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5-HT (1B/1D)

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https://www.readbyqxmd.com/read/28581633/population-pharmacokinetic-analysis-of-zolmitriptan-and-its-metabolite-in-adults-and-adolescents-to-support-dose-selection-in-children-with-migraine
#1
Wangda Zhou, Jianguo Li, Bruce Birmingham, Hongmei Xu, Stefan Lillieborg, Diansong Zhou, Nidal Al-Huniti
Zolmitriptan is a serotonin (5-HT) 1B/1D receptor agonist effective for the treatment of migraine. This analysis aimed to develop a population pharmacokinetic (PK) model for zolmitriptan and its active metabolite in adults and adolescents and provide appropriate dosing regimens to be used in clinical trials for children 6-11 years old. The data from a single-dose clinical study of 5.0-mg zolmitriptan nasal spray (ZNS) conducted in adult and adolescent patients with migraine between migraine attacks was applied...
June 5, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28384110/effects-of-the-novel-high-affinity-5-ht-1b-1d-receptor-ligand-frovatriptan-on-the-rat-carotid-artery
#2
Kremena E Saracheva, Natalia A Prissadova, Valentin I Turiiski, Valeri I Slavchev, Atanas D Krastev, Damianka P Getova
BACKGROUND: In blood vessels 5-HT stimulates sympathetic nerves, the endothelium and vascular smooth muscle cells. Triptans are specific anti-migraine drugs and they activate the serotoninergic 5HT1b/d receptors causing vasoconstriction of the cerebral vessels. AIM: To evaluate the effect of frovatriptan on isolated rat carotid artery. METHODS: Contractile activity of the preparations was registered isometrically. Krebs solution (pH = 7.4) was used for washing smooth muscle (SM) preparations aerated with 95% O2 and 5% CO2 at 37°C...
March 1, 2017: Folia Medica
https://www.readbyqxmd.com/read/28343185/frameworking-memory-and-serotonergic-markers
#3
Alfredo Meneses
The evidence for neural markers and memory is continuously being revised, and as evidence continues to accumulate, herein, we frame earlier and new evidence. Hence, in this work, the aim is to provide an appropriate conceptual framework of serotonergic markers associated with neural activity and memory. Serotonin (5-hydroxytryptamine [5-HT]) has multiple pharmacological tools, well-characterized downstream signaling in mammals' species, and established 5-HT neural markers showing new insights about memory functions and dysfunctions, including receptors (5-HT1A/1B/1D, 5-HT2A/2B/2C, and 5-HT3-7), transporter (serotonin transporter [SERT]) and volume transmission present in brain areas involved in memory...
March 27, 2017: Reviews in the Neurosciences
https://www.readbyqxmd.com/read/28201962/preparation-and-optimization-of-fast-dissolving-film-of-naratriptan-hydrochloride
#4
Krishna D Koradia, Pradip T Sidhdhapara, Navin R Sheth
BACKGROUND AND OBJECTIVE: Naratriptan is second-generation triptan class of antimigraine drug which selectively bind with 5-HT(1B/1D) receptor. It is widely used to treat the migraine attack due to its better tolerability and lower recurrence rate as compared to other triptans. Despite of the applicability, Naratriptan also have several drawback like slow onset of action and fist pass metabolism which reduce its efficacy. In order to increase the efficacy of naratriptan fast dissolving film is prepared...
February 12, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/27984097/anti-allodynic-effect-of-mangiferin-in-neuropathic-rats-involvement-of-nitric-oxide-cyclic-gmp-atp-sensitive-k-channels-pathway-and-serotoninergic-system
#5
Antonio Espinosa de Los Monteros-Zuñiga, Teresa Izquierdo, Geovanna Nallely Quiñonez-Bastidas, Héctor Isaac Rocha-González, Beatriz Godínez-Chaparro
The neurobiology of neuropathic pain is caused by injury in the central or peripheral nervous system. Recent evidence points out that mangiferin shows anti-nociceptive effect in inflammatory pain. However, its role in inflammatory and neuropathic pain and the possible mechanisms of action are not yet established. The purpose of this study was to determine the possible anti-allodynic effect of mangiferin in rats with spinal nerve ligation (SNL). Furthermore, we sought to investigate the possible mechanisms of action that contribute to these effects...
October 28, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/26588618/the-effect-of-zolmitriptan-on-cardiac-autonomic-modulation-in-patients-with-migraine-a-double-blind-placebo-controlled-crossover-study
#6
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
https://www.readbyqxmd.com/read/26168890/role-of-spinal-5-ht5a-and-5-ht1a-1b-1d-receptors-in-neuropathic-pain-induced-by-spinal-nerve-ligation-in-rats
#7
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
https://www.readbyqxmd.com/read/25993836/development-and-validation-of-uv-spectrophotometric-method-to-study-stress-degradation-behaviour-of-rizatriptan-benzoate
#8
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
https://www.readbyqxmd.com/read/25490985/genome-wide-association-study-for-grain-yield-and-related-traits-in-an-elite-spring-wheat-population-grown-in-temperate-irrigated-environments
#9
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
https://www.readbyqxmd.com/read/25476970/in-vivo-occupancy-of-the-5-ht1a-receptor-by-a-novel-pan-5-ht1-a-b-d-receptor-antagonist-gsk588045-using-positron-emission-tomography
#10
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
https://www.readbyqxmd.com/read/25324526/multidrug-toxicity-involving-sumatriptan
#11
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
https://www.readbyqxmd.com/read/25288493/human-%C3%AE-1-adrenoceptor-subtype-selectivity-of-substituted-homobivalent-4-aminoquinolines
#12
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
https://www.readbyqxmd.com/read/24678459/preparation-and-evaluation-of-sublingual-tablets-of-zolmitriptan
#13
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
https://www.readbyqxmd.com/read/24318669/emerging-targets-in-migraine
#14
REVIEW
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
https://www.readbyqxmd.com/read/24311349/vortioxetine-first-global-approval
#15
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
https://www.readbyqxmd.com/read/24213881/pharmacological-characterization-of-n1-2-methoxyphenyl-n4-hexylpiperazine-as-a-multi-target-antagonist-of-%C3%AE-1a-%C3%AE-1d-adrenoceptors-and-5-ht1a-receptors-that-blocks-prostate-contraction-and-cell-growth
#16
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
https://www.readbyqxmd.com/read/24192548/vasopressin-induced-constriction-of-the-isolated-rat-occipital-artery-is-segment-dependent
#17
COMPARATIVE STUDY
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
https://www.readbyqxmd.com/read/24016840/serotonergic-receptor-mechanisms-underlying-antidepressant-like-action-in-the-progesterone-withdrawal-model-of-hormonally-induced-depression-in-rats
#18
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
https://www.readbyqxmd.com/read/23994595/peripheral-and-spinal-5-ht-receptors-participate-in-the-pronociceptive-and-antinociceptive-effects-of-fluoxetine-in-rats
#19
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
https://www.readbyqxmd.com/read/23912626/sumatriptan-iontophoretic-transdermal-system-a-review-of-its-use-in-patients-with-acute-migraine
#20
REVIEW
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
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