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5-HT (1E )

Petr Jirásek, Sabine Amslinger, Jörg Heilmann
A strategy for the synthesis of natural and non-natural 5-deoxy-6,7-dihydrocurcuminoids (diarylheptanoids) was developed for the preparation of 14 compounds with varying aromatic substituent patterns and a different functionality in the aliphatic seven-carbon chain. The in vitro protective activity against glutamate-induced neuronal cell death was examined in the murine hippocampal cell line HT-22 to find structural motifs responsible for neuroprotective effects in vitro. Among the tested compounds the ferulic acid-like unit, present in the structures of (E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hept-1-en-3-one (5) and (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)hept-1-en-3-one (7), appeared to be an important feature for protection against glutamate-induced neurotoxicity...
October 24, 2014: Journal of Natural Products
Min Hong, Honglin Geng, Meiju Niu, Fei Wang, Dacheng Li, Jifeng Liu, Handong Yin
Five organotin(IV) compounds were synthesized from N'-[(1E)-(2-hydroxy-3-methoxyphenyl)methylidene]pyridine-4-carbohydrazone and the corresponding dialkyltin(IV) or trialkyltin(IV) precursor. Solid state structures were determined by IR, elemental analysis, NMR spectroscopy, and for 1, 2, 4 and 5 single crystal X-ray diffraction analysis. Compounds 1, 2 and 4 are monomers with the tin atoms five-coordinated in distorted trigonal bipyramid, of which the deprotonated Schiff base ligand chelate to tin center in the enolic tridentate mode...
October 30, 2014: European Journal of Medicinal Chemistry
Hitoshi Watanabe, Ryo Saito, Tatsuya Nakano, Hideyuki Takahashi, Yu Takahashi, Keisuke Sumiyoshi, Katsuyoshi Sato, Xiangning Chen, Natsumi Okada, Shunsuke Iwasaki, Dian W Harjanti, Natsumi Sekiguchi, Hiroaki Sano, Haruki Kitazawa, Michael T Rose, Shyuichi Ohwada, Kouichi Watanabe, Hisashi Aso
In mice, peripheral 5-HT induces an increase in the plasma concentrations of glucose, insulin and bile acids, and a decrease in plasma triglyceride, NEFA and cholesterol concentrations. However, given the unique characteristics of the metabolism of ruminants relative to monogastric animals, the physiological role of peripheral 5-HT on glucose and lipid metabolism in sheep remains to be established. Therefore, in this study, we investigated the effect of 5-HT on the circulating concentrations of metabolites and insulin using five 5-HT receptor (5HTR) antagonists in sheep...
2014: PloS One
Michael Ried, Tobias Potzger, Reiner Neu, Zsolt Sziklavari, Tamas Szöke, Andreas Liebold, Hans-Stefan Hofmann, Markus Hoenicka
PURPOSE: Both sildenafil and bosentan have been used clinically to treat pulmonary arterial hypertension. As these substances target different pathways to modulate vasoconstriction, we investigated the combined effects of both drug classes in isolated human pulmonary vessels. METHODS: Segments of pulmonary arteries (PA) and veins (PV) were harvested from 51 patients undergoing lobectomy. Contractile force was determined isometrically in an organ bath. Vessels were constricted with norepinephrine (NE) to determine effects of sildenafil...
February 2014: Cardiovascular Drugs and Therapy
Ifeoma I Ulasi, Shay Tzur, Walter G Wasser, Revital Shemer, Etty Kruzel, Elena Feigin, Chinwuba K Ijoma, Obinna D Onodugo, Julius U Okoye, Ejikeme B Arodiwe, Ngozi A Ifebunandu, Chinwe J Chukwuka, Cajetan C Onyedum, Uchenna N Ijoma, Emmanuel Nna, Macaulay Onuigbo, Saharon Rosset, Karl Skorecki
BACKGROUND: Continental Africa is facing an epidemic of chronic kidney disease (CKD). APOL1 risk variants have been shown to be strongly associated with an increased risk for non-diabetic kidney disease including HIV nephropathy, primary non-monogenic focal and segmental glomerulosclerosis, and hypertension-attributed nephropathy among African ancestry populations in the USA. The world's highest frequencies of APOL1 risk alleles have been reported in West African nations, overlapping regions with a high incidence of CKD and hypertension...
2013: Nephron. Clinical Practice
Saobo Lei
The entorhinal cortex (EC) is considered as the gate to control the flow of information into and out of the hippocampus. The EC is important for numerous physiological functions such as emotional control, learning and memory and pathological disorders including Alzheimer's disease, schizophrenia and temporal lobe epilepsy. Serotonin is a classical neurotransmitter which may modify these physiological functions and pathology of neurological diseases. The EC receives profuse serotonergic innervations from the raphe nuclei in the brainstem and expresses high density of serotonergic receptors including 5-HT(1A), 5-HT(1D), 5-HT(1E), 5-HT(2A), 5-HT(3) and 5-HT(6)...
2012: International Journal of Physiology, Pathophysiology and Pharmacology
Dongfeng Zhang, Zengchang Pang, Shuxia Li, Wenjie Jiang, Shaojie Wang, Mads Thomassen, Jacob V B Hjelmborg, Torben A Kruse, Kirsten Ohm Kyvik, Kaare Christensen, Gu Zhu, Qihua Tan
Elevated pulse pressure (PP) is associated with cardiovascular disorders and mortality in various populations. The genetic influence on PP has been confirmed by heritability estimates using related individuals. Recently, efforts have been made by mapping genes that are linked to the phenotype. We report the results of our gene mapping studies conducted in the Chinese population in mainland China. The genome-wide linkage and association scans were carried out on 63 middle-aged dizygotic twin pairs using high-density markers...
November 2012: Hypertension Research: Official Journal of the Japanese Society of Hypertension
Wen-Hua Wei, Gib Hemani, Attila Gyenesei, Veronique Vitart, Pau Navarro, Caroline Hayward, Claudia P Cabrera, Jennifer E Huffman, Sara A Knott, Andrew A Hicks, Igor Rudan, Peter P Pramstaller, Sarah H Wild, James F Wilson, Harry Campbell, Nicholas D Hastie, Alan F Wright, Chris S Haley
We surveyed gene-gene interactions (epistasis) in human body mass index (BMI) in four European populations (n<1200) via exhaustive pair-wise genome scans where interactions were computed as F ratios by testing a linear regression model fitting two single-nucleotide polymorphisms (SNPs) with interactions against the one without. Before the association tests, BMI was corrected for sex and age, normalised and adjusted for relatedness. Neither single SNPs nor SNP interactions were genome-wide significant in either cohort based on the consensus threshold (P=5...
August 2012: European Journal of Human Genetics: EJHG
M T Klein, M Teitler
BACKGROUND AND PURPOSE: The 5-ht(1E) receptor is highly expressed in the human brain and its structure is conserved in humans, suggesting an important physiological role for 5-ht(1E) receptors. However, neither the function nor the distribution of this receptor has been characterized in the mammalian brain. EXPERIMENTAL APPROACH: Rats and mice lack the 5-ht(1E) receptor gene; thus, we used guinea pig brain tissue and immunofluorescent staining techniques to provide the first specific localization of 5-ht(1E) receptors in the mammalian brain...
June 2012: British Journal of Pharmacology
Kazuya Otake, Satoru Azukizawa, Masaki Fukui, Kazuyoshi Kunishiro, Hikaru Kamemoto, Mamoru Kanda, Tomohiro Miike, Masayasu Kasai, Hiroaki Shirahase
A novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and (S)-2-[(2E,4E)-hexadienoyl]-7-(2-{5-methyl-2-[(1E)-5-methylhexen-1-yl]oxazol-4-yl}ethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14i) was identified as a potent human peroxisome proliferator-activated receptor γ (PPARγ) selective agonist (EC(50)=0.03 μM) and human protein-tyrosine phosphatase 1B (PTP-1B) inhibitor (IC(50)=1.18 μM). C(max) after oral administration of 14i at 10mg/kg was 2.2 μg/ml (4...
January 15, 2012: Bioorganic & Medicinal Chemistry
Sonja Kössler, Charity Nofziger, Martin Jakab, Silvia Dossena, Markus Paulmichl
Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1E,6E-heptadiene-3,5-dione or diferuloyl methane) is a polyphenol derived from the Curcuma longa plant, commonly known as turmeric. This substance has been used extensively in Ayurvedic medicine for centuries for its anti-oxidant, analgesic, anti-inflammatory and antiseptic activity. More recently curcumin has been found to possess anti-cancer properties linked to its pro-apoptotic and anti-proliferative actions. The underlying mechanisms of these diverse effects are complex, not fully elucidated and subject of intense scientific debate...
February 26, 2012: Toxicology
Simon Lobsiger, Hans-Martin Frey, Samuel Leutwyler, Philip Morgan, David Pratt
We report the analysis of the S1<--S0 rotational band contours of jet-cooled 5-methyl-2-hydroxypyrimidine (5M2HP), the enol form of deoxythymine. Unlike thymine, which exhibits a structureless spectrum, the vibronic spectrum of 5M2HP is well structured, allowing us to determine the rotational constants and the methyl group torsional barriers in the S0 and S1 states. The 0(0)(0), 6a(0)(1), 6b(0)(1), and 14(0)(1) band contours were measured at 900 MHz (0.03 cm(-1)) resolution using mass-specific two-color resonant two-photon ionization (2C-R2PI) spectroscopy...
November 24, 2011: Journal of Physical Chemistry. A
Michael T Klein, Małgorzata Dukat, Richard A Glennon, Milt Teitler
The 5-hydroxytryptamine (5-HT) 1E receptor is highly expressed in the human frontal cortex and hippocampus, and this distribution suggests the function of 5-HT(1E) receptors might be linked to memory. To test this hypothesis, behavioral experiments are needed. Because rats and mice lack a 5-HT(1E) receptor gene, knockout strategies cannot be used to elucidate this receptor's functions. Thus, selective pharmacological tools must be developed. The tryptamine-related agonist BRL54443 [5-hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole] is one of the few agents that binds 5-HT(1E) receptors with high affinity and some selectively; unfortunately, it binds equally well to 5-HT(1F) receptors (K(i) ≈ 1 nM)...
June 2011: Journal of Pharmacology and Experimental Therapeutics
Eric Mick, James J McGough, Frank A Middleton, Benjamin Neale, Stephen V Faraone
OBJECTIVE: We conducted a genome-wide association study of blood pressure in an open-label study of the methylphenidate transdermal system (MTS) for the treatment of attention-deficit/hyperactivity disorder (ADHD). METHOD: Genotyping was conducted with the Affymetrix Genome-Wide Human SNP Array 6.0. Multivariate association analyses were conducted using the software package PLINK. After data cleaning and quality control we tested 316,934 SNPs in 140 children with ADHD...
March 30, 2011: Progress in Neuro-psychopharmacology & Biological Psychiatry
C Falciani, B Lelli, J Brunetti, S Pileri, A Cappelli, A Pini, C Pagliuca, N Ravenni, L Bencini, S Menichetti, R Moretti, M De Prizio, M Scatizzi, L Bracci
The aim of this study was to demonstrate that oligo-branched peptides can be effective either for spotlighting tumor cells that overexpress peptide receptors, or for killing them, simply by exchanging the functional moiety coupled to the conserved receptor-targeting core. Tetra-branched peptides containing neurotensin (NT) sequence are described here as selective targeting agents for human colon, pancreas and prostate cancer. Fluorophore-conjugated peptides were used to measure tumor versus healthy tissue binding in human surgical samples, resulting in validation of neurotensin receptors as highly promising tumor-biomarkers...
November 2010: Current Cancer Drug Targets
V Granados-Soto, C F Argüelles, H I Rocha-González, B Godínez-Chaparro, F J Flores-Murrieta, C M Villalón
This study assessed the possible antinociceptive role of peripheral 5-HT(1) receptor subtypes in the rat formalin test. Rats were injected into the dorsum of the hind paw with 50 microl of diluted formalin (1%). Nociceptive behavior was quantified as the number of flinches of the injected paw. Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of the 5-HT(1) receptor agonists R(+)-UH-301 (5-HT(1A); 0.1-3 microg/paw), CGS-12066A (5-HT(1B); 0...
January 20, 2010: Neuroscience
Michael T Klein, Milt Teitler
Recent studies have indicated that the serotonin [5-hydroxytryptamine (5-HT)] 1E receptor, originally discovered in human brain tissue, is not expressed in rat or mouse brain. Thus, there have been few reports on 5-HT(1E) receptor drug development. However, expression of 5-HT(1E) receptor mRNA has been shown in guinea pig brain. To establish this species as an animal model for 5-HT(1E) drug development, we identified brain regions that exhibit 5-carboxyamidotryptamine, ritanserin, and LY344864 - insensitive [(3)H]5-HT binding (characteristic of the 5-HT(1E) receptor)...
April 2009: Journal of Neurochemistry
Calvin K Y Chan, Judith C Mak, Ricky Y K Man, Paul M Vanhoutte
Rho kinase is involved in the pathogenesis of hypertension, which favors the occurrence of endothelium-dependent contractions. The present study was designed to determine the effects of two Rho kinase inhibitors, HA1077 [1-(5-isoquinolinesulfonyl)-homopiperazine (fasudil)] and Y27632 [(+)-(R)-trans-4-(1-aminoethyl)-N-(4-pyridyl) cyclohexane carboxamide dihydrochloride], on endothelium-dependent and -independent contractions. Isometric tension of 1-year-old spontaneously hypertensive rat and Wistar Kyoto aortae were measured...
May 2009: Journal of Pharmacology and Experimental Therapeutics
Tsuyoshi Tsujimura, Jun Nagamine, Eiji Sugaru, Tsutomu Nakagawa, Michiko Ono-Kishino, Teruhisa Tokunaga, Makoto Kitoh, Ryu Nagata, Mutsuo Taiji
BACKGROUND/AIMS: Chronic kidney disease (CKD) is the common cause of end-stage renal disease. Antihypertensive agents are clinically used to inhibit the progression of CKD. However, these agents cannot completely prevent progression to renal failure. We have previously reported that 5-chloro-2-{(1E)-3-[2-(4-methoxybenzoyl)-4-methyl-1H- pyrrol-1-yl]prop-1en-1-yl}-N-(methylsulfonyl)benzamide (SMP-534) improves renal disease and prevents the production of extracellular matrix in vitro. Additionally, SMP-534 inhibits glomerular fibrosis and provides renoprotection in vivo...
2008: Nephron. Experimental Nephrology
Niels H Jensen, Ramona M Rodriguiz, Marc G Caron, William C Wetsel, Richard B Rothman, Bryan L Roth
Quetiapine is an atypical antipsychotic drug that is also US FDA approved for treating bipolar depression, albeit by an unknown mechanism. To discover the potential mechanism for this apparently unique action, we screened quetiapine, its metabolite N-Desalkylquetiapine, and dibenzo[b,f][1,4]thiazepine-11(10-H)-one (DBTO) against a large panel of G-protein-coupled receptors, ion channels, and neurotransmitter transporters. DBTO was inactive at all tested molecular targets. N-Desalkylquetiapine had a high affinity (3...
September 2008: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
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