ArticlePsychoneuroendocrinology2012
GPR30 is necessary for estradiol-induced desensitization of 5-HT1A receptor signaling in the paraventricular nucleus of the rat hypothalamus.
Article in Psychoneuroendocrinology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 33 citations in OpenAlex.
- The impact of estradiol on serotonin, glutamate, and dopamine systems.Frontiers in neuroscience · 2024Review
- Estradiol regulates voltage-gated potassium currents in corticotropin-releasing hormone neurons.The Journal of experimental biology · 2023Article
- Emerging Evidence on Membrane Estrogen Receptors as Novel Therapeutic Targets for Central Nervous System Pathologies.International journal of molecular sciences · 2023Review
- Regulation of Serotonin 1A Receptor SUMOylation by SENP2 and PIASxα.International journal of molecular sciences · 2021Article
- Gender Differences in Diabetic Kidney Disease: Focus on Hormonal, Genetic and Clinical Factors.International journal of molecular sciences · 2021Review
- Androgens and Their Role in Regulating Sex Differences in the Hypothalamic/Pituitary/Adrenal Axis Stress Response and Stress-Related Behaviors.Androgens: clinical research and therapeutics · 2021Review
- Roles for androgens in mediating the sex differences of neuroendocrine and behavioral stress responses.Biology of sex differences · 2020Review
- Sex differences in the hypothalamic-pituitary-adrenal axis' response to stress: an important role for gonadal hormones.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2019Review
- Understanding the role of steroids in typical and atypical brain development: Advantages of using a "brain in a dish" approach.Journal of neuroendocrinology · 2018Review
- Estrogen Receptors Modulation of Anxiety-Like Behavior.Vitamins and hormones · 2017Review
- International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators.Pharmacological reviews · 2015Review
- Gonadal steroid hormones and the hypothalamo-pituitary-adrenal axis.Frontiers in neuroendocrinology · 2014Review
- GPER1 stimulation alters posttranslational modification of RGSz1 and induces desensitization of 5-HT1A receptor signaling in the rat hypothalamus.Neuroendocrinology · 2014Article
- Estradiol potentiates 8-OH-DPAT-induced sumoylation of 5-HT₁A receptor: characterization and subcellular distribution of sumoylated 5-HT₁A receptors.Psychoneuroendocrinology · 2013Article
- Estradiol accelerates the effects of fluoxetine on serotonin 1A receptor signaling.Psychoneuroendocrinology · 2013Article
- Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Estrogen therapy used in combination with selective serotonin reuptake inhibitor (SSRI) treatment improves SSRI efficacy for the treatment of mood disorders. Desensitization of serotonin 1A (5-HT(1A)) receptors, which takes one to two weeks to develop in animals, is necessary for SSRI therapeutic efficacy. Estradiol modifies 5-HT(1A) receptor signaling and induces a partial desensitization in the paraventricular nucleus (PVN) of the rat within two days, but the mechanisms underlying this effect are currently unknown. The purpose of this study was to identify the estrogen receptor necessary for estradiol-induced 5-HT(1A) receptor desensitization. We previously showed that estrogen receptor β is not necessary for 5-HT(1A) receptor desensitization and that selective activation of estrogen receptor GPR30 mimics the effects of estradiol in rat PVN. Here, we used a recombinant adenovirus containing GPR30 siRNAs to decrease GPR30 expression in the PVN. Reduction of GPR30 prevented estradiol-induced desensitization of 5-HT(1A) receptor as measured by hormonal responses to the selective 5-HT(1A) receptor agonist, (+)8-OH-DPAT. To determine the possible mechanisms underlying these effects, we investigated protein and mRNA levels of 5-HT(1A) receptor signaling components including 5-HT(1A) receptor, Gαz, and RGSz1. We found that two days of estradiol increased protein and mRNA expression of RGSz1, and decreased 5-HT(1A) receptor protein but increased 5-HT(1A) mRNA; GPR30 knockdown prevented the estradiol-induced changes in 5-HT(1A) receptor protein in the PVN. Taken together, these data demonstrate that GPR30 is necessary for estradiol-induced changes in the 5-HT(1A) receptor signaling pathway and desensitization of 5-HT(1A) receptor signaling.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.