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5-HT (1B/1D)

Celal Kilit, Serdar Oruc, Turkan Pasali Kilit, Ersel Onrat
BACKGROUND: Triptans, which activate 5-hydroxytryptamine (5-HT)-1B/1D receptors in cerebral arteries, are very effective in aborting attacks of migraine. Although activation of 5-HT-1B/1D receptors diminishes the secretion of noradrenaline from cardiac sympathetic nerves, some studies report that they may cause chest discomfort, myocardial infarction and arrhythmias due to coronary vasospasm. The effect of zolmitriptan on cardiac autonomic modulation has not been evaluated in migraineurs...
November 2015: Neurology India
Sabino Hazael Avila-Rojas, Isabel Velázquez-Lagunas, Ana Belen Salinas-Abarca, Paulino Barragán-Iglesias, Jorge Baruch Pineda-Farias, Vinicio Granados-Soto
Serotonin (5-HT) participates in pain modulation by interacting with different 5-HT receptors. The role of 5-HT5A receptor in neuropathic pain has not previously studied. The purpose of this study was to investigate: A) the role of 5-HT5A receptors in rats subjected to spinal nerve injury; B) the expression of 5-HT5A receptors in dorsal spinal cord and dorsal root ganglia (DRG). Neuropathic pain was induced by L5/L6 spinal nerve ligation. Tactile allodynia in neuropathic rats was assessed with von Frey filaments...
October 5, 2015: Brain Research
Kempwade Amolkumar, Taranalli Ashok, Jadhav Kiran
Rizatriptan benzoate is a 5 HT 1B/1D receptor agonist which is prescribed for the treatment of migraine. In the present study new, simple, specific ultraviolet spectrophotometric method for rizatriptan benzoate was developed and validated. Forced degradation studies were carried out in acidic, alkaline and neutral pH conditions. The absorbance maxima peak was found to be 224 nm and linearity was observed in the concentration range of 0. 5-2. 5 µg . mL-1 with regression coefficient value of 0. 998 8. The method was validated and found to be precise...
January 2015: Guang Pu Xue Yu Guang Pu Fen Xi, Guang Pu
Sivakumar Sukumaran, Susanne Dreisigacker, Marta Lopes, Perla Chavez, Matthew P Reynolds
Through genome-wide association study, loci for grain yield and yield components were identified in chromosomes 5A and 6A in spring wheat (Triticum aestivum). Genome-wide association study (GWAS) was conducted for grain yield (YLD) and yield components on a wheat association mapping initiative (WAMI) population of 287 elite, spring wheat lines grown under temperate irrigated high-yield potential condition in Ciudad Obregón, Mexico, during four crop cycles (from 2009-2010 to 2012-2013). The population was genotyped with high-density Illumina iSelect 90K single nucleotide polymorphisms (SNPs) assay...
February 2015: TAG. Theoretical and Applied Genetics. Theoretische und Angewandte Genetik
Robert A Comley, Jasper van der Aart, Balázs Gulyás, Martine Garnier, Laura Iavarone, Christer Halldin, Eugenii A Rabiner
5-hydroxytryptamine 1 (5-HT1) receptor blockade in combination with serotonin reuptake inhibition may provide a more rapid elevation of synaptic 5-HT compared to serotonin reuptake alone, by blocking the inhibitory effect of 5-HT1 receptor activation on serotonin release. GSK588045 is a novel compound with antagonist activity at 5-HT1A/1B/1D receptors and nanomolar affinity for the serotonin transporter, which was in development for the treatment of depression and anxiety. Here we present the results of an in vivo assessment of the relationship between plasma exposure and 5-HT1A receptor occupancy...
May 2015: Neuropharmacology
Jessica L Knittel, Shawn P Vorce, Barry Levine, Rhome L Hughes, Thomas Z Bosy
A multidrug fatality involving sumatriptan is reported. Sumatriptan is a tryptamine derivative that acts at 5-HT(1B/1D) receptors and is used for the treatment of migraines. The decedent was a 21-year-old white female found dead in bed by her spouse. No signs of physical trauma were observed and a large number of prescription medications were discovered at the scene. Toxicological analysis of the central blood revealed sumatriptan at a concentration of 1.03 mg/L. Following therapeutic dosing guidelines, sumatriptan concentrations do not exceed 0...
January 2015: Journal of Analytical Toxicology
Junli Chen, Adrian P Campbell, Kaniz F Urmi, Laurence P G Wakelin, William A Denny, Renate Griffith, Angela M Finch
A series of ring-substituted ethyl- and heptyl-linked 4-aminoquinoline dimers were synthesized and evaluated for their affinities at the 3 human α(1)-adrenoceptor (α(1)-AR) subtypes and the human serotonin 5-HT(1A)-receptor (5-HT(1A)-R). We find that the structure-specificity profiles are different for the two series at the α(1)-AR subtypes, which suggests that homobivalent 4-aminoquinolines can be developed with α(1)-AR subtype selectivity. The 8-methyl (8-Me) ethyl-linked analogue has the highest affinity for the α(1A)-AR, 7 nM, and the greatest capacity for discriminating between α(1A)-AR and α(1B)-AR (6-fold), α(1D)-AR (68-fold), and the 5-HT(1A)-R (168-fold)...
November 1, 2014: Bioorganic & Medicinal Chemistry
Shailesh T Prajapati, Manoj V Patel, Chhaganbhai N Patel
AIM: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. MATERIALS AND METHODS: Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study...
January 2014: International Journal of Pharmaceutical Investigation
Jan Hoffmann, Peter J Goadsby
Migraine is a common and highly disabling neurological disorder. Despite the complexity of its pathophysiology, substantial advances have been achieved over the past 20 years in its understanding, as well as the development of pharmacological treatment options. The development of serotonin 5-HT(1B/1D) receptor agonists ("triptans") substantially improved the acute treatment of migraine attacks. However, many migraineurs do not respond satisfactorily to triptans and cardiovascular co-morbidities limit their use in a significant number of patients...
January 2014: CNS Drugs
Andrew Gibb, Emma D Deeks
Vortioxetine is an orally administered small molecule developed by Lundbeck A/S for the once-daily treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD). Vortioxetine received its first global approval for MDD in the USA in September 2013 and regulatory approval for its use in this indication in the EU (where it has received a positive opinion) and Canada is awaited. The drug is a bis-aryl-sulphanyl amine compound that combines serotonin (5-HT) reuptake inhibition with other characteristics, including receptor activity modulation...
January 2014: Drugs
Fernanda Chagas-Silva, Jéssica Barbosa Nascimento-Viana, Luiz Antonio S Romeiro, Luana C Barberato, François Noël, Claudia Lucia Martins Silva
Benign prostatic hyperplasia (BPH) is a progressive disease related to the imbalance of cell growth and apoptosis, and it plays a key role in the development of lower urinary tract symptoms (LUTS). The main pharmacological treatment is based on α1A-adrenoceptor blockers, but in several cases monotherapy has failed. Recent studies of prostate pathophysiology have noted the role of α1D-adrenoceptors and 5-HT1A receptors in prostate cell proliferation in addition to the usual role of α1A-adrenoceptors in prostate contraction...
March 2014: Naunyn-Schmiedeberg's Archives of Pharmacology
Stephen P Chelko, Chad W Schmiedt, Tristan H Lewis, Stephen J Lewis, Tom P Robertson
BACKGROUND: Circulating factors delivered to the nodose ganglion (NG) by the occipital artery (OA) have been shown to affect vagal afferent activity, and thus the contractile state of the OA may influence blood flow to the NG. METHODS: OA were isolated and bisected into proximal and distal segments relative to the external carotid artery. RESULTS: Bisection highlighted stark differences between maximal contractile responses and OA sensitivity...
2013: Journal of Vascular Research
Yan Li, Kasper F Raaby, Connie Sánchez, Maria Gulinello
Hormonally induced mood disorders such as premenstrual dysphoric disorder (PMDD) are characterized by a range of physical and affective symptoms including anxiety, irritability, anhedonia, social withdrawal and depression. Studies demonstrated rodent models of progesterone withdrawal (PWD) have a high level of constructive and descriptive validity to model hormonally-induced mood disorders in women. Here we evaluate the effects of several classes of antidepressants in PWD female Long-Evans rats using the forced swim test (FST) as a measure of antidepressant activity...
November 1, 2013: Behavioural Brain Research
C Cervantes-Durán, H I Rocha-González, V Granados-Soto
The role of 5-HT receptors in fluoxetine-induced nociception and antinociception in rats was assessed. Formalin produced a typical pattern of flinching and licking/lifting behaviors. Local peripheral ipsilateral, but not contralateral, pre-treatment with fluoxetine (0.3-3 nmol/paw) increased in a dose-dependent fashion 0.5% formalin-induced nociception. In contrast, intrathecal pretreatment with fluoxetine (0.3-3 nmol/rat) prevented nociception induced by formalin. The peripheral pronociceptive effect of fluoxetine was prevented by the 5-HT2A (ketanserin, 3-10 pmol/paw), 5-HT2B (3-(2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl)-2,4(1H,3H)-quinazolinedione(+) tartrate, RS-127445, 3-10 pmol/paw), 5-HT2C (8-[5-(2,4-dimethoxy-5-(4-trifluoromethylphenylsulphonamido) phenyl-5-oxopentyl]1,3,8-triazaspiro[4...
November 12, 2013: Neuroscience
Karly P Garnock-Jones
The sumatriptan iontophoretic transdermal system (ZECUITY®) [hereafter referred to as sumatriptan TDS] is the first transdermal treatment for migraine to be approved by the US FDA. This article reviews the available pharmacologic properties of sumatriptan TDS and its clinical efficacy and tolerability for the acute treatment of adult patients with migraine with or without aura. Sumatriptan, a selective 5-hydroxy-tryptamine receptor subtype 1 (5-HT₁) agonist, is presumed to exert its therapeutic effect on migraine patients by binding to the 5-HT(1B/1D) receptors on intracranial blood vessels and sensory nerves of the trigeminal system, resulting in cranial vessel constriction and the inhibition of the release of pro-inflammatory neuropeptides and plasma extravasation...
September 2013: Drugs
Martha B Ramírez Rosas, Sieneke Labruijere, Carlos M Villalón, Antoinette Maassen Vandenbrink
INTRODUCTION: The introduction of the triptans (5-hydroxytryptamine (5-HT)1B/1D receptor agonists) was a great improvement in the acute treatment of migraine. However, shortcomings of the triptans have prompted research on novel serotonergic targets for the treatment of migraine. AREAS COVERED: In this review the different types of antimigraine drugs acting at 5-HT receptors, their discovery and development are discussed. The first specific antimigraine drugs were the ergot alkaloids, consisting of ergotamine, dihydroergotamine and methysergide, which are agonists at 5-HT receptors, but can also bind α-adrenoceptors and dopamine receptors...
August 2013: Expert Opinion on Pharmacotherapy
Jian-Pu Zheng, Xuemei Zhang, Hao Wang, Yunman Wang, Zhuoan Cheng, Peihao Yin, Wen Peng
Cyclosporin A (CsA) is a widely used immunosuppressive agent that also causes hypertension. However, the molecular basis for CsA-induced hypertension remains elusive. In this study, we established an in vitro model for CsA-induced pathological changes in vasculature. Rat mesenteric arteries were incubated with CsA for 24 hr in an organ culture system. Both vasocontraction and vasorelaxation in mesenteric artery were studied using myograph technology, and mRNA expressions of the contractile receptors were determined by real-time PCR...
December 2013: Basic & Clinical Pharmacology & Toxicology
Jean-Philippe Guilloux, Indira Mendez-David, Alan Pehrson, Bruno P Guiard, Christelle Repérant, Sophie Orvoën, Alain M Gardier, René Hen, Bjarke Ebert, Silke Miller, Connie Sanchez, Denis J David
Vortioxetine (Lu AA21004) is an investigational novel antidepressant with multimodal activity that functions as a 5-HT3, 5-HT7 and 5-HT(1D) receptor antagonist, 5-HT(1B) receptor partial agonist, 5-HT(1A) receptor agonist and inhibitor of the 5-HT transporter in vitro. Here we explore its anxiolytic and antidepressant potential in adult mice. Vortioxetine was assessed in BalB/cJ@RJ mice using the open-field and forced-swim tests (acute: p.o. 1 h, repeated: daily p.o. 21 days), and in 129S6/SvEvTac mice using the novelty suppressed feeding paradigm (acute: p...
October 2013: Neuropharmacology
Kenneth J Broadley, Martina Fehler, William R Ford, Emma J Kidd
Trace amines including β-phenylethylamine (β-PEA) and amphetamines classically exert pharmacological actions via indirect sympathomimetic mechanisms. However, there is evidence for other mechanisms and this study explores the receptors mediating vasoconstriction in rat aorta. β-PEA, d-amphetamine, MDMA, cathinone and methylphenidate caused concentration-dependent contractions of rat isolated aortic rings which were unaffected by prazosin (1 μM), ICI-118,551 (1 μM), cocaine (10 μM) and pargyline (10 μM), to inhibit α1- and β2-adrenoceptors, neuronal transport and monoamine oxidase (MAO), respectively...
September 5, 2013: European Journal of Pharmacology
Atul R Mahableshwarkar, Paula L Jacobsen, Yinzhong Chen
OBJECTIVE: Vortioxetine (Lu AA21004) is an investigational antidepressant. In vitro studies indicate that vortioxetine is a 5-HT(3), 5-HT(7), and 5-HT(1D) receptor antagonist, 5-HT(1B) receptor partial agonist, 5-HT(1A) receptor agonist and inhibitor of the 5-HT transporter. This trial assessed the efficacy and tolerability of 2.5 and 5 mg vortioxetine for the treatment of MDD. RESEARCH DESIGN AND METHODS: Adults (N = 611) with MDD were randomized to 8 weeks of double-blind treatment with placebo, vortioxetine (2...
March 2013: Current Medical Research and Opinion
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