keyword
https://read.qxmd.com/read/38150333/development-of-2-aminotetralin-type-serotonin-5-ht-1-agonists-molecular-determinants-for-selective-binding-and-signaling-at-5-ht-1a-5-ht-1b-5-ht-1d-and-5-ht-1f-receptors
#1
JOURNAL ARTICLE
Ryan P McGlynn, Meng Cui, Brittany Brems, Otto Holbrook, Raymond G Booth
The serotonin (5-hydroxytryptamine, 5-HT) 5-HT1 G-protein coupled receptor subtypes (5-HT1A/1B/1D/1E/1F ) share a high sequence homology, confounding development of subtype-specific ligands. This study used a 5-HT1 structure-based ligand design approach to develop subtype-selective ligands using a 5-substituted-2-aminotetralin (5-SAT) chemotype, leveraging results from pharmacological, molecular modeling, and mutagenesis studies to delineate molecular determinants for 5-SAT binding and function at 5-HT1 subtypes...
December 27, 2023: ACS Chemical Neuroscience
https://read.qxmd.com/read/38110471/characterization-of-a-novel-rnai-yeast-insecticide-that-silences-mosquito-5-ht1-receptor-genes
#2
JOURNAL ARTICLE
Keshava Mysore, Teresia M Njoroge, Akilah T M Stewart, Nikhella Winter, Majidah Hamid-Adiamoh, Longhua Sun, Rachel Shui Feng, Lester D James, Azad Mohammed, David W Severson, Molly Duman-Scheel
G protein-coupled receptors (GPCRs), which regulate numerous intracellular signaling cascades that mediate many essential physiological processes, are attractive yet underexploited insecticide targets. RNA interference (RNAi) technology could facilitate the custom design of environmentally safe pesticides that target GPCRs in select target pests yet are not toxic to non-target species. This study investigates the hypothesis that an RNAi yeast insecticide designed to silence mosquito serotonin receptor 1 (5-HTR1) genes can kill mosquitoes without harming non-target arthropods...
December 15, 2023: Scientific Reports
https://read.qxmd.com/read/38066980/characterization-of-vasoreactivity-in-a-semi-arboreal-snake-the-tokara-habu-protobothrops-tokarensis
#3
JOURNAL ARTICLE
Tomoki Ootawa, Siyuan Wu, Ryoya Sekio, Henry Smith, Md Zahorul Islam, Ha Thi Thanh Nguyen, Yasuhiro Uno, Mitsuya Shiraishi, Atsushi Miyamoto
Vasoreactivity is relatively well documented in terrestrial snakes but has previously been investigated in only one semi-arboreal snake species. Consequently, the extent to which vasoreactivity is common across snake taxa or varies by habitat is unclear. The Tokara habu ( Protobothrops tokarensis ) is a semi-arboreal snake endemic to only two small adjacent Japanese islands, and hence a useful species for further investigation of vasoreactivity. We evaluated responses to known vasoactive substances in thoracic aortas isolated from Tokara habu...
November 23, 2023: Animals: An Open Access Journal From MDPI
https://read.qxmd.com/read/37817438/structural-studies-of-serotonin-receptor-family
#4
Apeksha Parajulee, Kuglae Kim
Serotonin receptors, also known as 5-HT receptors, belong to the G protein-coupled receptors (GPCRs) superfamily. They mediate the effects of serotonin, a neurotransmitter that plays a key role in a wide range of functions including mood regulation, cognition and appetite. The functions of serotonin are mediated by a family of 5-HT receptors including 12 GPCRs belonging to six major families: 5-HT1, 5-HT2, 5-HT4, 5-HT5, 5-HT6 and 5-HT7. Despite their distinct characteristics and functions, these receptors' subtypes share common structural features and signaling mechanisms...
October 11, 2023: BMB Reports
https://read.qxmd.com/read/37723479/the-discovery-structure-and-function-of-5-htr1e-serotonin-receptor
#5
REVIEW
Vinay Kumar Sharma, Y Peng Loh
Serotonin (5-hydroxytryptamine, 5-HT) is a unique neurotransmitter which can regulate various biological processes by activating thirteen different receptors. These serotonin receptors are divided into seven different classes based on their structure and functions. Since these receptors co-express in various tissue and cell types and share the same ligand (5-HT), it has been a challenge for the researchers to define specific pathway and separate physiological role for each of these serotonin receptors. Though the evidence of operational diversity of these receptors is continuously emerging, much work remains to be done...
September 18, 2023: Cell Communication and Signaling: CCS
https://read.qxmd.com/read/37685004/reduced-nitric-oxide-synthase-involvement-in-aigamo-duck-basilar-arterial-relaxation
#6
JOURNAL ARTICLE
Siyuan Wu, Tomoki Ootawa, Ryoya Sekio, Henry Smith, Md Zahorul Islam, Ha Thi Thanh Nguyen, Yasuhiro Uno, Mitsuya Shiraishi, Atsushi Miyamoto
The basilar arterial endothelium mediates blood vessel relaxation partly through the release of nitric oxide (NO). Apoptosis of cerebrovascular endothelial cells is linked to a high mortality rate in chickens infected with the highly pathogenic avian influenza virus, but interestingly, ducks exhibit a greater resistance to this virus. In this study, we examined the responsiveness of duck basilar arteries (BAs) to various vasoactive substances, including 5-hydroxytryptamine (5-HT), histamine (His), angiotensin (Ang) II, noradrenaline (NA), acetylcholine (ACh), and avian bradykinin ornithokinin (OK), aiming to characterize the receptor subtypes involved and the role of endothelial NO in vitro...
August 28, 2023: Animals: An Open Access Journal From MDPI
https://read.qxmd.com/read/37584461/spinal-motoneurons-respond-aberrantly-to-serotonin-in-a-rabbit-model-of-cerebral-palsy
#7
JOURNAL ARTICLE
Emily J Reedich, Landon T Genry, Preston R Steele, Elvia Mena Avila, Lisa Dowaliby, Alexander Drobyshevsky, Marin Manuel, Katharina A Quinlan
Cerebral palsy (CP) is caused by a variety of factors that damage the developing central nervous system. Impaired motor control, including muscle stiffness and spasticity, is the hallmark of spastic CP. Rabbits that experience hypoxic-ischaemic (HI) injury in utero (at 70%-83% gestation) are born with muscle stiffness, hyperreflexia and, as recently discovered, increased 5-HT in the spinal cord. To determine whether serotonergic modulation of spinal motoneurons (MNs) contributes to motor deficits, we performed ex vivo whole cell patch clamp in neonatal rabbit spinal cord slices at postnatal day (P) 0-5...
August 16, 2023: Journal of Physiology
https://read.qxmd.com/read/37509503/serotonergic-modulation-of-neurovascular-transmission-a-focus-on-prejunctional-5-ht-receptors-mechanisms
#8
REVIEW
Abimael González-Hernández, Bruno A Marichal-Cancino, Antoinette MaassenVanDenBrink, Carlos M Villalón
5-Hydroxytryptamine (5-HT), or serotonin, plays a crucial role as a neuromodulator and/or neurotransmitter of several nervous system functions. Its actions are complex, and depend on multiple factors, including the type of effector or receptor activated. Briefly, 5-HT can activate: (i) metabotropic (G-protein-coupled) receptors to promote inhibition (5-HT1 , 5-HT5 ) or activation (5-HT4 , 5-HT6 , 5-HT7 ) of adenylate cyclase, as well as activation (5-HT2 ) of phospholipase C; and (ii) ionotropic receptor (5-HT3 ), a ligand-gated Na+ /K+ channel...
June 29, 2023: Biomedicines
https://read.qxmd.com/read/37409181/antibacterial-activity-and-anxiolytic-like-effect-of-ziziphus-joazeiro-mart-leaves-in-adult-zebrafish-danio-rerio
#9
JOURNAL ARTICLE
Antônio Barros de Souza, Jacqueline Cosmo Andrade Pinheiro, Juliete Bezerra Soares, José Ismael Feitosa de Araújo, Sandra Maria Barbosa de Araújo, Francisco Lucas Alves Batista, Kalina Kelma Oliveira de Sousa, Saulo Relison Tintino, Isaac Moura Araujo, Francisco Ernani Alves Magalhães, Laura Hévila Inocencio Leite, Francisco Roberto de Azevedo
Ziziphus joazeiro Mart. is an endemic plant of the Caatinga that presents a great socioeconomic importance for the Northeast and Semiarid Region of Brazil. In view of this, this study aimed to evaluate the antibacterial activity and anxiolytic-like effects of Ziziphus joazeiro Mart leaves in adult zebrafish ( Danio rerio ). The characterization of the main classes of metabolites was performed through chemical reactions. The antibacterial and antibiotic potentiating activity was evaluated by broth microdilution assays...
December 15, 2023: Fish Shellfish Immunol Rep
https://read.qxmd.com/read/37204759/5-ht-7-receptors-mediate-dilation-of-rat-cremaster-muscle-arterioles-in-vivo
#10
JOURNAL ARTICLE
William F Jackson, Armond Daci, Janice M Thompson, Gregory D Fink, Stephanie W Watts
OBJECTIVE: Serotonin (5-HT) infusion in vivo causes hypotension and a fall in total peripheral resistance. However, the vascular segment and the receptors that mediate this response remain in question. We hypothesized that 5-HT7 receptors mediate arteriolar dilation to 5-HT in skeletal muscle microcirculation. METHODS: Cremaster muscles of isoflurane-anesthetized male Sprague-Dawley rats were prepared for in vivo microscopy of third- and fourth-order arterioles and superfused with physiological salt solution at 34°C...
May 19, 2023: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
https://read.qxmd.com/read/37052334/buspirone-for-early-satiety-and-symptoms-of-gastroparesis-a%C3%A2-multi-centre-randomised-placebo-controlled-double-masked-trial-besst
#11
RANDOMIZED CONTROLLED TRIAL
Henry P Parkman, Katherine P Yates, Irene Sarosiek, Robert S Bulat, Thomas L Abell, Kenneth L Koch, Braden Kuo, Madhusudan Grover, Gianrico Farrugia, Paul Silver, Amirah Abdullah, Alan H Maurer, Zubair Malik, Laura A Miriel, James Tonascia, Frank Hamilton, Pankaj J Pasricha, Richard W McCallum
BACKGROUND: Patients with gastroparesis and related disorders have symptoms including early satiety, postprandial fullness and bloating. Buspirone, a 5-HT1 receptor agonist, may improve fundic accommodation. AIM: To determine if buspirone treatment improves early satiety and postprandial fullness in patients with symptoms of gastroparesis. METHODS: This 4-week multi-centre clinical trial randomised patients with symptoms of gastroparesis and moderate-to-severe symptoms of fullness (Gastroparesis Cardinal Symptom Index [GCSI] early satiety/postprandial fullness subscore [ES/PPF]) to buspirone (10 mg orally) or placebo three times per day...
June 2023: Alimentary Pharmacology & Therapeutics
https://read.qxmd.com/read/37038661/anxiolytic-effects-of-n-4-5-dihydro-5-oxo-1-2-dithiolo-4-3-b-pyrrole-6-yl-n-methylformamide-a-pyrroloformamide-isolated-from-a-marine-streptomyces-sp-in-adult-zebrafish-by-the-5-ht-system
#12
JOURNAL ARTICLE
Hozana Patrícia S de F Cesário, Francisca Crislândia O Silva, Maria Kueirislene A Ferreira, Jane Eire S A de Menezes, Hélcio S Dos Santos, Aluísio Marques da Fonseca, Carlos Emídio S Nogueira, Marcia M Marinho, Emmanuel S Marinho, Alexandre Magno R Teixeira, Edilberto R Silveira, Otília Deusdênia L Pessoa
General anxiety disorders are among the most prevalent mental health problems worldwide. The emergence and development of anxiety disorders can be due to genetic (30-50%) or non-genetic (50-70%) factors. Despite medical progress, available pharmacotherapies are sometimes ineffective or can cause undesirable side effects. Thus, it becomes necessary to discover new safe and effective drugs against anxiety. This study evaluated the anxiolytic effect in adult zebrafish ( Danio rerio ) of a natural pyrroloformamide (PFD), N -(4,5-dihydro-5-oxo-1,2-dithiolo-[4,3,b]-pyrrole-6-yl)- N -methylformamide, isolated from a Streptomyces sp...
April 10, 2023: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/36902177/ergotamine-stimulates-human-5-ht-4-serotonin-receptors-and-human-h-2-histamine-receptors-in-the-heart
#13
JOURNAL ARTICLE
Hannes Jacob, Pauline Braekow, Rebecca Schwarz, Christian Höhm, Uwe Kirchhefer, Britt Hofmann, Joachim Neumann, Ulrich Gergs
Ergotamine (2'-methyl-5'α-benzyl-12'-hydroxy-3',6',18-trioxoergotaman) is a tryptamine-related alkaloid from the fungus Claviceps purpurea . Ergotamine is used to treat migraine. Ergotamine can bind to and activate several types of 5-HT1 -serotonin receptors. Based on the structural formula of ergotamine, we hypothesized that ergotamine might stimulate 5-HT4 -serotonin receptors or H2 -histamine receptors in the human heart. We observed that ergotamine exerted concentration- and time-dependent positive inotropic effects in isolated left atrial preparations in H2 -TG (mouse which exhibits cardiac-specific overexpression of the human H2 -histamine receptor)...
March 1, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/36889668/activation-of-renal-vascular-smooth-muscle-trpv4-channels-by-5-hydroxytryptamine-impairs-kidney-function-in-neonatal-pigs
#14
JOURNAL ARTICLE
Jeremiah M Afolabi, Olugbenga S Michael, Olufunke O Falayi, Praghalathan Kanthakumar, Pratheesh D Mankuzhy, Hitesh Soni, Adebowale Adebiyi
Control of microvascular reactivity by 5-hydroxytryptamine (5-HT; serotonin) is complex and may depend on vascular bed type and 5-HT receptors. 5-HT receptors consist of seven families (5-HT1 -5-HT7 ), with 5-HT2 predominantly mediating renal vasoconstriction. Cyclooxygenase (COX) and smooth muscle intracellular Ca2+ levels ([Ca2+ ]i ) have been implicated in 5-HT-induced vascular reactivity. Although 5-HT receptor expression and circulating 5-HT levels are known to be dependent on postnatal age, control of neonatal renal microvascular function by 5-HT is unclear...
March 6, 2023: Microvascular Research
https://read.qxmd.com/read/36722266/mast-cell-associated-serotonin-in-acupoint-contributes-to-acupuncture-analgesia-in-arthritis-rats-by-mediating-atp-release
#15
JOURNAL ARTICLE
Bing-Rong Li, Yu-Jia Li, Jing-Wen Xu, Meng Huang, Li-Na Wang, Di Zhang, Xue-Yong Shen, Guang-Hong Ding
BACKGROUND: The activation of subcutaneous mast cells (MCs) helps to trigger the analgesic effect induced by acupuncture (AP), a traditional oriental therapy, that has been gradually accepted worldwide. This work aimed to reveal whether the serotonin (5-hydroxytryptamine, 5-HT) released from MCs plays an important role in this process, which has a controversial effect in the mechanism of pain. METHODS: In vivo tests, a 20-min session of AP was applied at Zusanli acupuncture point (acupoint) of acute ankle arthritis rats...
January 9, 2023: Frontiers in Bioscience (Landmark Edition)
https://read.qxmd.com/read/36674892/renal-sympathetic-hyperactivity-in-diabetes-is-modulated-by-5-ht-1d-receptor-activation-via-no-pathway
#16
JOURNAL ARTICLE
Juan Francisco Fernández-González, José Ángel García-Pedraza, José Luis Ordóñez, Anaïs Clara Terol-Úbeda, María Luisa Martín, Asunción Morán, Mónica García-Domingo
Renal vasculature, which is highly innervated by sympathetic fibers, contributes to cardiovascular homeostasis. This renal sympathetic outflow is inhibited by 5-HT in normoglycaemic rats. Considering that diabetes induces cardiovascular complications, we aimed to determine whether diabetic state modifies noradrenergic input at renal level and its serotonergic modulation in rats. Alloxan diabetic rats were anaesthetized (pentobarbital; 60 mg/kg i.p.) and prepared for in situ autoperfusion of the left kidney to continuously measure systemic blood pressure (SBP), heart rate (HR), and renal perfusion pressure (RPP)...
January 10, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/36601513/investigating-the-potential-of-mirtazapine-to-induce-drug-seeking-behavior-in-free-choice-drinking-mouse-model
#17
JOURNAL ARTICLE
Yusuf S Althobaiti
Addiction to various drugs and chemicals is a significant public health concern worldwide. Addiction to prescription medications has increased due to the psychoactive effects of these medications, their availability, low price, and the lack of legal consequences for abusers. One of such prescription medication is mirtazapine (MIRT). MIRT is an antidepressant that has recently been reported to be abused and could induce withdrawal symptoms in different case studies. No previous study has investigated its abuse potential in animal models of drug addiction...
December 2022: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://read.qxmd.com/read/36548050/memory-and-anxiety-like-behavior-of-rats-in-the-plus-maze-discriminative-avoidance-task-role-of-serotonergic-transmission-in-the-basolateral-amygdala
#18
JOURNAL ARTICLE
João P F Kurita, Anderson H F F Leão, Vinicius S Bioni, Raphael Wuo-Silva, Alvaro C Lima, Murilo A Paiva-Santos, Gabriela F Marinho, Débora M G Cunha, Marcela Becegato, Leonardo B Lopes-Silva, Alessandra M Ribeiro, Regina H Silva
Optimal levels of anxiety are critical to memory consolidation, but maladaptive anxiety can disrupt memory acquisition. Serotonergic activity within the amygdala influences both anxiety-like behavior and aversive memory consolidation. To evaluate the effects of serotoninergic manipulations within the basolateral amygdala (BLA) on anxiety-like behavior and aversive memory in rats tested in the plus-maze discriminative avoidance task (PMDAT). The PMDAT investigates aversive memory and anxiety-like behavior simultaneously in rodents...
April 2023: Behavioral Neuroscience
https://read.qxmd.com/read/36521179/pharmacological-mechanism-of-the-non-hallucinogenic-5-ht-2a-agonist-ariadne-and-analogs
#19
JOURNAL ARTICLE
Michael J Cunningham, Hailey A Bock, Inis C Serrano, Benjamin Bechand, D J Vidyadhara, Emma M Bonniwell, David Lankri, Priscilla Duggan, Antonina L Nazarova, Andrew B Cao, Maggie M Calkins, Prashant Khirsariya, Christopher Hwu, Vsevolod Katritch, Sreeganga S Chandra, John D McCorvy, Dalibor Sames
Ariadne is a non-hallucinogenic analog in the phenylalkylamine chemical class of psychedelics that is closely related to an established synthetic hallucinogen, 2,5-dimethoxy-4-methyl-amphetamine (DOM), differing only by one methylene group in the α-position to the amine. Ariadne has been tested in humans including clinical trials at Bristol-Myers Company that indicate a lack of hallucinogenic effects and remarkable therapeutic effects, such as rapid remission of psychotic symptoms in schizophrenics, relaxation in catatonics, complete remission of symptoms in Parkinson's disease (PD), and improved cognition in geriatric subjects...
December 15, 2022: ACS Chemical Neuroscience
https://read.qxmd.com/read/36473166/fpt-a-2-aminotetralin-is-a-potent-serotonin-5-ht-1a-5-ht-1b-and-5-ht-1d-receptor-agonist-that-modulates-cortical-electroencephalogram-activity-in-adult-fmr1-knockout-mice
#20
JOURNAL ARTICLE
Tanishka S Saraf, Ryan P McGlynn, Omkar M Bhatavdekar, Raymond G Booth, Clinton E Canal
There are no approved medicines for fragile X syndrome (FXS), a monogenic, neurodevelopmental disorder. Electroencephalogram (EEG) studies show alterations in resting-state cortical EEG spectra, such as increased gamma-band power, in patients with FXS that are also observed in Fmr1 knockout models of FXS, offering putative biomarkers for drug discovery. Genes encoding serotonin receptors (5-HTRs), including 5-HT1A , 5-HT1B , and 5-HT1D Rs, are differentially expressed in FXS, providing a rationale for investigating them as pharmacotherapeutic targets...
December 6, 2022: ACS Chemical Neuroscience
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