2004
DOI: 10.1016/j.biopsych.2004.06.020
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The –1438A/G polymorphism in the 5-hydroxytryptamine type 2A receptor gene affects promoter activity

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Cited by 232 publications
(148 citation statements)
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“…57,58 The antagonistic effect exerted by risperidone on these receptors will inhibit prolactin secretion, therefore counteracting the increase induced by risperidone binding to D2 receptors. The presence of a HTR2A-1438G allele leads to a lower density of these receptors, 37,38 resulting in higher prolactin secretion and increased levels of this hormone in patients homozygous for this allele, and also to a diminished therapy response (as described above). On the other hand, the lack of association with the DRD2 gene, in agreement with earlier studies, 33,59,60 reinforces the idea that the serotonin receptors have a more important function in regulating prolactin secretion induced by risperidone than by other drugs because of the differences in the pharmacodynamic profile between risperidone and other atypicals, such as clozapine and olanzapine.…”
Section: Pharmacogenetics Of Risperidone In Autismmentioning
confidence: 96%
See 1 more Smart Citation
“…57,58 The antagonistic effect exerted by risperidone on these receptors will inhibit prolactin secretion, therefore counteracting the increase induced by risperidone binding to D2 receptors. The presence of a HTR2A-1438G allele leads to a lower density of these receptors, 37,38 resulting in higher prolactin secretion and increased levels of this hormone in patients homozygous for this allele, and also to a diminished therapy response (as described above). On the other hand, the lack of association with the DRD2 gene, in agreement with earlier studies, 33,59,60 reinforces the idea that the serotonin receptors have a more important function in regulating prolactin secretion induced by risperidone than by other drugs because of the differences in the pharmacodynamic profile between risperidone and other atypicals, such as clozapine and olanzapine.…”
Section: Pharmacogenetics Of Risperidone In Autismmentioning
confidence: 96%
“…35,36 A decrease in promoter activity of the -1438G allele relative to the A allele results in lower density of these receptors in the brain. 37,38 The poorer response to risperidone observed in patients homozygous for the low expression G allele may therefore be explained by a lower availability of the 5-HT2A receptors and consequent decreased effectiveness of the drug. Another polymorphism in this gene, HTR2A 102T4C, has been more extensively studied.…”
Section: Pharmacogenetics Of Risperidone In Autismmentioning
confidence: 99%
“…116,121,[123][124][125] This polymorphism is in complete LD with a À1438-G/A promoter polymorphism in Caucasian populations (the extent of linkage may vary in different ethnic groups). The G allele of this last polymorphism shows a lower promoter activity than the A allele 171 and may partly explain the associations with response. 121,126,127 A second study did not find differences in expression between both alleles, but found that the À1438-G allele was associated with decreased promoter activity when expressed in combination with a À783-G variant in the same gene.…”
Section: Pharmacodynamic Factorsmentioning
confidence: 98%
“…Genetic variability in the 5HT2A promoter (À1438 G/A), as well as the beta subunit of its G-protein second messenger (GNB3 C825T) may have functional consequences that may affect serotonergic transmission through this receptor (Levine et al, 1990;Parsons et al, 2004). Recent analysis of the differential expression of the À1438 SNP has suggested that the AA genotype is associated with higher 5HT2A gene expression in cell lines also endogenously expressing 5HT2A (Parsons et al, 2004).…”
Section: Introductionmentioning
confidence: 99%
“…Recent analysis of the differential expression of the À1438 SNP has suggested that the AA genotype is associated with higher 5HT2A gene expression in cell lines also endogenously expressing 5HT2A (Parsons et al, 2004). Another investigation published by Murphy and colleagues (Murphy et al, 2003) showed that the silent 5HT2A (T102C) SNP in linkage disequilibrium with the À1438 polymorphism was significantly related to antidepressant intolerance in elderly subjects treated with paroxetine.…”
Section: Introductionmentioning
confidence: 99%