2,068 results match your criteria 5-ht receptor-mediated


X-linked serotonin 2C receptor is associated with a non-canonical pathway for sudden unexpected death in epilepsy.

Brain Commun 2021 9;3(3):fcab149. Epub 2021 Jul 9.

Developmental Neurogenetics Laboratory, Department of Neurology, Baylor College of Medicine, Houston, TX 77030, USA.

Sudden Unexpected Death in Epilepsy is a leading cause of epilepsy-related mortality, and the analysis of mouse Sudden Unexpected Death in Epilepsy models is steadily revealing a spectrum of inherited risk phenotypes based on distinct genetic mechanisms. Serotonin (5-HT) signalling enhances post-ictal cardiorespiratory drive and, when elevated in the brain, reduces death following evoked audiogenic brainstem seizures in inbred mouse models. However, no gene in this pathway has yet been linked to a spontaneous epilepsy phenotype, the defining criterion of Sudden Unexpected Death in Epilepsy. Read More

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Reduction in Hindquarter Vascular Resistance Supports 5-HT Receptor Mediated Hypotension.

Front Physiol 2021 24;12:679809. Epub 2021 Jun 24.

Department of Pharmacology and Toxicology, Michigan State University, East Lansing, MI, United States.

The 5-HT receptor is the primary mediator of both the (Read More

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Novel and atypical pathways for serotonin signaling.

Fac Rev 2021 1;10:52. Epub 2021 Jun 1.

The Institute of Functional Genomics (IGF), University of Montpellier, CNRS, INSERM, Montpellier, France.

Serotonin (5-HT) appeared billions of years before 5-HT receptors and synapses. It is thus not surprising that 5-HT can control biological processes independently of its receptors. One example is serotonylation, which consists of covalent binding of 5-HT to the primary amine of glutamine. Read More

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Kappa Opioid Receptor Mediated Differential Regulation of Serotonin and Dopamine Transporters in Mood and Substance Use Disorder.

Handb Exp Pharmacol 2021 Jun 17. Epub 2021 Jun 17.

Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA, USA.

Dynorphin (DYN) is an endogenous neurosecretory peptide which exerts its activity by binding to the family of G protein-coupled receptors, namely the kappa opioid receptor (KOR). Opioids are associated with pain, analgesia, and drug abuse, which play a central role in mood disorders with monoamine neurotransmitter interactions. Growing evidence demonstrates the cellular signaling cascades linked to KOR-mediated monoamine transporters regulation in cell models and native brain tissues. Read More

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Molecular and clinical aspects of potential neurotoxicity induced by new psychoactive stimulants and psychedelics.

Exp Neurol 2021 Sep 4;343:113778. Epub 2021 Jun 4.

Division of Clinical Pharmacology and Toxicology, University Hospital Basel and University of Basel, Basel, Switzerland; Institute of Pharmacology, Medical University of Vienna, Vienna, Austria; Institute of Applied Physics, TU Wien, Vienna, Austria. Electronic address:

New psychoactive stimulants and psychedelics continue to play an important role on the illicit new psychoactive substance (NPS) market. Designer stimulants and psychedelics both affect monoaminergic systems, although by different mechanisms. Stimulant NPS primarily interact with monoamine transporters, either as inhibitors or as substrates. Read More

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September 2021

Impact of endogenous melatonin on rhythmic behaviors, reproduction, and survival revealed in melatonin-proficient C57BL/6J congenic mice.

J Pineal Res 2021 Jun 4:e12748. Epub 2021 Jun 4.

Laboratory for the Molecular Dynamics of Mental Disorders, Center for Brain Science, RIKEN, Wako-shi, Saitama, Japan.

The hormone melatonin is synthesized from serotonin by two enzymatic reactions (AANAT and ASMT/HIOMT) in the pineal gland following a circadian rhythm with low levels during the day and high levels at night. The robust nightly peak of melatonin secretion is an output signal of the circadian clock to the whole organism. However, so far the regulatory roles of endogenous melatonin in mammalian biological rhythms and physiology processes are poorly understood. Read More

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Effects of Withdrawal from Cocaine Self-Administration on Rat Orbitofrontal Cortex Parvalbumin Neurons Expressing : Sex-Dependent Changes in Neuronal Function and Unaltered Serotonin Signaling.

eNeuro 2021 Jul-Aug;8(4). Epub 2021 Jul 8.

Electrophysiology Research Section, Cellular Neurobiology Branch with: Cellular and Neurocomputational Systems Branch

The orbitofrontal cortex (OFC) is a brain region involved in higher-order decision-making. Rodent studies show that cocaine self-administration (CSA) reduces OFC contribution to goal-directed behavior and behavioral strategies to avoid drug intake. This change in OFC function persists for many weeks after cocaine withdrawal, suggesting involvement in the process of addiction. Read More

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Evidence for 5-HT receptor-mediated antiallodynic and antihyperalgesic effects of apigenin in mice suffering from mononeuropathy.

Br J Pharmacol 2021 Oct 22;178(19):4005-4025. Epub 2021 Jun 22.

Department of Pharmacology, Ningbo University, School of Medical Science, Ningbo, China.

Background And Purpose: Neuropathic pain places a devastating health burden, with very few effective therapies. We investigated the potential antiallodynic and antihyperalgesic effects of apigenin, a natural flavonoid with momoamine oxidase (MAO) inhibitory activity, against neuropathic pain and investigated the mechanism(s).

Experimental Approach: The neuropathic pain model was produced by chronic constriction injury of sciatic nerves in male C57BL/6J mice, with pain-related behaviours being assayed by von Frey test and Hargreaves test. Read More

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October 2021

Synthesis and Biological Evaluation of Tc-Labeled Phenylpiperazine Derivatives as Selective Serotonin-7 Receptor Ligands for Brain Tumor Imaging.

Mol Pharm 2021 06 24;18(6):2360-2374. Epub 2021 May 24.

Department of Radiopharmacy, Faculty of Pharmacy, Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Iran.

With a poor prognosis, glioblastoma multiforme is the most aggressive tumor of the central nervous system in humans. The aim of this study was to develop novel tracers for the tumor targeting and imaging of overexpressed serotonin-7 receptors (5-HTRs) in U-87 MG glioma xenografted nude mice. Two phenylpiperazine derivatives named as and were designed, and the corresponding radiotracers Tc- and Tc- were synthesized in high radiochemical purity (>95%). Read More

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Serotonin 5-HT7 receptors require cyclin-dependent kinase 5 to rescue hippocampal synaptic plasticity in a mouse model of Fragile X Syndrome.

Eur J Neurosci 2021 May 5. Epub 2021 May 5.

Department of Biomedical and Biotechnological Sciences, University of Catania, Catania, Italy.

Fragile X Syndrome is a genetic form of intellectual disability associated with autism, epilepsy and mood disorders. Electrophysiology studies in Fmr1 knockout (KO) mice, a murine model of Fragile X Syndrome, have demonstrated alterations of synaptic plasticity, with exaggerated long-term depression induced by activation of metabotropic glutamate receptors (mGluR-LTD) in Fmr1 KO hippocampus. We have previously demonstrated that activation of serotonin 5-HT7 receptors reverses mGluR-LTD in the hippocampus of wild-type and Fmr1 KO mice, thus correcting a synaptic dysfunction typically observed in this disease model. Read More

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5-HT receptor- and M muscarinic acetylcholine receptor-mediated activation of Gα in postmortem dorsolateral prefrontal cortex of opiate addicts.

Pharmacol Rep 2021 Aug 9;73(4):1155-1163. Epub 2021 Apr 9.

Laboratory of Neuropharmacology, IUNICS/IdISPa, University of the Balearic Islands (UIB), Palma de Mallorca, Spain.

Background: Chronic exposure to opiates causes the development of tolerance and physical dependence as well as persistent brain neuroplasticity. Despite a wealth of postmortem human studies for opiate addicts, little direct information regarding the functional status of serotonergic and cholinergic receptor-mediated signaling pathways in the human brain of opiate addicts is yet available.

Methods: Functional activation of Gα proteins coupled to 5-HT and M type muscarinic acetylcholine receptor (mAChR) was assessed by using the method named [S]GTPγS binding/immunoprecipitation in frontal cortical membrane preparations from postmortem human brains obtained from opiate addicts and matched controls. Read More

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Receptor-mediated biological effects of extracts obtained from three species.

Z Naturforsch C J Biosci 2021 Sep 7;76(9-10):367-373. Epub 2021 Apr 7.

Department of Chemical Sciences, Faculty of Pharmacy, Medical University of Plovdiv, 15A Vassil Aprilov Str., 4002 Plovdiv, Bulgaria.

This study reports the effects of aqueous extracts obtained from three fern species of Bulgarian origin: L., L., and L. Read More

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September 2021

[Neuroendorine paraneoplastic syndromes].

Authors:
M Böhm R Gellner

Hautarzt 2021 Apr 4;72(4):299-306. Epub 2021 Mar 4.

Medizinische Klinik B, Universitätsklinikum Münster, Münster, Deutschland.

Skin is commonly affected by neuroendorine paraneoplastic syndromes (PNS). This is due to the expression of receptors in the skin by which abnormally secreted neuroendocrine hormones and mediators elicit directly, and indirectly, cutaneous key signs and thus facilitate early diagnosis of these diseases. In acromegaly, induction of the growth hormone-insulin-like growth factor‑1 axis results in trophic changes of the acral portions of the skin and mucosal membranes including cutis verticis gyrata. Read More

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Role of 5-HT and 5-HT receptors of the dorsal periaqueductal gray in the anxiety- and panic-modulating effects of antidepressants in rats.

Behav Brain Res 2021 04 8;404:113159. Epub 2021 Feb 8.

Department of Pharmacology, School of Medicine of Ribeirão Preto, University of São Paulo (USP), Ribeirão Preto, SP, Brazil. Electronic address:

Antidepressant drugs are first-line treatment for panic disorder. Facilitation of 5-HT receptor-mediated neurotransmission in the dorsal periaqueductal gray (dPAG), a key panic-associated area, has been implicated in the panicolytic effect of the selective serotonin reuptake inhibitor fluoxetine. However, it is still unknown whether this mechanism accounts for the antipanic effect of other classes of antidepressants drugs (ADs) and whether the 5-HT interaction with 5-HT receptors in this midbrain area (which increases anxiety) is implicated in the anxiogenic effect caused by short-term treatment with ADs. Read More

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Intracranial mast cells contribute to the control of social behavior in male mice.

Behav Brain Res 2021 04 28;403:113143. Epub 2021 Jan 28.

Department of Integrative Physiology, Institute of Biomedical Sciences, Tokushima University Graduate School, Tokushima, Japan.

Mast cells (MCs) exist intracranially and have been reported to affect higher brain functions in rodents. However, the role of MCs in the regulation of emotionality and social behavior is unclear. In the present study, using male mice, we examined the relationship between MCs and social behavior and investigated the underlying mechanisms. Read More

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Serotonin 5-HT receptor-mediated behavior and binding in mice with the overactive and dysregulated serotonin transporter Ala56 variant.

Psychopharmacology (Berl) 2021 Apr 29;238(4):1111-1120. Epub 2021 Jan 29.

Department of Psychiatry, New York State Psychiatric Institute, Columbia University, 1051 Riverside Dr., Unit 78, New York, NY, 10032, USA.

Rationale: Elevated whole-blood serotonin (5-HT) is a robust biomarker in ~ 30% of patients with autism spectrum disorders, in which repetitive behavior is a core symptom. Furthermore, elevated whole-blood 5-HT has also been described in patients with pediatric obsessive-compulsive disorder. The 5-HT receptor is associated with repetitive behaviors seen in both disorders. Read More

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Deep Brain Stimulation of the dorsal raphe abolishes serotonin 1A facilitation of AMPA receptor-mediated synaptic currents in the ventral hippocampus.

Behav Brain Res 2021 04 18;403:113134. Epub 2021 Jan 18.

Instituto Farmacologia e Neurociências, Faculdade de Medicina, Universidade de Lisboa, Lisboa, Portugal; Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, Lisboa, Portugal.

In a previous study we showed that Deep Brain Stimulation (DBS) of the rat dorsal subregion of the dorsal raphe (DRD), which sends serotonergic projections to forebrain areas, such as the ventral hippocampus, induces anxiolytic-like effects. The purpose of the present study was to investigate neurobiological alterations which might underline these behavioral effects. For that, we tested the influence of DBS upon the neuromodulatory action of serotonin on excitatory post-synaptic currents (EPSCs) in the ventral hippocampus. Read More

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Serotonin and amyloid deposition: A link between depression and Alzheimer's disease?: An Editorial Highlight on "Pimavanserin, a 5HT receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease" on page 658.

J Neurochem 2021 03 18;156(5):560-562. Epub 2021 Jan 18.

Department of Nuclear Medicine, Bern University Hospital, Bern, Switzerland.

Indirect agonism has been invoked as part of the mechanism of antipsychotic action at dopamine D receptors, and more recently as a salient neuropharmacological aspect of the serotonin 5-HT drug pimavanserin (Pim). We now comment on an article in this volume showing that Pim treatment attenuates the deposition of Aβ protein in brain of transgenic Alzheimer's disease model mice. Pim treatment may interfere with Aβ deposition by shifting the balance between two 5-HT signaling pathways, that is, antagonism of G signaling and agonism of G signaling. Read More

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Role of 5-HT receptor-mediated serotonergic transmission in the medial prefrontal cortex in acute restraint stress-induced augmentation of rewarding memory of cocaine in mice.

Neurosci Lett 2021 01 19;743:135555. Epub 2020 Dec 19.

Laboratory of Molecular Pharmacology, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, 920-1192, Japan. Electronic address:

Stress enhances cocaine craving. We recently reported that acute restraint stress increases cocaine conditioned place preference (CPP) in mice; however, the underlying mechanisms remain unclear. This study aimed to examine the role of serotonergic transmission in the medial prefrontal cortex (mPFC) in cocaine CPP enhancement by acute restraint stress, which increases extracellular serotonin (5-HT) levels in the mPFC. Read More

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January 2021

Central Mechanisms of Apomorphine and m-Chlorophenylpiperazine on Synergistic Action for Ejaculation in Rats.

J Sex Med 2021 02 23;18(2):231-239. Epub 2020 Nov 23.

Department of Physiology and Anatomy, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, Miyagi, Japan.

Background: We previously reported that the combination of the dopamine (DA) receptor agonist apomorphine and the 5-hydroxytryptamine (5-HT) receptor agonist m-chlorophenylpiperazine (m-CPP) in rats potently and selectively facilitates the ejaculatory response through activation of D-like and 5-HT receptors, respectively.

Aim: The aim of this study was to clarify the target level of the proejaculatory effects induced by combination of these agonists.

Methods: For in vivo behavioral studies, apomorphine and m-CPP were given intracerebroventricularly and intrathecally alone or in combination with either drug administered systemically. Read More

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February 2021

Oxidized phospholipids affect small intestine neuromuscular transmission and serotonergic pathways in juvenile mice.

Neurogastroenterol Motil 2021 04 22;33(4):e14036. Epub 2020 Nov 22.

Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.

Background: Oxidized phospholipid derivatives (OxPAPCs) act as bacterial lipopolysaccharide (LPS)-like damage-associated molecular patterns. OxPAPCs dose-dependently exert pro- or anti-inflammatory effects by interacting with several cellular receptors, mainly Toll-like receptors 2 and 4. It is currently unknown whether OxPAPCs may affect enteric nervous system (ENS) functional and structural integrity. Read More

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A Subset of Purposeless Oral Movements Triggered by Dopaminergic Agonists Is Modulated by 5-HT Receptors in Rats: Implication of the Subthalamic Nucleus.

Int J Mol Sci 2020 Nov 12;21(22). Epub 2020 Nov 12.

Centre National de la Recherche Scientifique (Unité Mixte de Recherche 5287), 146 Rue Léo Saignat, 33076 Bordeaux CEDEX, France.

Dopaminergic medication for Parkinson's disease is associated with troubling dystonia and dyskinesia and, in rodents, dopaminergic agonists likewise induce a variety of orofacial motor responses, certain of which are mimicked by serotonin2C (5-HT) receptor agonists. However, the neural substrates underlying these communalities and their interrelationship remain unclear. In Sprague-Dawley rats, the dopaminergic agonist, apomorphine (0. Read More

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November 2020

Insights on Molecular Mechanisms of Ovarian Development in Decapod Crustacea: Focus on Vitellogenesis-Stimulating Factors and Pathways.

Front Endocrinol (Lausanne) 2020 6;11:577925. Epub 2020 Oct 6.

Fisheries Division, Japan International Research Center for Agricultural Sciences, Tsukuba, Japan.

Vitellogenesis in crustaceans is an energy-consuming process. Though the underlying mechanisms of ovarian maturation in decapod Crustacea are still unclear, evidence indicates the process to be regulated by antagonistically-acting inhibitory and stimulating factors specifically originating from X-organ/sinus gland (XO/SG) complex. Among the reported neuromediators, neuropeptides belonging to the crustacean hyperglycemic hormone (CHH)-family have been studied extensively. Read More

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Layer-specific serotonergic induction of long-term depression in the prefrontal cortex of rats.

Korean J Physiol Pharmacol 2020 Nov;24(6):517-527

Department of Physiology, The Catholic University of Korea, Seoul 06591, Korea.

Layer 2/3 pyramidal neurons (L2/3 PyNs) of the cortex extend their basal dendrites near the soma and as apical dendritic tufts in layer 1, which mainly receive feedforward and feedback inputs, respectively. It is suggested that neuromodulators such as serotonin and acetylcholine may regulate the information flow between brain structures depending on the brain state. However, little is known about the dendritic compartment-specific induction of synaptic transmission in single PyNs. Read More

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November 2020

5-HT receptor-mediated Gα activation in psychiatric disorders: A postmortem study.

World J Biol Psychiatry 2021 09 9;22(7):505-515. Epub 2020 Nov 9.

Laboratory of Neuropharmacology, IUNICS/IdISPa, University of the Balearic Islands (UIB), Palma de Mallorca, Spain.

Objectives: Serotonin-2A (5-HT) receptors play an important role in the regulation of many brain functions that are disturbed in patients with such psychiatric diseases as mood disorders and schizophrenia. The objective of this study was to evaluate 5-HT receptor-mediated signalling pathway through Gα activation in psychiatric patients by using post-mortem brain samples.

Methods: Functional activation of Gα proteins coupled to 5-HT receptors was determined by means of [S]GTPγS binding/immunoprecipitation assay in post-mortem prefrontal cortex of psychiatric patients diagnosed as bipolar disorder (BP), major depressive disorder (MDD), and schizophrenia, and individually matched controls. Read More

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September 2021

Pharmacology profile of F17464, a dopamine D receptor preferential antagonist.

Eur J Pharmacol 2021 Jan 14;890:173635. Epub 2020 Oct 14.

Innovation Unit CNS, CEPC Pierre Fabre Laboratories, Bel Air de Campans, 81106, Castres, France. Electronic address:

F17464 (N-(3-{4-[4-(8-Oxo-8H-[1,3]-dioxolo-[4,5-g]-chromen-7-yl)-butyl]-piperazin-1-yl}-phenyl)-methanesulfonamide, hydrochloride) is a new potential antipsychotic with a unique profile. The compound exhibits high affinity for the human dopamine receptor subtype 3 (hD) (K = 0.17 nM) and the serotonin receptor subtype 1a (5-HT) (K = 0. Read More

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January 2021

5-HT receptor-mediated attenuation of synaptic transmission in rat medial vestibular nucleus impacts on vestibular-related motor function.

J Physiol 2021 01 23;599(1):253-267. Epub 2020 Oct 23.

School of Biomedical Sciences, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong, PR China.

Key Points: Chemogenetic activation of medial vestibular nucleus-projecting 5-HT neurons resulted in deficits in vestibular-mediated tasks, including negative geotaxis, balance beam and rota-rod tests. The 5-HT receptor mediates the vestibular-related behavioural effects of 5-HT in the vestibular nucleus. 5-HT receptor activation attenuated evoked excitatory postsynaptic currents and evoked inhibitory postsynaptic currents via a presynaptic mechanism in the vestibular nucleus. Read More

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January 2021

Upregulated 5-HT receptor-mediated currents in the prefrontal cortex layer 5 neurons in the 15q11-13 duplication mouse model of autism.

Mol Brain 2020 08 24;13(1):115. Epub 2020 Aug 24.

Department of Pharmacology, Nippon Medical School, 1-1-5 Sendagi, Bunkyo-ku, Tokyo, 113-8602, Japan.

Serotonin (5-HT) is a well-known modulator of behavioral, physiological, and emotional functions of the forebrain region. We recently discovered alterations of serotonergic synaptic modulations in both, the prefrontal cortex (PFC) and the somatosensory cortex, in the 15q dup mouse model of autism spectrum disorder (ASD). To further understand the roles of the 5-HT system implicated in developmental disorders such as ASD, comparison with model animals exhibiting different phenotypes may be useful. Read More

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Metabolism and Functions of Amino Acids in Sense Organs.

Authors:
Guoyao Wu

Adv Exp Med Biol 2020 ;1265:201-217

Department of Animal Science, Texas A&M University, College Station, TX, USA.

Sense organs (eyes, ears, nose, tongue, and skin) provide senses of sight, hearing, smell, taste, and touch, respectively, to aid the survival, development, learning, and adaptation of humans and other animals (including fish). Amino acids (AAs) play an important role in the growth, development, and functions of the sense organs. Recent work has identified receptor-mediated mechanisms responsible for the chemosensory transduction of five basic taste qualities (sweet, sour, bitter, umami and salty tastes). Read More

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September 2020

Developmental programming of appetite and growth in male rats increases hypothalamic serotonin (5-HT)5A receptor expression and sensitivity.

Int J Obes (Lond) 2020 09 27;44(9):1946-1957. Epub 2020 Jul 27.

Buckingham Institute of Translational Medicine, University of Buckingham, Hunter Street, Buckingham, MK18 1EG, UK.

Background: Though it is well established that neonatal nutrition plays a major role in lifelong offspring health, the mechanisms underpinning this have not been well defined. Early postnatal accelerated growth resulting from maternal nutritional status is associated with increased appetite and body weight. Likewise, slow growth correlates with decreased appetite and body weight. Read More

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September 2020