PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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. Imipramine 146-156 solute carrier family 6 member 4 Homo sapiens 11-32 15625090-6 2005 This effect was mimicked by the tricyclic antidepressants imipramine and clomipramine, and by the SSRI citalopram, with relative efficacies that matched their known relative selectivities for the 5-HT transporter. Imipramine 58-68 solute carrier family 6 member 4 Homo sapiens 196-212 11746710-11 2001 Although the affinities of several non-amines were unchanged in the mutant SERT, the affinity of imipramine was decreased, revealing possible differences in amine and non-amine binding domains on the SERT. Imipramine 97-107 solute carrier family 6 member 4 Homo sapiens 200-204 15023476-3 2004 RESULTS: The platelet 5-HT transporter has been found to have an inconsistent association with suicidality; furthermore, the specificity of imipramine for the 5-HT transporter is most likely low, since the number of platelet impramine binding sites has not been reliably associated with platelet serotonin uptake (Vmax). Imipramine 140-150 solute carrier family 6 member 4 Homo sapiens 159-175 12849931-4 2003 Under the conditions of the assays, [(3)H]paroxetine binding in the LC was specific for the SERT, based on the rank order of affinity of compounds for inhibiting [(3)H]paroxetine binding in the LC, i.e. citalopram > imipramine > desipramine > mazindol. Imipramine 219-229 solute carrier family 6 member 4 Homo sapiens 92-96 8050484-3 1994 Many of these compounds are derivatives with modified naphthalenesulfonamide or isoquinolinesulfonamide structures, which appear to compete directly with imipramine for binding to the serotonin transporter. Imipramine 154-164 solute carrier family 6 member 4 Homo sapiens 184-205 11677251-5 2001 The potencies of the antidepressants citalopram, fluoxetine, paroxetine and imipramine were several-fold higher at hSERT compared with bSERT. Imipramine 76-86 solute carrier family 6 member 4 Homo sapiens 115-120 10869387-3 2000 5-HT reuptake blockers (e.g., imipramine, paroxetine) also raised [(3)H]5-HT efflux, reaching approximately one-third of the maximal effect of the hSERT substrates. Imipramine 30-40 solute carrier family 6 member 4 Homo sapiens 147-152 8863842-2 1996 Previously, using chimeric proteins, we determined that domains or residues distal to transmembrane domain 11 (amino acid 531) dictate the increased sensitivity of human SERT to imipramine. Imipramine 178-188 solute carrier family 6 member 4 Homo sapiens 170-174 8923121-5 1996 Also, concurrent inhibition of the 5-HT and noradrenaline transporters with 20 mg/kg imipramine increases cortical extracellular 5-HT concentration more than SSRI doses which maximally block the 5-HT transporter. Imipramine 85-95 solute carrier family 6 member 4 Homo sapiens 195-211 7478203-9 1995 Imipramine binding could be inhibited by potent non-tricyclic inhibitors of the serotonin transporter such as paroxetine and fluoxetine but also by the tricyclic antidepressant drugs clomipramine and desipramine. Imipramine 0-10 solute carrier family 6 member 4 Homo sapiens 80-101 7928004-4 1994 The uptake of [3H]5-HT was temperature, sodium and chloride dependent and was potently inhibited by the antidepressants clomipramine, imipramine, fluoxetine and fluvoxamine, which are specific for the 5-HT transporter. Imipramine 134-144 solute carrier family 6 member 4 Homo sapiens 201-217 11513817-8 2001 Measurements obtained before ingestion of the AA drink indicated that, relative to control subjects URs exhibited lower serotonin platelet concentrations, lower affinity, and fewer binding sites of the serotonin transporter for imipramine; these differences were unaffected by ATD. Imipramine 228-238 solute carrier family 6 member 4 Homo sapiens 202-223 10624553-5 1999 RESULTS: Unaffected relatives manifested lower platelet 5-HTT function than control participants as revealed both by reduced number and diminished affinity of imipramine binding sites and diminished platelet 5-HT content. Imipramine 159-169 solute carrier family 6 member 4 Homo sapiens 56-61 9832351-4 1998 Using the human neuroblastoma cell line IMR32 we demonstrate a GBR-12909 and cocaine-sensitive specific uptake of dopamine, whereas dopamine uptake in platelets is performed by an imipramine-sensitive serotonin transporter. Imipramine 180-190 solute carrier family 6 member 4 Homo sapiens 201-222 7711157-2 1995 Decreased platelet serotonin (5-HT) transport and reduced binding of imipramine or paroxetine to brain and platelet 5-HT uptake sites/transporters in patients with depression and suicide victims define the 5-HT transporter (5-HTT) as a candidate gene. Imipramine 69-79 solute carrier family 6 member 4 Homo sapiens 206-222 7758754-0 1995 Dithiothreithol promotes a higher affinity state of the serotonin transporter for the tricyclic antidepressant, imipramine. Imipramine 112-122 solute carrier family 6 member 4 Homo sapiens 56-77 8016192-3 1994 Among the compounds tested, indatraline, imipramine and fluoxetine, selective inhibitors of neuronal serotonin transporter, were the most potent inhibitors of [3H]-dopamine uptake in lymphocytes. Imipramine 41-51 solute carrier family 6 member 4 Homo sapiens 101-122 19892699-2 2010 SERT is the target for widely used antidepressant drugs, including imipramine, fluoxetine, and (S)-citalopram, which are competitive inhibitors of the transport function. Imipramine 67-77 solute carrier family 6 member 4 Homo sapiens 0-4 8218295-10 1993 The ligands of the serotonin transporter (imipramine, paroxetine, and fluoxetine) showed intermediate inhibitory potencies, whereas the ligands of the dopamine transporter (bupropion and GBR 12909) were the least potent. Imipramine 42-52 solute carrier family 6 member 4 Homo sapiens 19-40 3816412-1 1986 [3H]Imipramine and [3H]paroxetine label with high affinity a site associated with the serotonin transporter in brain and platelets. Imipramine 4-14 solute carrier family 6 member 4 Homo sapiens 86-107 2947974-4 1987 The affinity of imipramine for the 5-HT transporter is progressively enhanced with decreasing incubation temperature, thus favoring the selectivity of [3H]imipramine for the 5-HT transporter at 0 degrees C. At 37 degrees C, the Ki of imipramine for inhibition of [3H]paroxetine binding is 32 nM, and equals its Ki value for inhibition of 5-HT uptake into human platelets. Imipramine 155-165 solute carrier family 6 member 4 Homo sapiens 174-190 34417466-8 2021 Our SERT structure with bound imipramine and vilazodone reveals a unique binding pocket for vilazodone, expanding the boundaries of the extracellular vestibule. Imipramine 30-40 solute carrier family 6 member 4 Homo sapiens 4-8 2811859-2 1989 Iodoimipramine competitively inhibits [3H]imipramine binding with a KI of 0.52 nM and also inhibits [3H]serotonin transport competitively, suggesting that serotonin, imipramine, and iodoimipramine all bind to the same site on the serotonin transporter. Imipramine 4-14 solute carrier family 6 member 4 Homo sapiens 230-251 2898799-4 1988 The association of high affinity [3H]imipramine binding with the serotonin transporter in brain and platelets is well established. Imipramine 37-47 solute carrier family 6 member 4 Homo sapiens 65-86 2947974-2 1987 As this apparent discrepancy could be related to the assay temperature, we studied the thermodynamics of drug interaction with the 5-HT transporter at assay temperatures between 0 degrees C and 37 degrees C, using as radioligands [3H]imipramine (0 degrees C and 20 degrees C) and [3H]paroxetine (20 degrees C and 37 degrees C), a newly available probe for the 5-HT transporter. Imipramine 234-244 solute carrier family 6 member 4 Homo sapiens 131-147 2947974-4 1987 The affinity of imipramine for the 5-HT transporter is progressively enhanced with decreasing incubation temperature, thus favoring the selectivity of [3H]imipramine for the 5-HT transporter at 0 degrees C. At 37 degrees C, the Ki of imipramine for inhibition of [3H]paroxetine binding is 32 nM, and equals its Ki value for inhibition of 5-HT uptake into human platelets. Imipramine 16-26 solute carrier family 6 member 4 Homo sapiens 35-51 2947974-4 1987 The affinity of imipramine for the 5-HT transporter is progressively enhanced with decreasing incubation temperature, thus favoring the selectivity of [3H]imipramine for the 5-HT transporter at 0 degrees C. At 37 degrees C, the Ki of imipramine for inhibition of [3H]paroxetine binding is 32 nM, and equals its Ki value for inhibition of 5-HT uptake into human platelets. Imipramine 16-26 solute carrier family 6 member 4 Homo sapiens 174-190 2947974-4 1987 The affinity of imipramine for the 5-HT transporter is progressively enhanced with decreasing incubation temperature, thus favoring the selectivity of [3H]imipramine for the 5-HT transporter at 0 degrees C. At 37 degrees C, the Ki of imipramine for inhibition of [3H]paroxetine binding is 32 nM, and equals its Ki value for inhibition of 5-HT uptake into human platelets. Imipramine 155-165 solute carrier family 6 member 4 Homo sapiens 35-51 2947974-4 1987 The affinity of imipramine for the 5-HT transporter is progressively enhanced with decreasing incubation temperature, thus favoring the selectivity of [3H]imipramine for the 5-HT transporter at 0 degrees C. At 37 degrees C, the Ki of imipramine for inhibition of [3H]paroxetine binding is 32 nM, and equals its Ki value for inhibition of 5-HT uptake into human platelets. Imipramine 155-165 solute carrier family 6 member 4 Homo sapiens 174-190 2947974-4 1987 The affinity of imipramine for the 5-HT transporter is progressively enhanced with decreasing incubation temperature, thus favoring the selectivity of [3H]imipramine for the 5-HT transporter at 0 degrees C. At 37 degrees C, the Ki of imipramine for inhibition of [3H]paroxetine binding is 32 nM, and equals its Ki value for inhibition of 5-HT uptake into human platelets. Imipramine 155-165 solute carrier family 6 member 4 Homo sapiens 35-51 6835029-0 1983 [3H]2-Nitroimipramine: a selective "slowly-dissociating" probe of the imipramine binding site ("serotonin transporter") in platelets and brain. Imipramine 11-21 solute carrier family 6 member 4 Homo sapiens 96-118 3871227-0 1985 Tryptamine, a substrate for the serotonin transporter in human platelets, modifies the dissociation kinetics of [3H]imipramine binding: possible allosteric interaction. Imipramine 116-126 solute carrier family 6 member 4 Homo sapiens 32-53 6835029-3 1983 Our results support the relative utility of this ligand for studying the impramine binding site (serotonin transporter) since this analogue has both a higher affinity and specific activity than [3H]imipramine. Imipramine 73-82 solute carrier family 6 member 4 Homo sapiens 97-118 7056713-3 1982 This process requires Na+ and is blocked by imipramine, indicating that it is mediated by the serotonin transporter. Imipramine 44-54 solute carrier family 6 member 4 Homo sapiens 94-115 21129485-3 2011 Codon-optimization of this de novo constructed genes and construction of stable cell lines improved expression 3.5-fold and single-step immunoaffinity purification with FLAG-epitope tag yielded around one milligram functional SERT per liter culture medium assessed by [(3)H] imipramine ligand binding. Imipramine 275-285 solute carrier family 6 member 4 Homo sapiens 226-230 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). Imipramine 251-261 solute carrier family 6 member 4 Homo sapiens 66-70 23385211-5 2013 Imipramine dimers were only found to be moderate inhibitors of the human serotonin transporter (hSERT) having IC(50) values in the micromolar region whilst the induction of cell death occurred independently of hSERT expression. Imipramine 0-10 solute carrier family 6 member 4 Homo sapiens 73-94 23385211-5 2013 Imipramine dimers were only found to be moderate inhibitors of the human serotonin transporter (hSERT) having IC(50) values in the micromolar region whilst the induction of cell death occurred independently of hSERT expression. Imipramine 0-10 solute carrier family 6 member 4 Homo sapiens 96-101 23385211-5 2013 Imipramine dimers were only found to be moderate inhibitors of the human serotonin transporter (hSERT) having IC(50) values in the micromolar region whilst the induction of cell death occurred independently of hSERT expression. Imipramine 0-10 solute carrier family 6 member 4 Homo sapiens 210-215 21853482-4 2011 This novel TCA also exhibits an increased selectivity (relative to imipramine) in binding to hSERT versus the human norepinephrine transporter (hNET). Imipramine 67-77 solute carrier family 6 member 4 Homo sapiens 93-98 21853482-5 2011 Even higher selectivity could be obtained with 3,7-dihydroxymethyl imipramine, which was found to be 167-fold more selective for hSERT over hNET, representative of a 120-fold gain in selectivity relative to the parent imipramine. Imipramine 67-77 solute carrier family 6 member 4 Homo sapiens 129-134 21853482-6 2011 These results further validate our previous model for the binding of imipramine and high-affinity analogues of imipramine to the central binding site of hSERT. Imipramine 69-79 solute carrier family 6 member 4 Homo sapiens 153-158 21853482-6 2011 These results further validate our previous model for the binding of imipramine and high-affinity analogues of imipramine to the central binding site of hSERT. Imipramine 111-121 solute carrier family 6 member 4 Homo sapiens 153-158 27089947-4 2016 We employ ultraviolet-induced crosslinking with p-azido-L-phenylalanine (azF) at selected positions in hSERT to map the binding site of imipramine, a prototypical tricyclic antidepressant, and vortioxetine, a novel multimodal antidepressant. Imipramine 136-146 solute carrier family 6 member 4 Homo sapiens 103-108 20073575-9 2010 Finally, exposure of the cells to serotonin promoted an increase in MSCs apoptosis prevented by pargyline and the SERT inhibitor imipramine. Imipramine 129-139 solute carrier family 6 member 4 Homo sapiens 114-118 19641126-2 2009 Several of these drugs, including imipramine, citalopram, sertraline, and fluoxetine (Prozac), bound more avidly to SERT in the presence of Cl(-). Imipramine 34-44 solute carrier family 6 member 4 Homo sapiens 116-120 18801947-1 2008 Although several antidepressants (including fluoxetine, imipramine, citalopram, venlafaxine, and duloxetine) are known to inhibit the serotonin transporter (SERT), whether or not these molecules compete with 5-hydroxytryptamine (serotonin) (5-HT) for binding to SERT has remained controversial. Imipramine 56-66 solute carrier family 6 member 4 Homo sapiens 134-155 18801947-1 2008 Although several antidepressants (including fluoxetine, imipramine, citalopram, venlafaxine, and duloxetine) are known to inhibit the serotonin transporter (SERT), whether or not these molecules compete with 5-hydroxytryptamine (serotonin) (5-HT) for binding to SERT has remained controversial. Imipramine 56-66 solute carrier family 6 member 4 Homo sapiens 157-161 17499240-7 2007 Further, R-citalopram previously thought of as an inactive enantiomer strongly attenuated dissociation of the wild-type [(3)H]-imipramine:hSERT complex, whereas S-citalopram had almost no effect on this complex. Imipramine 127-137 solute carrier family 6 member 4 Homo sapiens 138-143 20829432-5 2010 Two approaches were used subsequently to differentiate between three clusters of potential docking poses: 1) a diagnostic SERT(Y95F) mutation, which greatly reduced the affinity for [(3)H]imipramine but did not affect substrate binding; 2) competition binding experiments in the presence and absence of carbamazepine (i.e., a tricyclic imipramine analog with a short side chain that competes with [(3)H]imipramine binding to SERT). Imipramine 188-198 solute carrier family 6 member 4 Homo sapiens 122-126 19948720-3 2010 We present an experimentally validated structural model of imipramine and analogous TCAs in the central substrate binding site of hSERT. Imipramine 59-69 solute carrier family 6 member 4 Homo sapiens 130-135 19213730-6 2009 We have identified a residue (Ser-438) located within the 5HT-binding pocket in hSERT to be a critical determinant for the potency of several antidepressants, including the selective serotonin reuptake inhibitor citalopram and the tricyclic antidepressants imipramine, clomipramine, and amitriptyline. Imipramine 257-267 solute carrier family 6 member 4 Homo sapiens 80-85