin transporter (SLC6A4) has been shown to moderate the acute subjective effects of cocaine. Cocaine 115-122 solute carrier family 6 member 4 Homo sapiens 48-54 34798166-3 2022 In this study, methylation of the SLC6A4 gene was investigated in the moderation of the subjective effects of cocaine. Cocaine 110-117 solute carrier family 6 member 4 Homo sapiens 34-40 34798166-8 2022 Participants with SLC6A4 hypermethylation reported greater subjective response to cocaine for "depressed" relative to participants with SLC6A4 hypomethylation (experiment-wise p =.002). Cocaine 82-89 solute carrier family 6 member 4 Homo sapiens 18-24 34798166-9 2022 These findings indicate that SLC6A4 methylation moderates the "depressed" subjective effect of cocaine in non-treatment-seeking cocaine-dependent participants. Cocaine 95-102 solute carrier family 6 member 4 Homo sapiens 29-35 34798166-9 2022 These findings indicate that SLC6A4 methylation moderates the "depressed" subjective effect of cocaine in non-treatment-seeking cocaine-dependent participants. Cocaine 128-135 solute carrier family 6 member 4 Homo sapiens 29-35 34798166-1 2022 Genetic variation in the serotonin transporter (SLC6A4) has been shown to moderate the acute subjective effects of cocaine. Cocaine 115-122 solute carrier family 6 member 4 Homo sapiens 25-46 25873594-1 2015 The membrane transporters for the monoamines serotonin (SERT) and dopamine (DAT) are prominent targets of various psychoactive substances, including competitive inhibitors, such as tricyclic antidepressants, methylphenidate, and cocaine. Cocaine 229-236 solute carrier family 6 member 4 Homo sapiens 45-54 34199621-3 2021 We previously identified a novel allosteric site in the DAT and the related human serotonin transporter that lies outside the central orthosteric substrate- and cocaine-binding pocket. Cocaine 161-168 solute carrier family 6 member 4 Homo sapiens 82-103 6443374-0 1984 Platelet serotonin transporter in cocaine patients. Cocaine 34-41 solute carrier family 6 member 4 Homo sapiens 9-30 33658787-0 2021 Association of Serotonin Transporter (SERT) Polymorphisms with Opioid Dependence and Dimensional Aspects of Cocaine Use in a Caucasian Cohort of Opioid Users. Cocaine 108-115 solute carrier family 6 member 4 Homo sapiens 15-36 33658787-0 2021 Association of Serotonin Transporter (SERT) Polymorphisms with Opioid Dependence and Dimensional Aspects of Cocaine Use in a Caucasian Cohort of Opioid Users. Cocaine 108-115 solute carrier family 6 member 4 Homo sapiens 38-42 33658787-4 2021 We hypothesize that SLC6A4 variants are associated with cocaine exposure in subjects with an opioid dependence diagnosis (OD), and also in non-dependent opioid users (NOD). Cocaine 56-63 solute carrier family 6 member 4 Homo sapiens 20-26 33658787-10 2021 A nominally significant association was identified with the [SL+SS] genotype of SLC6A4 and cocaine KMSK scores >="cutpoint" for a cocaine dependence diagnosis (p=0.026). Cocaine 91-98 solute carrier family 6 member 4 Homo sapiens 80-86 33658787-13 2021 Conclusion: The functional SERT promoter tandem repeat genotype may be associated to heavy cocaine exposure and more rapid escalation of cocaine use, in persons with and without opioid dependence diagnosis. Cocaine 91-98 solute carrier family 6 member 4 Homo sapiens 27-31 33658787-13 2021 Conclusion: The functional SERT promoter tandem repeat genotype may be associated to heavy cocaine exposure and more rapid escalation of cocaine use, in persons with and without opioid dependence diagnosis. Cocaine 137-144 solute carrier family 6 member 4 Homo sapiens 27-31 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 125-132 solute carrier family 6 member 4 Homo sapiens 247-268 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 125-132 solute carrier family 6 member 4 Homo sapiens 270-274 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 125-132 solute carrier family 6 member 4 Homo sapiens 270-274 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 194-215 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 217-221 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 247-268 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 270-274 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 270-274 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 194-215 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 217-221 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 247-268 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 270-274 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 270-274 31570504-2 2019 SERT is the target for many antidepressant medications as well as psychostimulants such as cocaine and ecstasy (3,4-methylenedioxymethamphetamine). Cocaine 91-98 solute carrier family 6 member 4 Homo sapiens 0-4 30680295-9 2019 Herein, we describe the implementation of the same using recordings obtained from HEK293 cells stably expressing the human serotonin transporter (SERT), which were challenged with the inhibitor cocaine. Cocaine 194-201 solute carrier family 6 member 4 Homo sapiens 123-144 30680295-9 2019 Herein, we describe the implementation of the same using recordings obtained from HEK293 cells stably expressing the human serotonin transporter (SERT), which were challenged with the inhibitor cocaine. Cocaine 194-201 solute carrier family 6 member 4 Homo sapiens 146-150 27140629-5 2016 Using membranes from HeLa cells expressing SERT and intact rat basophilic leukemia cells, we show that agents such as Na(+) and cocaine that stabilize outward-open conformations of SERT decreased phosphorylation and agents that stabilize inward-open conformations (e.g., 5-HT, ibogaine) increased phosphorylation. Cocaine 128-135 solute carrier family 6 member 4 Homo sapiens 43-47 33785354-11 2021 Compared to cocaine, they showed comparable potency inhibiting uptake at DAT and higher potency at SERT. Cocaine 12-19 solute carrier family 6 member 4 Homo sapiens 99-103 33888022-7 2021 Amphetamine and cocaine"s IC50 and EC50 on DAT and SERT determined by this method were consistent with previous reports. Cocaine 16-23 solute carrier family 6 member 4 Homo sapiens 51-55 32494974-0 2020 Serotonin transporter protein in autopsied brain of chronic users of cocaine. Cocaine 69-76 solute carrier family 6 member 4 Homo sapiens 0-21 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 125-132 solute carrier family 6 member 4 Homo sapiens 194-215 32494974-1 2020 RATIONALE: The long-held speculation that the brain serotonin system mediates some behavioral effects of the psychostimulant cocaine is supported in part by the high affinity of cocaine for the serotonin transporter (SERT) and by reports that the serotonin transporter (SERT), estimated by SERT binding, is increased in brain of human chronic cocaine users. Cocaine 125-132 solute carrier family 6 member 4 Homo sapiens 217-221 29357981-1 2018 BACKGROUND: Reduced expression of the serotonin transporter (SERT) promotes anxiety and cocaine intake in both humans and rats. Cocaine 88-95 solute carrier family 6 member 4 Homo sapiens 38-59 29357981-1 2018 BACKGROUND: Reduced expression of the serotonin transporter (SERT) promotes anxiety and cocaine intake in both humans and rats. Cocaine 88-95 solute carrier family 6 member 4 Homo sapiens 61-65 28590957-0 2017 Genetic moderation of cocaine subjective effects by variation in the TPH1, TPH2, and SLC6A4 serotonin genes. Cocaine 22-29 solute carrier family 6 member 4 Homo sapiens 85-91 28590957-1 2017 OBJECTIVE: This study investigated variants of tryptophan hydroxylase (TPH)1, TPH2, and SLC6A4 in the moderation of the subjective effects of cocaine. Cocaine 142-149 solute carrier family 6 member 4 Homo sapiens 88-94 28590957-10 2017 CONCLUSION: These findings indicate that TPH1, TPH2, and SLC6A4 variants moderate the subjective effects of cocaine in non-treatment-seeking cocaine-dependent participants. Cocaine 108-115 solute carrier family 6 member 4 Homo sapiens 57-63 28590957-10 2017 CONCLUSION: These findings indicate that TPH1, TPH2, and SLC6A4 variants moderate the subjective effects of cocaine in non-treatment-seeking cocaine-dependent participants. Cocaine 141-148 solute carrier family 6 member 4 Homo sapiens 57-63 26110342-0 2015 Serotonin transporter gene promoter polymorphism predicts relationship between years of cocaine use and impulsivity. Cocaine 88-95 solute carrier family 6 member 4 Homo sapiens 0-21 25873594-1 2015 The membrane transporters for the monoamines serotonin (SERT) and dopamine (DAT) are prominent targets of various psychoactive substances, including competitive inhibitors, such as tricyclic antidepressants, methylphenidate, and cocaine. Cocaine 229-236 solute carrier family 6 member 4 Homo sapiens 56-60 25873594-5 2015 We exemplify our approach by measuring the kinetics of cocaine, methylphenidate, and desipramine binding to SERT and DAT. Cocaine 55-62 solute carrier family 6 member 4 Homo sapiens 108-112 24973209-10 2014 The sorting pattern was further confirmed by visualizing internalization of SERT using the fluorescent cocaine analog JHC1-64 and by reversible and pulse-chase biotinylation assays showing evidence for lysosomal degradation of the internalized transporter. Cocaine 103-110 solute carrier family 6 member 4 Homo sapiens 76-80 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 4 Homo sapiens 86-90 23518607-1 2013 A number of studies have reported associations between the serotonin transporter gene (SLC6A4) and alcohol, heroin, cocaine, or methamphetamine abuse. Cocaine 116-123 solute carrier family 6 member 4 Homo sapiens 87-93 23518607-1 2013 A number of studies have reported associations between the serotonin transporter gene (SLC6A4) and alcohol, heroin, cocaine, or methamphetamine abuse. Cocaine 116-123 solute carrier family 6 member 4 Homo sapiens 59-80 24120036-1 2013 We genotyped the LPR and VNTR polymorphisms of the serotonin transporter gene in 504 cocaine-dependent patients and 508 controls. Cocaine 85-92 solute carrier family 6 member 4 Homo sapiens 51-72 21309950-0 2012 The SLC6A4 VNTR genotype determines transcription factor binding and epigenetic variation of this gene in response to cocaine in vitro. Cocaine 118-125 solute carrier family 6 member 4 Homo sapiens 4-10 23706649-0 2013 Thermostabilisation of the serotonin transporter in a cocaine-bound conformation. Cocaine 54-61 solute carrier family 6 member 4 Homo sapiens 27-48 23706649-7 2013 Inhibitor binding assays showed that both of the thermostabilised SERT mutants bound [(125)I]RTI55 (beta-CIT) with affinity similar to that of the wild-type transporter, although cocaine bound with increased affinity (17- to 56-fold) whilst ibogaine, imipramine and paroxetine all bound with lower affinity (up to 90-fold). Cocaine 179-186 solute carrier family 6 member 4 Homo sapiens 66-70 23776432-1 2013 The competitive inhibitor cocaine and the non-competitive inhibitor ibogaine induce different conformational states of the human serotonin transporter. Cocaine 26-33 solute carrier family 6 member 4 Homo sapiens 129-150 22925276-4 2012 Cocaine-positive urines dropped from 78% to 54% for the disulfiram group and from 77% to 76% for the placebo group among the 5-HTTLPR S" allele carriers (F = 16.2; df = 1,301; P < 0.0001). Cocaine 0-7 solute carrier family 6 member 4 Homo sapiens 125-133 21309950-1 2012 We demonstrated that the genotype of the variable number tandem repeats (VNTRs) in the linked polymorphic region (LPR) of the 5" promoter and in the intron 2 (Stin2) transcriptional regulatory domains of the serotonin transporter SLC6A4 gene determined its promoter interactions with transcription factors and co-activators in response to cocaine in the JAr cell line. Cocaine 339-346 solute carrier family 6 member 4 Homo sapiens 230-236 21309950-5 2012 Concurrently, cocaine increased the association of positive histone marks over the SLC6A4 gene locus. Cocaine 14-21 solute carrier family 6 member 4 Homo sapiens 83-89 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 4 Homo sapiens 4-25 22379462-2 2011 Cocaine, a competitive antagonist of the serotonin transporter, similar to selective serotonin reuptake inhibitors (SSRIs), also blocks dopamine and norepinephrine transporters, leaving the direct mechanism through which cocaine disrupts the developing serotonin system unclear. Cocaine 0-7 solute carrier family 6 member 4 Homo sapiens 41-62 22379462-2 2011 Cocaine, a competitive antagonist of the serotonin transporter, similar to selective serotonin reuptake inhibitors (SSRIs), also blocks dopamine and norepinephrine transporters, leaving the direct mechanism through which cocaine disrupts the developing serotonin system unclear. Cocaine 221-228 solute carrier family 6 member 4 Homo sapiens 41-62 21420984-1 2011 Cocaine binds and inhibits dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter. Cocaine 0-7 solute carrier family 6 member 4 Homo sapiens 92-113 21473026-6 2004 In earlier studies it was shown that a (123)I-labeled nortropane cocaine analog, 2beta-carbomethoxy-3beta-(4 -((Z)-2-[(123)I]iodoethenyl)phenyl)nortropane ([(123)I]pZIENT), had a high affinity for the human SERT and was suitable for the visualization of this transporter in non-human primates with single-photon emission computed tomography (38). Cocaine 65-72 solute carrier family 6 member 4 Homo sapiens 207-211 21146984-1 2011 Cocaine, a potent stimulant of the central nervous system, owes its reinforcing and stimulant properties to its ability to inhibit monoamine uptake systems such as the Dopamine Transporter (DAT), and the Serotonin Transporter (SERT) located on presynaptic neurons in the striatum. Cocaine 0-7 solute carrier family 6 member 4 Homo sapiens 204-225 21146984-1 2011 Cocaine, a potent stimulant of the central nervous system, owes its reinforcing and stimulant properties to its ability to inhibit monoamine uptake systems such as the Dopamine Transporter (DAT), and the Serotonin Transporter (SERT) located on presynaptic neurons in the striatum. Cocaine 0-7 solute carrier family 6 member 4 Homo sapiens 227-231 19351213-1 2009 BACKGROUND AND AIM: The human serotonin (5-hydroxytryptamine) transporter, encoded by the SLC6A4 gene on chromosome 17q11.1-q12, is the cellular reuptake site for serotonin and a site of action for several drugs with central nervous system effects, including both therapeutic agents (e.g. antidepressants) and drugs of abuse (e.g. cocaine). Cocaine 331-338 solute carrier family 6 member 4 Homo sapiens 90-96 19837674-5 2009 Cross-linking also inhibited transport, and this process was blocked by cocaine, which is expected to stabilize SERT in conformations where the two positions are separated, but cocaine did not decrease accessibility of either of the two cysteines to modification by 2-aminoethyl methanethiosulfonate. Cocaine 72-79 solute carrier family 6 member 4 Homo sapiens 112-116 19572987-7 2009 It has been demonstrated that several drugs of abuse such as amphetamine and cocaine inhibit the SERT expression; however, the role of alcohol is yet to be elucidated. Cocaine 77-84 solute carrier family 6 member 4 Homo sapiens 97-101 20159976-1 2010 The plasma membrane serotonin (5-HT) transporter (SERT, SLC6A4) clears 5-HT after release at nerve termini and is targeted by both antidepressant medications and psychostimulants (e.g. MDMA, cocaine). Cocaine 191-198 solute carrier family 6 member 4 Homo sapiens 50-54 20159976-1 2010 The plasma membrane serotonin (5-HT) transporter (SERT, SLC6A4) clears 5-HT after release at nerve termini and is targeted by both antidepressant medications and psychostimulants (e.g. MDMA, cocaine). Cocaine 191-198 solute carrier family 6 member 4 Homo sapiens 56-62 18321529-0 2008 Relationship of the serotonin transporter with prolactin response to meta-chlorophenylpiperazine in cocaine dependence. Cocaine 100-107 solute carrier family 6 member 4 Homo sapiens 20-41 19086766-8 2008 Selective serotonin transporter (SERT) inhibitors were also effective in reducing cocaine use and blocked cocaine-induced brain activation and increases in extracellular dopamine. Cocaine 82-89 solute carrier family 6 member 4 Homo sapiens 10-31 19086766-8 2008 Selective serotonin transporter (SERT) inhibitors were also effective in reducing cocaine use and blocked cocaine-induced brain activation and increases in extracellular dopamine. Cocaine 82-89 solute carrier family 6 member 4 Homo sapiens 33-37 19086766-8 2008 Selective serotonin transporter (SERT) inhibitors were also effective in reducing cocaine use and blocked cocaine-induced brain activation and increases in extracellular dopamine. Cocaine 106-113 solute carrier family 6 member 4 Homo sapiens 10-31 19086766-8 2008 Selective serotonin transporter (SERT) inhibitors were also effective in reducing cocaine use and blocked cocaine-induced brain activation and increases in extracellular dopamine. Cocaine 106-113 solute carrier family 6 member 4 Homo sapiens 33-37 18321529-1 2008 BACKGROUND: Preclinical evidence indicates that exposure to cocaine influences the activity of the serotonin transporter (5-HTT) as well as several 5-HT receptor subtypes. Cocaine 60-67 solute carrier family 6 member 4 Homo sapiens 99-120 18321529-10 2008 CONCLUSIONS: Disturbances in serotonin transporter binding and post-synaptic 5-HT receptor function seem to be associated in cocaine-dependent subjects. Cocaine 125-132 solute carrier family 6 member 4 Homo sapiens 29-50 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 4 Homo sapiens 271-275 19075665-4 2008 Therapeutic strategies have mainly focused on the development of compounds that block the activity of SERT, for instance reuptake inhibitors (e.g. tricyclics, "selective" serotonin reuptake inhibitors) and in the past, specific substrate-type releasers (e.g. amphetamine and cocaine derivatives). Cocaine 275-282 solute carrier family 6 member 4 Homo sapiens 102-106 17698848-2 2007 Ibogaine also inhibited binding to SERT of the cocaine analog 2beta-2-carbomethoxy-3-(4-[(125)I]iodophenyl)tropane. Cocaine 47-54 solute carrier family 6 member 4 Homo sapiens 35-39 17000009-0 2006 Polymorphism in the serotonin transporter gene and moderators of prolactin response to meta-chlorophenylpiperazine in African-American cocaine abusers and controls. Cocaine 135-142 solute carrier family 6 member 4 Homo sapiens 20-41 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 4 Homo sapiens 417-421 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 4 Homo sapiens 417-421 16272152-3 2006 The hSERT I172M mutant displays a marked loss of inhibitor potency for multiple inhibitors such as (RS)-CIT, clomipramine, RTI-55, fluoxetine, cocaine, nisoxetine, mazindol, and nomifensine, whereas recognition of substrates, including serotonin and 3,4-methylenedioxymethamphetamine, is unaffected. Cocaine 143-150 solute carrier family 6 member 4 Homo sapiens 4-9 16451060-1 2006 The nortropane cocaine analogue, 2beta-carbomethoxy-3beta-[4"-((Z)-2-iodoethenyl)phenyl]nortropane (ZIENT), is a high affinity, selective serotonin transporter (SERT) ligand that has shown promise as a SERT imaging agent for single photon computed tomography (SPECT) when labeled with I-123. Cocaine 15-22 solute carrier family 6 member 4 Homo sapiens 138-159 16451060-1 2006 The nortropane cocaine analogue, 2beta-carbomethoxy-3beta-[4"-((Z)-2-iodoethenyl)phenyl]nortropane (ZIENT), is a high affinity, selective serotonin transporter (SERT) ligand that has shown promise as a SERT imaging agent for single photon computed tomography (SPECT) when labeled with I-123. Cocaine 15-22 solute carrier family 6 member 4 Homo sapiens 161-165 16451060-1 2006 The nortropane cocaine analogue, 2beta-carbomethoxy-3beta-[4"-((Z)-2-iodoethenyl)phenyl]nortropane (ZIENT), is a high affinity, selective serotonin transporter (SERT) ligand that has shown promise as a SERT imaging agent for single photon computed tomography (SPECT) when labeled with I-123. Cocaine 15-22 solute carrier family 6 member 4 Homo sapiens 202-206 15091312-0 2004 Relationship between serotonin transporter gene polymorphisms and platelet serotonin transporter sites among African-American cocaine-dependent individuals and healthy volunteers. Cocaine 126-133 solute carrier family 6 member 4 Homo sapiens 75-96 16112691-1 2005 Mutants of serotonin transporter that are altered in their regulation by cGMP were tested for the ability of cocaine and the antidepressant drugs imipramine, sertraline, citalopram and fluoxetine to inhibit serotonin transport. Cocaine 109-116 solute carrier family 6 member 4 Homo sapiens 11-32 16109588-0 2005 Polymorphism in the serotonin transporter gene and response to treatment in African American cocaine and alcohol-abusing individuals. Cocaine 93-100 solute carrier family 6 member 4 Homo sapiens 20-41 16109588-3 2005 The aims of the study were to investigate whether 5-HTTLPR genotypes differed in their response to treatment in cocaine- and alcohol-abusing patients. Cocaine 112-119 solute carrier family 6 member 4 Homo sapiens 50-58 16250852-3 2005 For this aim, an increasing number of radiopharmaceuticals labelled with [123I], [99mTc], [11C] or [18F] have been developed such as cocaine derivatives for the DAT, compounds from the diphenyl sulfide family for the SERT, and dihydrotetrabenazine derivatives for the VMAT2. Cocaine 133-140 solute carrier family 6 member 4 Homo sapiens 217-221 15091312-4 2004 Polymerase chain reaction-based genotyping of a 44 base pair insertion/deletion polymorphism in 5-HTTLPR was performed in 138 cocaine-dependent African-American subjects and 60 African-American controls. Cocaine 126-133 solute carrier family 6 member 4 Homo sapiens 96-104 15091312-8 2004 Bmax values were significantly lower in cocaine-dependent patients (640 +/- 233) than controls (906 +/- 225) (P < 0.001); however, 5-HTTLPR genotype distributions or allele frequencies did not differ between the two groups. Cocaine 40-47 solute carrier family 6 member 4 Homo sapiens 134-142 15091312-12 2004 Although platelet 5-HTT densities are reduced in patients with cocaine dependence compared with healthy volunteers, these genotypic variations in the serotonin transporter do not seem to influence levels of platelet 5-HTT in cocaine-dependent patients or healthy volunteers. Cocaine 63-70 solute carrier family 6 member 4 Homo sapiens 18-23 14593087-4 2004 This species selectivity was explored using computer-generated comparative molecular field analysis to model the interactions of the cocaine analogs and substituted amphetamines at hSERT, dSERT, and the cross-species chimera. Cocaine 133-140 solute carrier family 6 member 4 Homo sapiens 181-186 11904159-4 2002 Transient currents at hSERT and rSERT are also blocked by spermine and spermidine in the mM range, and by fluoxetine, cocaine, QX-314, and QX-222 in the microM range. Cocaine 118-125 solute carrier family 6 member 4 Homo sapiens 22-27 14644011-5 2003 The severity of gastrointestinal effects caused by drugs that inhibit SERT, such as tricyclic antidepressants, selective serotonin reuptake inhibitors and cocaine, does not usually prevent their therapeutic or recreational use because backup transporters and alterations in receptor gene expression allow the gut to adapt, albeit imperfectly, to their toxicity. Cocaine 155-162 solute carrier family 6 member 4 Homo sapiens 70-74 12590403-0 2003 Seasonal variations in the binding of [3H]paroxetine to the platelet serotonin transporter sites in African-American cocaine-dependent patients and healthy volunteers. Cocaine 117-124 solute carrier family 6 member 4 Homo sapiens 69-90 12491807-6 2002 Analyses of the genes provide new insight into their relation to neuronal diseases since NET, DAT and SERT are the molecular targets for many antidepressants as well as drugs of abuse such as cocaine and amphetamine. Cocaine 192-199 solute carrier family 6 member 4 Homo sapiens 102-106 12218660-2 2002 Since the serotonin transporter (5HTT) may be involved in modulating effects of cocaine, we investigated whether allelic variants of the 5HTT gene may confer susceptibility to cocaine dependence among African-American individuals. Cocaine 80-87 solute carrier family 6 member 4 Homo sapiens 10-31 12218660-2 2002 Since the serotonin transporter (5HTT) may be involved in modulating effects of cocaine, we investigated whether allelic variants of the 5HTT gene may confer susceptibility to cocaine dependence among African-American individuals. Cocaine 80-87 solute carrier family 6 member 4 Homo sapiens 33-37 12180970-0 2002 A cocaine insensitive chimeric insect serotonin transporter reveals domains critical for cocaine interaction. Cocaine 2-9 solute carrier family 6 member 4 Homo sapiens 38-59 12180970-0 2002 A cocaine insensitive chimeric insect serotonin transporter reveals domains critical for cocaine interaction. Cocaine 89-96 solute carrier family 6 member 4 Homo sapiens 38-59 12180970-2 2002 Molecular cloning of a serotonin transporter from the central nervous system of the insect Manduca sexta enabled us to define domains that affect antagonist action, particularly cocaine. Cocaine 178-185 solute carrier family 6 member 4 Homo sapiens 23-44 12180970-6 2002 To delineate domains and residues that could play a role in cocaine interaction, the human serotonin transporter was mutated to incorporate unique amino acid substitutions, detected in the Manduca homologue. Cocaine 60-67 solute carrier family 6 member 4 Homo sapiens 91-112 12180970-10 2002 The chimera MasSERT1-67/hSERT109-630, which involved only the TMD1 swap, showed greater sensitivity to cocaine (IC50 = 0.225 micro m) than the human transporter. Cocaine 103-110 solute carrier family 6 member 4 Homo sapiens 24-29 12057823-0 2002 Serotonin transporter polymorphisms and measures of impulsivity, aggression, and sensation seeking among African-American cocaine-dependent individuals. Cocaine 122-129 solute carrier family 6 member 4 Homo sapiens 0-21 12057823-1 2002 Considerable evidence indicates that serotonergic mechanisms, particularly the serotonin transporter (5HTT), may mediate central effects of cocaine and may also be involved in impulsive and aggressive behavior. Cocaine 140-147 solute carrier family 6 member 4 Homo sapiens 79-100 12057823-1 2002 Considerable evidence indicates that serotonergic mechanisms, particularly the serotonin transporter (5HTT), may mediate central effects of cocaine and may also be involved in impulsive and aggressive behavior. Cocaine 140-147 solute carrier family 6 member 4 Homo sapiens 102-106 12057823-2 2002 We investigated whether polymorphisms in the 5HTT gene were related to traits of impulsivity, sensation seeking, and aggression among cocaine abusers. Cocaine 134-141 solute carrier family 6 member 4 Homo sapiens 45-49 11900612-1 2001 Studies indicate that the serotonin system, particularly the serotonin transporter (5-HTT), may modulate the central effects of cocaine. Cocaine 128-135 solute carrier family 6 member 4 Homo sapiens 84-89 11408487-5 2001 The addition of either cocaine or serotonin (5-HT) protected SERT against MTSET inactivation. Cocaine 23-30 solute carrier family 6 member 4 Homo sapiens 61-65 11408487-0 2001 A lithium-induced conformational change in serotonin transporter alters cocaine binding, ion conductance, and reactivity of Cys-109. Cocaine 72-79 solute carrier family 6 member 4 Homo sapiens 43-64 9464199-0 1998 Cocaine, ethanol, and genotype effects on human midbrain serotonin transporter binding sites and mRNA levels. Cocaine 0-7 solute carrier family 6 member 4 Homo sapiens 57-78 10364189-2 1999 SERT is the major binding site in the brain for antidepressant drugs, and it also binds amphetamines and cocaine. Cocaine 105-112 solute carrier family 6 member 4 Homo sapiens 0-4 16160948-5 1999 Some cocaine-derived radioligands allow SERT imaging of the human brain using positron emission tomography (PET) although they have a limited selectivity. Cocaine 5-12 solute carrier family 6 member 4 Homo sapiens 40-44 11207425-4 2000 Quantitative autoradiography of [125I]RTI-55 was used to map and measure the effect of chronic cocaine use on SERT densities in the striatum, substantia nigra, amygdala, and adjacent paralimbic cortical areas of cocaine overdose (CO) victims with and without preterminal evidence of excited delirium (ED). Cocaine 95-102 solute carrier family 6 member 4 Homo sapiens 110-114 11207425-9 2000 Chronic cocaine exposure upregulated SERT densities in the substantia nigra of the CO, but not ED victims. Cocaine 8-15 solute carrier family 6 member 4 Homo sapiens 37-41 10873923-0 2000 Elevated central serotonin transporter binding availability in acutely abstinent cocaine-dependent patients. Cocaine 81-88 solute carrier family 6 member 4 Homo sapiens 17-38 10873923-4 2000 RESULTS: Significant increases in diencephalic and brainstem serotonin transporter binding (16.7% and 31.6%, respectively) were observed in cocaine-dependent subjects. Cocaine 140-147 solute carrier family 6 member 4 Homo sapiens 61-82 10427004-5 1999 Nontransported SERT antagonists such as cocaine and antidepressants were permissive for SERT phosphorylation but blocked serotonin effects. Cocaine 40-47 solute carrier family 6 member 4 Homo sapiens 15-19 10427004-5 1999 Nontransported SERT antagonists such as cocaine and antidepressants were permissive for SERT phosphorylation but blocked serotonin effects. Cocaine 40-47 solute carrier family 6 member 4 Homo sapiens 88-92 10473187-0 1999 PET examination of three potent cocaine derivatives as specific radioligands for the serotonin transporter. Cocaine 32-39 solute carrier family 6 member 4 Homo sapiens 85-106 9733975-1 1998 The serotonin (5-HT) transporter (5-HTT) is known to play a role in depression and many 5-HT related diseases, and is the target site for drugs of abuse, such as cocaine, MDMA, and methamphetamine. Cocaine 162-169 solute carrier family 6 member 4 Homo sapiens 34-39 9517841-4 1998 Quantitative ligand binding studies revealed a novel high affinity [125I]RTI-55 binding site assayed under 5-HT transporter (SERT) conditions which has low affinity for almost all classic biogenic amine transporter ligands, including high affinity 5-HT transporter inhibitors such as paroxetine, but which retains high affinity for cocaine analogs. Cocaine 332-339 solute carrier family 6 member 4 Homo sapiens 107-123 9517841-4 1998 Quantitative ligand binding studies revealed a novel high affinity [125I]RTI-55 binding site assayed under 5-HT transporter (SERT) conditions which has low affinity for almost all classic biogenic amine transporter ligands, including high affinity 5-HT transporter inhibitors such as paroxetine, but which retains high affinity for cocaine analogs. Cocaine 332-339 solute carrier family 6 member 4 Homo sapiens 125-129 9517841-4 1998 Quantitative ligand binding studies revealed a novel high affinity [125I]RTI-55 binding site assayed under 5-HT transporter (SERT) conditions which has low affinity for almost all classic biogenic amine transporter ligands, including high affinity 5-HT transporter inhibitors such as paroxetine, but which retains high affinity for cocaine analogs. Cocaine 332-339 solute carrier family 6 member 4 Homo sapiens 248-264 9517841-9 1998 Viewed collectively with the observation that ligands with high affinity for SERT(site2) are mostly cocaine analogs, these data lead us to speculate that actions of cocaine which differ from those of classic biogenic amine uptake inhibitors may be mediated in part via SERT(site2). Cocaine 100-107 solute carrier family 6 member 4 Homo sapiens 77-81 9517841-9 1998 Viewed collectively with the observation that ligands with high affinity for SERT(site2) are mostly cocaine analogs, these data lead us to speculate that actions of cocaine which differ from those of classic biogenic amine uptake inhibitors may be mediated in part via SERT(site2). Cocaine 165-172 solute carrier family 6 member 4 Homo sapiens 77-81 9517841-9 1998 Viewed collectively with the observation that ligands with high affinity for SERT(site2) are mostly cocaine analogs, these data lead us to speculate that actions of cocaine which differ from those of classic biogenic amine uptake inhibitors may be mediated in part via SERT(site2). Cocaine 165-172 solute carrier family 6 member 4 Homo sapiens 269-273 9464199-2 1998 The present investigation tested the hypothesis that brain serotonin transporter function is altered in chronic users of ethanol and cocaine, which might be related to a common serotonin transporter promoter polymorphism. Cocaine 133-140 solute carrier family 6 member 4 Homo sapiens 59-80 9464199-2 1998 The present investigation tested the hypothesis that brain serotonin transporter function is altered in chronic users of ethanol and cocaine, which might be related to a common serotonin transporter promoter polymorphism. Cocaine 133-140 solute carrier family 6 member 4 Homo sapiens 177-198 7789954-3 1995 SERT is a site of action for several drugs with CNS effects, including both therapeutic agents (e.g., antidepressants) and drugs of abuse (e.g., cocaine). Cocaine 145-152 solute carrier family 6 member 4 Homo sapiens 0-4 7488148-1 1995 The serotonin transporter expressed in brain, platelets, and placenta is a primary target for antidepressants, cocaine, and amphetamines. Cocaine 111-118 solute carrier family 6 member 4 Homo sapiens 4-25 9353288-0 1997 The third transmembrane domain of the serotonin transporter contains residues associated with substrate and cocaine binding. Cocaine 108-115 solute carrier family 6 member 4 Homo sapiens 38-59 8981589-7 1996 Time-dependent changes in DA or 5-HT transporter expression produced by prenatal cocaine exposure could likewise play an important role in some of the behavioral effects observed when offspring are tested postnatally. Cocaine 81-88 solute carrier family 6 member 4 Homo sapiens 32-48 7969065-1 1994 The serotonin transporter (SERT) is a target for many clinically significant drugs, such as cocaine, amphetamine, and antidepressants. Cocaine 92-99 solute carrier family 6 member 4 Homo sapiens 4-25 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 4 Homo sapiens 49-53 7969065-1 1994 The serotonin transporter (SERT) is a target for many clinically significant drugs, such as cocaine, amphetamine, and antidepressants. Cocaine 92-99 solute carrier family 6 member 4 Homo sapiens 27-31 8066050-9 1994 These results suggest that the association kinetics for the interaction of cocaine and RTI-55 with the placental serotonin transporter are significantly different. Cocaine 75-82 solute carrier family 6 member 4 Homo sapiens 113-134 8066050-0 1994 Human placenta as a target organ for cocaine action: interaction of cocaine with the placental serotonin transporter. Cocaine 37-44 solute carrier family 6 member 4 Homo sapiens 95-116 8066050-0 1994 Human placenta as a target organ for cocaine action: interaction of cocaine with the placental serotonin transporter. Cocaine 68-75 solute carrier family 6 member 4 Homo sapiens 95-116 8066050-1 1994 The interaction of cocaine and its analog 2 beta-carbomethoxy-3 beta-(4-iodophenyl) tropane (RTI-55) with the human placental serotonin transporter was investigated. Cocaine 19-26 solute carrier family 6 member 4 Homo sapiens 126-147 8066050-11 1994 It is concluded that cocaine and its analog RTI-55 are potent inhibitors of the function of the serotonin transporter that is expressed in the normal human placenta and in cultured human placental choriocarcinoma cells. Cocaine 21-28 solute carrier family 6 member 4 Homo sapiens 96-117 8066050-12 1994 Since the reported values for cocaine concentration in the blood of cocaine users are several-fold higher than the inhibition constant for cocaine, the present study strongly suggests that the function of the placental serotonin transporter may be severely impaired by maternal use of cocaine during pregnancy. Cocaine 30-37 solute carrier family 6 member 4 Homo sapiens 219-240 8066050-12 1994 Since the reported values for cocaine concentration in the blood of cocaine users are several-fold higher than the inhibition constant for cocaine, the present study strongly suggests that the function of the placental serotonin transporter may be severely impaired by maternal use of cocaine during pregnancy. Cocaine 68-75 solute carrier family 6 member 4 Homo sapiens 219-240 8066050-12 1994 Since the reported values for cocaine concentration in the blood of cocaine users are several-fold higher than the inhibition constant for cocaine, the present study strongly suggests that the function of the placental serotonin transporter may be severely impaired by maternal use of cocaine during pregnancy. Cocaine 68-75 solute carrier family 6 member 4 Homo sapiens 219-240 8066050-12 1994 Since the reported values for cocaine concentration in the blood of cocaine users are several-fold higher than the inhibition constant for cocaine, the present study strongly suggests that the function of the placental serotonin transporter may be severely impaired by maternal use of cocaine during pregnancy. Cocaine 68-75 solute carrier family 6 member 4 Homo sapiens 219-240