41,905 results match your criteria 5-ht receptors


Additive effects of mGluR positive allosteric modulation, mGluR orthosteric stimulation and 5-HTR antagonism on dyskinesia and psychosis-like behaviours in the MPTP-lesioned marmoset.

Naunyn Schmiedebergs Arch Pharmacol 2021 Sep 22. Epub 2021 Sep 22.

Neurodegenerative Disease Group, Montreal Neurological Institute-Hospital (The Neuro), 3801 University St, Montreal, QC, H3A 2B4, Canada.

Purpose: Antagonising serotonin (5-HT) type 2A receptors (5-HTR) is an effective strategy to alleviate both dyskinesia and psychosis in Parkinson's disease (PD). We have recently shown that activation of metabotropic glutamate 2 receptors (mGluR), via either orthosteric stimulation or positive allosteric modulation, enhances the anti-dyskinetic and anti-psychotic effects of 5-HTR antagonism. Here, we investigated if greater therapeutic efficacy would be achieved by combining 5-HTR antagonism with concurrent mGluR orthosteric stimulation and mGluR positive allosteric modulation. Read More

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September 2021

ATCC 6475 metabolites upregulate the serotonin transporter in the intestinal epithelium.

Benef Microbes 2021 Sep 22:1-18. Epub 2021 Sep 22.

Department of Pathology & Immunology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX 77030, USA.

The serotonin transporter (SERT) readily takes up serotonin (5-HT), thereby regulating the availability of 5-HT within the intestine. In the absence of SERT, 5-HT remains in the interstitial space and has the potential to aberrantly activate the many 5-HT receptors distributed on the epithelium, immune cells and enteric neurons. Perturbation of SERT is common in many gastrointestinal disorders as well as mouse models of colitis. Read More

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September 2021

The interplay between 5-HT and 5-HT receptors in the dorsal periaqueductal gray mediates anxiety-like behavior in mice.

Behav Brain Res 2021 Sep 18:113588. Epub 2021 Sep 18.

Psychobiology Group/Department of Psychology/CECH-UFSCar, São Carlos, SP, 13565-905, Brazil; Joint Graduate Program in Physiological Sciences UFSCar/UNESP. Rod. Washington Luís, Km 235, São Carlos, SP, 13565-905, Brazil; Graduate Program in Psychology UFSCar, Rod. Washington Luís, Km 235, São Carlos, SP, 13565-905, Brazil; Neuroscience and Behavioral Institute, Av. do Café, 2.450, 14050-220 Ribeirão Preto, SP, Brazil. Electronic address:

The monoamine neurotransmitter serotonin (5-HT) modulates anxiety by its activity on 5-HT receptors (5-HTR) expressed in the dorsal periaqueductal gray (dPAG). Here, we investigated the presence of 5-HT receptors (5-HTR) in the dPAG, and the interplay between 5-HTR and 5-HTR in the dPAG in mediating anxiety-like behavior in mice. We found that 5-HTR is expressed in the dPAG and the blockade of these receptors using intra-dPAG infusion of ondansetron (5-HTR antagonist; 3. Read More

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September 2021

Purinergic neurotransmission in the gustatory system.

Auton Neurosci 2021 Sep 11;236:102874. Epub 2021 Sep 11.

Dept. Cell & Developmental Biology, Dept. Otolaryngology, Univ. Colorado School of Medicine, Anschutz Medical Campus, MS 8108, Room L18-11118, RC-1, 12801 E. 17th Ave., Aurora, CO 80045, United States of America.

Taste buds consist of specialized epithelial cells which detect particular tastants and synapse onto the afferent taste nerve innervating the endorgan. The nature of the neurotransmitter released by taste cells onto the nerve fiber was enigmatic early in this century although neurotransmitters for other sensory receptor cell types, e.g. Read More

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September 2021

Supplementation Prevents Early Life Stress-Induced Anxiety and Depressive-Like Behavior in Maternal Separation Model-Possible Involvement of Microbiota-Gut-Brain Axis in Differential Regulation of MicroRNA124a/132 and Glutamate Receptors.

Front Neurosci 2021 31;15:719933. Epub 2021 Aug 31.

Behavioural Neuroscience Laboratory, Department of Animal Science, School of Life Sciences, Bharathidasan University, Tiruchirappalli, India.

This study was designed to investigate stressful social experience (SSE) in early life by examining how it can induce alterations in the microbiota-gut-brain axis. To test this, different experimental groups of pups experienced the presence of either a stranger (S) with mother (M+P+S) or without their mother (MS+S-M). Animals were assessed for anxiety-like behavior and high-throughput bacterial 16s rRNA sequencing was performed to analyze the structure of the gut microbiota. Read More

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The gut, its microbiome, and the brain: connections and communications.

J Clin Invest 2021 Sep;131(18)

Department of Pediatrics, Columbia University Vagelos College of Physicians and Surgeons, New York, New York, USA.

Modern research on gastrointestinal behavior has revealed it to be a highly complex bidirectional process in which the gut sends signals to the brain, via spinal and vagal visceral afferent pathways, and receives sympathetic and parasympathetic inputs. Concomitantly, the enteric nervous system within the bowel, which contains intrinsic primary afferent neurons, interneurons, and motor neurons, also senses the enteric environment and controls the detailed patterns of intestinal motility and secretion. The vast microbiome that is resident within the enteric lumen is yet another contributor, not only to gut behavior, but to the bidirectional signaling process, so that the existence of a microbiota-gut-brain "connectome" has become apparent. Read More

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September 2021

Mechanistic insights into dopaminergic and serotonergic neurotransmission - concerted interactions with helices 5 and 6 drive the functional outcome.

Chem Sci 2021 Aug 2;12(33):10990-11003. Epub 2021 Jul 2.

Research Programme on Biomedical Informatics (GRIB), Hospital del Mar Medical Research Institute (IMIM) - Pompeu Fabra University (UPF) Dr Aiguader 88 Barcelona E-08003 Spain

Brain functions rely on neurotransmitters that mediate communication between billions of neurons. Disruption of this communication can result in a plethora of psychiatric and neurological disorders. In this work, we combine molecular dynamics simulations, live-cell biosensor and electrophysiological assays to investigate the action of the neurotransmitter dopamine at the dopaminergic D receptor (DR). Read More

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Platelet FcγRIIA-induced serotonin release exacerbates the severity of Transfusion-Related Acute Lung Injury in mice.

Blood Adv 2021 Sep 14. Epub 2021 Sep 14.

Etablissement Français du Sang-Grand Est, Strasbourg, France.

Transfusion-related acute lung injury (TRALI) remains a major cause of transfusion-related fatalities. The mechanism of human antibody-mediated TRALI, especially the involvement of the Fcγ receptors, is not clearly established. Contrary to mice, human platelets are unique in their expression of the FcγRIIA/CD32A receptor, suggesting that our understanding of the pathogenesis of antibody-mediated TRALI is partial, since the current murine models incompletely recapitulate the human immunology. Read More

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September 2021

Discovery of G Protein-Biased Antagonists against 5-HTR.

J Med Chem 2021 Sep 14. Epub 2021 Sep 14.

Brain Science Institute, Korea Institute of Science and Technology, Seongbuk-gu, Seoul 02792, Republic of Korea.

5-HTR belongs to a family of G protein-coupled receptors and is associated with a variety of physiological processes in the central nervous system via the activation of the neurotransmitter serotonin (5-HT). To develop selective and biased 5-HTR ligands, we designed and synthesized a series of pyrazolyl-diazepanes and pyrazolyl-piperazines , which were evaluated for binding affinities to 5-HTR subtypes and functional selectivity for G protein and β-arrestin signaling pathways of 5-HTR. Among them, 1-(3-(3-chlorophenyl)-1-pyrazol-4-yl)-1,4-diazepane showed the best binding affinity for 5-HTR and selectivity over other 5-HTR subtypes. Read More

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September 2021

Synaptic mechanism underlying serotonin modulation of transition to cocaine addiction.

Science 2021 09 9;373(6560):1252-1256. Epub 2021 Sep 9.

Department of Basic Neurosciences, Medical Faculty, University of Geneva, CH-1211 Geneva, Switzerland.

[Figure: see text]. Read More

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September 2021

5-HT1A Receptors Alter Temporal Responses to Broadband Vocalizations in the Mouse Inferior Colliculus Through Response Suppression.

Front Neural Circuits 2021 27;15:718348. Epub 2021 Aug 27.

Department of Neurobiology and Anatomy, McGovern Medical School, The University of Texas Health Science Center at Houston, Houston, TX, United States.

Neuromodulatory systems may provide information on social context to auditory brain regions, but relatively few studies have assessed the effects of neuromodulation on auditory responses to acoustic social signals. To address this issue, we measured the influence of the serotonergic system on the responses of neurons in a mouse auditory midbrain nucleus, the inferior colliculus (IC), to vocal signals. Broadband vocalizations (BBVs) are human-audible signals produced by mice in distress as well as by female mice in opposite-sex interactions. Read More

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A prolactin-dependent sexually dimorphic mechanism of migraine chronification.

Cephalalgia 2021 Sep 12:3331024211039813. Epub 2021 Sep 12.

Department of Pharmacology, College of Medicine, University of Arizona, Tucson, AZ 85724.

Objective: Determination of possible sex differences in mechanisms promoting migraine progression and the contribution of prolactin and the prolactin long (PRLR-L) and short (PRLR-S) receptor isoforms.

Background: The majority of patients with chronic migraine and medication overuse headache are female. Prolactin is present at higher levels in women and increases migraine. Read More

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September 2021

Serotonin activates paraventricular thalamic neurons through direct depolarization and indirect disinhibition from Zona Incerta.

J Physiol 2021 Sep 12. Epub 2021 Sep 12.

Department of Psychology, Florida State University, Tallahassee, FL, 32306, USA.

Key Points: Serotonin (5-HT) depolarizes and excites paraventricular thalamic nucleus (PVT) neurons. 5-HT receptors are responsible for 5-HT excitation of PVT neurons and the coupling of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels to 5-HT receptors in part mediates the excitatory effect of 5-HT. 5-HT depresses the frequency of spontaneous inhibitory but not excitatory postsynaptic currents in PVT neurons. Read More

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September 2021

Sudden infant death syndrome: Melatonin, serotonin, and CD34 factor as possible diagnostic markers and prophylactic targets.

PLoS One 2021 10;16(9):e0256197. Epub 2021 Sep 10.

Saint-Petersburg State Pediatric Medical University, St. Petersburg, Russian Federation.

Sudden infant death syndrome (SIDS) is one of the primary causes of death of infants in the first year of life. According to the WHO's data, the global infant mortality rate is 0.64-2 per 1,000 live-born children. Read More

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September 2021

Effects of Sleep Deprivation by Olfactorily Induced Sexual Arousal Compared to Immobilization Stress and Manual Sleep Deprivation on Neuromessengers and Time Keeping Genes in the Suprachiasmatic Nuclei and Other Cerebral Entities of Syrian Hamsters-An Immunohistochemical Study.

Int J Environ Res Public Health 2021 Aug 31;18(17). Epub 2021 Aug 31.

Institute for Anatomy II, Goethe-Universität Frankfurt am Main, 60590 Frankfurt am Main, Germany.

We investigated the effects of sexual arousal induced by olfactory stimuli on the expression of neuromodulators, neurotransmitters and sexual steroid receptors in the suprachiasmatic nucleus (SCN, the circadian pacemaker of mammals) and other cerebral entities of Syrian hamsters () compared to manual sleep deprivation and immobilization stress. The hamsters kept under a 12:12 hours (h) light:dark cycle were deprived of sleep by sexual stimulation, gentle manual handling or immobilization stress for 1 h at the beginning of the light phase and subsequently sacrificed at zeitgeber time 01:00, respectively; for comparison, hamsters were manually sleep deprived for 6 or 20 h or sacrificed after completing a full sleep phase. As demonstrated by immunohistochemistry, apart from various alterations after manual sleep deprivation, sexual stimulation caused down-regulation of arginine-vasopressin (AVP), vasointestinal peptide (VIP), serotonin (5-HT), substance P (SP), and met-enkephalin (ME) in the SCN. Read More

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ACETYL-L-CARNITINE IN CHRONIC PAIN: A NARRATIVE REVIEW.

Pharmacol Res 2021 Sep 6:105874. Epub 2021 Sep 6.

Department of Medical Biotechnology and Molecular Medicine, Università degli Studi di Milano Milan, Italy.

Acetyl-L-carnitine (ALC) is an endogenous molecule that not only plays a role in energy metabolism, but also has antioxidant properties, protects from oxidative stress, modulates brain neurotransmitters such as acetylcholine, serotonin and dopamine, and acts on neurotrophic factors such as nerve growth factor (NGF) and metabotropic glutamate (mGlu) receptors by means of epigenetic mechanisms. Importantly, it induces mGlu2 expression at nerve terminals, thus giving rise to analgesia and preventing spinal sensitisation. It has also been found to have even long-term neurotrophic and analgesic activity in experimental models of chronic inflammatory and neuropathic pain. Read More

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September 2021

Vortioxetine as a new frontier in the treatment of chronic neuropathic pain: a review and update.

Ther Adv Psychopharmacol 2021 3;11:20451253211034320. Epub 2021 Sep 3.

Department of Neuroscience, Reproductive Sciences and Dentistry, University of Naples Federico II, Naples, Italy.

Chronic neuropathic pain (CNP) is a disabling medical condition that impairs the health-related quality-of-life of affected patients. A high prevalence of anxiety, depression, sleep disturbance and cognitive impairment has frequently been reported in association with CNP, making the management of this disease complex and often multidisciplinary. Dual-acting agents such as selective serotonin and noradrenalin reuptake inhibitors (SNRIs) are considered particularly useful in the modulation of pain and in treatment of the mood disorders frequently associated with CNP. Read More

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September 2021

The roles of serotonin in cell adhesion and migration, and cytoskeletal remodeling.

Cell Adh Migr 2021 12;15(1):261-271

National Centre for Biological Sciences, Tata Institute of Fundamental Research, Bengaluru, India.

Serotonin is well known as a neurotransmitter. Its roles in neuronal processes such as learning, memory or cognition are well established, and also in disorders such as depression, schizophrenia, bipolar disorder, and dementia. However, its effects on adhesion and cytoskeletal remodelling which are strongly affected by 5-HT receptors, are not as well studied with some exceptions for e. Read More

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December 2021

Cannabidiol and the corticoraphe circuit in post-traumatic stress disorder.

IBRO Neurosci Rep 2021 Dec 21;11:88-102. Epub 2021 Aug 21.

Department of Biology, Lamar University, Beaumont, TX 77710, USA.

Post-Traumatic Stress Disorder (PTSD), characterized by re-experiencing, avoidance, negative affect, and impaired memory processing, may develop after traumatic events. PTSD is complicated by impaired plasticity and medial prefrontal cortex (mPFC) activity, hyperactivity of the amygdala, and impaired fear extinction. Cannabidiol (CBD) is a promising candidate for treatment due to its multimodal action that enhances plasticity and calms hyperexcitability. Read More

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December 2021

Current status and future prospects of PET-imaging applications in patients with gastro-entero-pancreatic neuroendocrine tumors (GEP-NETs).

Eur J Radiol 2021 Aug 25;143:109932. Epub 2021 Aug 25.

Positron Emission Tomography Department, Clinical Center (CC), National Institutes of Health (NIH), Bethesda, MD 20814, USA.

Gastro-entero-pancreatic neuroendocrine tumors (GEP-NETs) represent a heterogeneous group of rare neoplasms with increasing incidence over the last decades. Localization of GEP-NETs and their metastases is a vital component for the implementation of accurate and patient-tailored treatment strategies. Addressing this challenge requires the employment of multidisciplinary imaging approaches, with hybrid positron emission tomography/computed tomography (PET/CT) imaging techniques standing at the forefront of this effort. Read More

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5-HT receptors enhance inhibitory synaptic input to principal neurons in the mouse basal amygdala.

Neuropharmacology 2021 Sep 3;198:108779. Epub 2021 Sep 3.

Department of Physiology, Maj Institute of Pharmacology, Polish Academy of Sciences, Smętna 12 Str., 31-343, Kraków, Poland. Electronic address:

The basal amygdala (BA) has been implicated in encoding fear and its extinction. The level of serotonin (5-HT) in the BA increases due to arousal and stress related to aversive stimuli. The effects of 5-HT receptor (5-HTR) activation and blockade on the activity of BA neurons have not yet been investigated. Read More

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September 2021

Transcriptome analysis provides genome annotation and expression profiles in the central nervous system of Lymnaea stagnalis at different ages.

BMC Genomics 2021 Sep 3;22(1):637. Epub 2021 Sep 3.

Department of Biology, College of Arts and Sciences, Saint Louis University, St. Louis, MO, USA.

Background: The pond snail, Lymnaea stagnalis (L. stagnalis), has served as a valuable model organism for neurobiology studies due to its simple and easily accessible central nervous system (CNS). L. Read More

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September 2021

Orexin receptors 1 and 2 in serotonergic neurons differentially regulate peripheral glucose metabolism in obesity.

Nat Commun 2021 09 2;12(1):5249. Epub 2021 Sep 2.

Max Planck Institute for Metabolism Research, Department of Neuronal Control of Metabolism, Cologne, Germany.

The wake-active orexin system plays a central role in the dynamic regulation of glucose homeostasis. Here we show orexin receptor type 1 and 2 are predominantly expressed in dorsal raphe nucleus-dorsal and -ventral, respectively. Serotonergic neurons in ventral median raphe nucleus and raphe pallidus selectively express orexin receptor type 1. Read More

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September 2021

Zonisamide attenuates the severity of levodopa-induced dyskinesia via modulation of the striatal serotonergic system in a rat model of Parkinson's disease.

Neuropharmacology 2021 Aug 30;198:108771. Epub 2021 Aug 30.

Department of Neurology, Kansai Medical University, Hirakata city, Osaka, Japan.

Glutamate, GABA, acetylcholine, dopamine, and serotonin interact with each other to regulate the flow of neural information in the striatum. Serotonin type 1A receptor (5HT1A) is primarily expressed on glutamatergic nerve terminals, and 5HT1B is expressed on GABAergic medium spiny neurons (MSNs). Zonisamide (ZNS) reportedly improves the off period without worsening levodopa-induced dyskinesia (LID) in patients with advanced Parkinson's disease. Read More

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Characterization of the spontaneous degenerative mitral valve disease in FVB mice.

PLoS One 2021 2;16(9):e0257022. Epub 2021 Sep 2.

Laboratoire de Pharmacologie et Toxicologie NeuroCardiovasculaire UR7296, Fédération de Médecine Translationnelle, Centre Hospitalier Universitaire et Université de Strasbourg, Centre de Recherche en Biomédecine de Strasbourg (CRBS), Strasbourg, France.

Background: The development of new non-surgical treatments dedicated to mitral valve degeneration is limited by the absence of relevant spontaneous and rapidly progressing animal experimental models.

Animals: We characterized the spontaneous mitral valve degeneration in two inbred FVB mouse strains compared to C57BL/6J and investigated a contribution of the serotonergic system.

Methods: Males and females FVB/NJ and FVB/NRj were compared to the putative C57BL/6J control at 12, 16, 20 and 24 weeks of age. Read More

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September 2021

Liquid chromatography-mass spectrometry in-depth analysis and in silico verification of the potential active ingredients of Baihe Dihuang decoction in vivo and in vitro.

J Sep Sci 2021 Sep 2. Epub 2021 Sep 2.

Department of Analysisand Testing, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, P. R. China.

Baihe Dihuang decoction is a commonly used herbal formula to treat depression and insomnia in traditional Chinese medicine. This study established a liquid chromatography-mass spectrometry method to investigate the potential active ingredients and the components absorbed in the blood and brain tissue of mice. Using a new data processing method, 94 chemical components were identified, 33 and 9 of which were absorbed in the blood and brain. Read More

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September 2021

Depression and dry eye: a narrative review.

Rev Assoc Med Bras (1992) 2021 Mar;67(3):462-467

Centro Universitário de João Pessoa - João Pessoa (PB), Brazil.

Dry eye disease (DED) is a multifactorial disease affecting tear quality and/or production and eye surface and is one of the most common eye disorders found in clinical practice. The association between psychiatric disorders and dry eye has been the subject of several studies since patients with this syndrome present a tendency toward a depressive mood. This narrative review aims to demonstrate the relationship between depression and DED, which is due to the side effects of psychotropic drugs or the tendency of the low pain threshold of the depressive patient. Read More

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Activity of ("Kratom") Alkaloids at Serotonin Receptors.

J Med Chem 2021 Sep 1. Epub 2021 Sep 1.

Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United States.

Kratom alkaloids have mostly been evaluated for their opioid activity but less at other targets that could contribute to their physiological effects. Here, we investigated the in vitro and in vivo activity of kratom alkaloids at serotonin receptors (5-HTRs). Paynantheine and speciogynine exhibited high affinity for 5-HTRs and 5-HTRs, unlike the principal kratom alkaloid mitragynine. Read More

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September 2021

Recent advances in the treatment of irritable bowel syndrome.

Pol Arch Intern Med 2021 Aug 30;131(7-8):709-715. Epub 2021 Aug 30.

Irritable bowel syndrome (IBS) is a chronic functional gastrointestinal disorder which presents with abdominal pain and altered bowel habits. It affects about 20% of the general population, mainly women, and has a considerable impact on the quality of life and health care costs. Four different entities of IBS have been identified: IBS with constipation (IBS‑ C), IBS with diarrhea (IBS D), IBS with a mixed pattern of constipation and diarrhea, and unclassified IBS. Read More

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Development of neuroactive steroids for the treatment of postpartum depression.

J Neuroendocrinol 2021 Jul 27:e13019. Epub 2021 Jul 27.

Sage Therapeutics, Inc, Cambridge, MA, USA.

Postpartum depression (PPD) is a common major depressive episode surrounding childbirth, with estimated rates ranging from 5.5% to 23.5% of all live births across Europe and the USA based on the presence of key symptoms. Read More

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