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Raphael Rodrigues Perim, Daryl P Fields, Gordon S Mitchell
Intermittent spinal serotonin receptor activation elicits phrenic motor facilitation (pMF), a form of spinal respiratory motor plasticity. Episodic activation of either serotonin type-2 (5-HT2) or 7 (5-HT7) receptors elicits pMF, although they do so via distinct cellular mechanisms known as the Q (5-HT2) and S (5-HT7) pathways to pMF. When co-activated, these pathways interact via mutual, cross-talk inhibition. Although we have a rudimentary understanding of mechanisms mediating cross-talk interactions between spinal 5-HT2 subtype-A (5-HT2A) and 5-HT7 receptor activation, we do not know if similar interactions exist between 5-HT2 subtype-B (5-HT2B) and 5-HT7 receptors...
January 31, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
Karolina Pytka, Katarzyna Socała, Anna Rapacz, Dorota Nieoczym, Mateusz Pieróg, Anna Gryboś, Agata Siwek, Anna Waszkielewicz, Piotr Wlaź
Most antidepressants lower seizure threshold, which might be due to the modulation of serotonergic neurotransmission. Here, we investigated the effects of two 5-HT1A, 5-HT7 and 5-HT3 antagonists, i.e., 1-(2-(2-(2,6-dimethylphenoxy)ethoxy)ethyl)-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-{2-[2-(2-chloro-6-methylphenoxy)ethoxy]ethyl}-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15), with antidepressant- and anxiolytic-like properties, on seizure thresholds in three acute seizure tests, i.e...
October 3, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
Hongyan Zhao, Yang Lin, Shurui Chen, Xin Li, Hongliang Huo
BACKGROUND: Epilepsy is a syndrome of brain dysfunction caused by spontaneous, abnormal discharge. Many anti-epileptic drugs have developed in past decades. 5-HT is an important neurotransmitter in the central and peripheral nervous system of the human body which is involved in a number of physiological activities, such as sensation, movement, and behavior. 5-HT subtype have been divided into seven sub-groups from 5-HT1 to 5HT7. However, the role of 5-HT3 receptor on epilepsy is unclear...
2018: Current Neuropharmacology
Edward Ofori, Xue Y Zhu, Jagan R Etukala, Kwakye Peprah, Kamanski R Jordan, Adia A Adkins, Barbara A Bricker, Hye J Kang, Xi-Ping Huang, Bryan L Roth, Seth Y Ablordeppey
5-HT1A and 5-HT7 receptors have been at the center of discussions recently due in part to their major role in the etiology of major central nervous system diseases such as depression, sleep disorders, and schizophrenia. As part of our search to identify dual targeting ligands for these receptors, we have carried out a systematic modification of a selective 5HT7 receptor ligand culminating in the identification of several dual 5-HT1A and 5-HT7 receptor ligands. Compound 16, a butyrophenone derivative of tetrahydroisoquinoline (THIQ), was identified as the most potent agent with low nanomolar binding affinities to both receptors...
August 15, 2016: Bioorganic & Medicinal Chemistry
Dawn Bruijnzeel, Mehdi Yazdanpanah, Uma Suryadevara, Rajiv Tandon
INTRODUCTION: Antipsychotic medications are the foundation of the pharmacological treatment of schizophrenia and lurasidone is the most recent of the 65 agents around the world to become available. In order to use it optimally, it is important to understand its pharmacological and clinical nature and its comparative effectiveness to other antipsychotic agents in the treatment of schizophrenia. AREAS COVERED: Following a comprehensive review of the literature, this article summarizes current information about the pharmacology of lurasidone, data about its short- and long-term efficacy and safety/tolerability in the treatment of schizophrenia, its comparative effectiveness to other antipsychotic agents, and guidance about its optimal use in the treatment of individuals with schizophrenia...
2015: Expert Opinion on Pharmacotherapy
Stephen M Stahl
Vortioxetine is an antidepressant that targets multiple pharmacologic modes of action at sites--or nodes--where serotonergic neurons connect to various brain circuits. These multimodal pharmacologic actions of vortioxetine lead to enhanced release of various neurotransmitters, including serotonin, at various nodes within neuronal networks.
April 2015: CNS Spectrums
L Samalin, M Ben Gharbia, M Garnier, P-M Llorca
Lurasidone is a new second-generation antipsychotic approved in October 2010 by the Food and Drug Administration and in March 2014 by the European Medicines Agency for the treatment of schizophrenia. Like other second-generation antipsychotics, lurasidone is an antagonist of D2 dopamine and 5HT2A serotonin receptors, but differs from the other second-generation antipsychotics in its action profile for certain receptors. Lurasidone is the second-generation antipsychotic with the greatest affinity for 5HT7 receptors and has a low affinity for α1 and α2C-adrenergic and 5HT2C serotonin receptors, and no affinity for histaminergic H1 or muscarinic M1 receptors...
December 2014: L'Encéphale
Gabriela Rusu, F Mitu, Cătălina Elena Lupuşoru, M Nechifor, R V Lupuşoru, Liliana Mititelu-Tarţău
AIM: To investigate the effects of two serotonin receptor antagonists on spontaneous behavior in rats. MATERIAL AND METHOD: The experiment was carried out on white male Wistar rats (150-200g) divided into 3 groups of 6 animals each, treated intraperitoneally with the same volume of solution as follows: Group I (Control): saline solution 0.1 ml/10 g weight; Group II (SB-269970): SB-269970 1 mg/kbw; Group III (NAN-190): NAN-190 1 mg/kbw. The effects of serotonin receptor antagonists on the spontaneous psychomotor skills of rats were tested in Actimeter LE-8811 (PanLab)...
July 2014: Revista Medico-chirurgicală̆ a Societă̆ţ̜ii de Medici ş̧i Naturaliş̧ti Din Iaş̧i
Paulina S Rojas, David Neira, Mauricio Muñoz, Sergio Lavandero, Jenny L Fiedler
Serotonin (5-HT) production and expression of 5-HT receptors (5-HTRs) occur early during prenatal development. Recent evidence suggests that, in addition to its classical role as a neurotransmitter, 5-HT regulates neuronal connectivity during mammalian development by modulating cell migration and neuronal cytoarchitecture. Given the variety of 5-HTRs, researchers have had difficulty clarifying the specific role of each receptor subtype in brain development. Signalling mediated by the G-protein-coupled 5-HT1A R and 5-HT7 R, however, has been associated with neuronal plasticity...
August 2014: Journal of Neuroscience Research
Aparna Chitta, Sree Kanth Sivan, Vijjulatha Manga
To understand the structural requirements of 5-hydroxytryptamine (5HT7) receptor inhibitors and to design new ligands against 5HT7 receptor with enhanced inhibitory potency, a three-dimensional quantitative structure-activity relationship study with comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) for a data set of 56 molecules consisting of oxindole, tetrahydronaphthalene, aryl ketone substituted arylpiperazinealkylamide derivatives was performed. Derived model showed good statistical reliability in terms of predicting 5HT7 inhibitory activity of the molecules, based on molecular property fields like steric, electrostatic, hydrophobic, hydrogen bond donor and hydrogen bond acceptor fields...
June 2014: Journal of Receptor and Signal Transduction Research
Nicholas Patocka, Nidhi Sharma, Mohammed Rashid, Paula Ribeiro
Serotonin is an important neuroactive substance in all the parasitic helminths. In Schistosoma mansoni, serotonin is strongly myoexcitatory; it potentiates contraction of the body wall muscles and stimulates motor activity. This is considered to be a critical mechanism of motor control in the parasite, but the mode of action of serotonin is poorly understood. Here we provide the first molecular evidence of a functional serotonin receptor (Sm5HTR) in S. mansoni. The schistosome receptor belongs to the G protein-coupled receptor (GPCR) superfamily and is distantly related to serotonergic type 7 (5HT7) receptors from other species...
January 2014: PLoS Pathogens
J L Klotz, G E Aiken, J M Johnson, K R Brown, L P Bush, J R Strickland
Pharmacologic profiling of serotonin (5HT) receptors of bovine lateral saphenous vein has shown that cattle grazing endophyte-infected (Neotyphodium coenophialum) tall fescue (Lolium arundinaceum) have altered responses to ergovaline, 5HT, 5HT2A, and 5HT7 agonists. To determine if 5HT receptor activity of tall fescue alkaloids is affected by grazing endophyte-free (EF), wild-type [Kentucky-31 (KY31)], novel endophyte AR542-infected (MAXQ), or novel endophyte AR584-infected (AR584) tall fescue, contractile responses of lateral saphenous veins biopsied from cattle grazing these different fescue-endophyte combinations were evaluated in presence or absence of antagonists for 5HT2A (ketanserin) or 5HT7 (SB-269970) receptors...
September 2013: Journal of Animal Science
Stephen M Stahl, Clara Lee-Zimmerman, Sylvia Cartwright, Debbi Ann Morrissette
The current generation of antidepressant drugs acts predominantly by targeting the serotonin transporter (SERT). The original trend to do this selectively (e.g., with SSRIs or selective serotonin reuptake inhibitors) has given way to combining various additional pharmacologic mechanisms with SERT inhibition, including dual actions by single drugs (e.g., SNRIs or serotonin norepinephrine reuptake inhibitors), or by augmenting SSRIs with a second drug of a different mechanism (e.g., bupropion with dopamine and norepinephrine reuptake inhibition; trazodone with 5HT2A antagonism; mirtazapine with 5HT2A/5HT2C/5HT3/alpha2 antagonism; buspirone or some atypical antipsychotics with 5HT1A partial agonism; other atypical antipsychotics with 5HT2C/5HT7 antagonism and other mechanisms)...
May 1, 2013: Current Drug Targets
Núria Cruz, Eduard Vieta
DEVELOPMENT: Asenapine, recently marketed in United States and ready to be so in Europe, is a multimodal action second-generation antipsychotic, with high affinity for multiple dopaminergic (D2, D3 y D4), serotonergic (5HT2A, 5HT2B, 5HT2C, 5HT6 and 5HT7) and adrenergic (α1A, α2A, α2B and α2C) receptors. Asenapine has to be administered sublingually. After going through succesfully the preliminary phases of development, several clinical trials have been completed in two main indications: schizophrenia and mania...
April 2011: Revista de Psiquiatrí́a y Salud Mental
Shambria F Nolan, Marian W Roman
Lurasidone is a new atypical antipsychotic that has demonstrated positive effects on psychosis, mood, and cognition. This improved efficacy and safety profile for the treatment of schizophrenia. Its overall tolerability profile seems to be comparable to the other atypical antipsychotics. Perhaps its more potent blockade on the 5HT7 receptor will give it more of an advantage in treating the negative symptoms as well as improve cognitive and depressive symptoms associated with schizophrenia. Additionally, it does not appear to have any significant adverse impact on the metabolic profile, such as weight, glucose, or lipid metabolism...
May 2012: Issues in Mental Health Nursing
Aparna Chitta, Mohan Babu Jatavath, Sabiha Fatima, Vijjulatha Manga
To study the pharmacophore properties of quinazolinone derivatives as 5HT(7) inhibitors, 3D QSAR methodologies, namely Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) were applied, partial least square (PLS) analysis was performed and QSAR models were generated. The derived model showed good statistical reliability in terms of predicting the 5HT(7) inhibitory activity of the quinazolione derivative, based on molecular property fields like steric, electrostatic, hydrophobic, hydrogen bond donor and hydrogen bond acceptor fields...
February 2012: Journal of Receptor and Signal Transduction Research
Shrinivas K Kulkarni, Ashish Dhir
BACKGROUND: The World Health Organization (WHO) report has predicted that major depression will become a key cause of illness-induced disability by the year 2020, second only to ischemic heart diseases. OBJECTIVES/METHODS: Although a large number of antidepressant drugs (from monoamine oxidase inhibitors and tricyclic antidepressants to dual reuptake inhibitors) are available for treatment of the disease, approximately 30% of patients failed to respond to this therapy...
June 2009: Expert Opinion on Investigational Drugs
Reto M Agosti
Serotonin was the first neurotransmitter believed to be involved in cephalic pain transfer forward to the cortex, but the precise mechanism was confirmed only after sumatriptan, a 5-HT(1B/1D0) high affinity agonist, was introduced in the acute treatment of migraine. Although very efficient for migraine relief, activation of 5-HT(1B) receptor may also cause vasoconstriction outside brain, within the heart arteries for example. Unlike 5-HT(1B), the 5-HT(1D) receptor is not located in vascular tissues but exclusively within neuronal, but high affinity agonists for 5-HT(1D) failed to prove clinical significance in randomized trials...
August 2007: CNS & Neurological Disorders Drug Targets
Colin J Suckling, John A Murphy, Abedawn I Khalaf, Sheng-ze Zhou, Dimitris E Lizos, Albert Nguyen van Nhien, Hiroshi Yasumatsu, Allan McVie, Louise C Young, Corinna McCraw, Peter G Waterman, Brian J Morris, Judith A Pratt, Alan L Harvey
Chronic low-dose treatment of rats with the psychomimetic drug, phencyclidine, induces regionally specific metabolic and neurochemical changes in the CNS that mirror those observed in the brains of schizophrenic patients. Recent evidence suggests that drugs targeting serotoninergic and muscarinic receptors, and in particular 5-HT(7) antagonists and M(4) agonists, exert beneficial effects in this model of schizophrenia. Compounds that display this combined pattern of activity we refer to as serominic compounds...
May 1, 2007: Bioorganic & Medicinal Chemistry Letters
Najam A Sharif, Michelle Senchyna
PURPOSE: To determine the relative density and tissue localization of mRNAs for serotonin (5-hydroxytryptamine; 5HT) receptor subtypes in human ocular tissues and correlate with their possible functions in the eye. METHODS: Total RNA was extracted from human ocular tissues samples from multiple donors and transcribed into cDNA. An optimized reverse transcriptase polymerase chain reaction (RT-PCR) procedure was then used to amplify the signals using primers designed against human 5HT receptor cDNAs...
2006: Molecular Vision
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