Results 231 to 240 of about 770,157 (273)

Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for alpha radionuclide therapy

Nuclear Medicine and Biology, 2015
Sigma receptors are overexpressed in a variety of human tumors, making them potential targets for radionuclide receptor therapy. We have previously synthesized and evaluated (131)I-labeled (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol [(+)-[(131)I]pIV], which has a high affinity for sigma receptors.
Kazuma Ogawa, Yoshiaki Mizuno, Kohshin Washiyama, Kazuhiro Shiba, Naruto Takahashi, Takashi Kozaka, Shigeki Watanabe, Atsushi Shinohara, Akira Odani   +8 more
openaire   +2 more sources

High specific activity tritium labelling of some sigma-1 receptor agonists

Journal of Radioanalytical and Nuclear Chemistry, 2011
The high specific activity tritiation of (+)-SKF-10,047 (1) and N,N-dimethyltryptamine (4) is described. [N-allyl-3H] (+)-SKF-10,047 (3) was prepared by Lindlar catalyst tritiation of (+)-N-propargylnormetazocine (2) and [N-methyl-3H] N,N-dimethyltryptamine (6) was synthesized by the alkylation of N-methyltryptamine (5) with [3H] methyl iodide.
David G. Ahern, Richard J. Seguin, Crist N. Filer   +2 more
openaire   +1 more source

Synthesis and evaluation of [18F] labeled benzamides: High affinity sigma receptor ligands for PET imaging

Nuclear Medicine and Biology, 1997
We have synthesized and characterized four new fluorinated halobenzamides as sigma receptor ligands for use with positron emission tomography (PET). All the compounds were found to have high sigma-1 affinities (Ki = 0.38-0.98 nM), and the 4-fluoro-substituted benzamides were found to be more potent sigma-2 ligands (Ki = 3.77-4.02 nM) than their ...
C S, Dence, C S, John, W D, Bowen, M J, Welch   +3 more
openaire   +2 more sources

Differential labeling of dopamine and sigma sites by [3H]nemonapride and [3H]raclopride in postmortem human brains

Brain Research, 1997
The difference between the binding of [3H]nemonapride and [3H]raclopride has been used to quantify dopamine D4 receptors in postmortem schizophrenic brain studies. Recent work, however, has suggested that at least part of the differential between [3H]nemonapride and [3H]raclopride binding may represent sigma rather than D4 receptor sites.
S W, Tang, D M, Helmeste, H, Fang, M, Li, R, Vu, W, Bunney, S, Potkin, E G, Jones   +7 more
openaire   +2 more sources

[Concentration, purification, and isotopic labeling of sigma virus].

Comptes rendus hebdomadaires des seances de l'Academie des sciences. Serie D: Sciences naturelles, 1975
Sigma virus has been concentrated by means of polyethylene-glycol and diafiltration; the latter method is more efficient in preserving infectivity. When purified on sucrose gradient, sigma banded in a sharp peak without any polydispersion. We are now able to label sigma genome with 3H-uridine in Drosophila cell cultures.
J, Bernard, A M, Petitjean
openaire   +1 more source

Formal Analysis of an Airplane Accident in $N{\it \Sigma}$ -Labeled Calculus

2009
$N{\it \Sigma}$-labeled calculus is a formal system for representation, verification and analysis of time-concerned recognition, knowledge, belief and decision of humans or computer programs together with related external physical or logical phenomena.In this paper, a formal verification and analysis of the JAL near miss accident is presented as an ...
Tetsuya Mizutani, Shigeru Igarashi, Yasuwo Ikeda, Masayuki Shio   +3 more
openaire   +2 more sources

[3H]opipramol labels a novel binding site and sigma receptors in rat brain membranes.

Molecular Pharmacology, 1991
Opipramol (OP), a clinically effective antidepressant with a tricyclic structure, is inactive as an inhibitor of biogenic amine uptake. [3H]Opipramol binds saturably to rat brain membranes (apparent KD = 4 nM, Bmax = 3 pmol/mg of protein). [3H]Opipramol binding can be differentiated into haloperidol-sensitive and -resistant components, with Ki values ...
C D, Ferris, D J, Hirsch, B P, Brooks, A M, Snowman, S H, Snyder   +4 more
openaire   +2 more sources

[3H]RS-23597-190, a potent 5-hydroxytryptamine4 antagonist labels sigma-1 but not sigma-2 binding sites in guinea pig brain.

The Journal of Pharmacology and Experimental Therapeutics, 1994
Recent findings have suggested a relationship between 5-hydroxytryptamine (5-HT)4 receptors and sigma binding sites. To test this idea, the affinity of 5-HT4 receptor ligands for sigma binding sites was examined. In contrast to the 5-HT4 receptor ligands BIMU-1 [endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3- dihydro-3-ethyl-2-oxo-1H-benzimidazole-1-
D W, Bonhaus, D N, Loury, L B, Jakeman, S A, Hsu, Z P, To, E, Leung, K D, Zeitung, R M, Eglen, E H, Wong   +8 more
openaire   +2 more sources

18F-Labeled indole-based analogs as highly selective radioligands for imaging sigma-2 receptors in the brain

Bioorganic & Medicinal Chemistry, 2017
We have designed and synthesized a series of indole-based σ2 receptor ligands containing 5,6-dimethoxyisoindoline or 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline as pharmacophore. In vitro competition binding assays showed that all ten ligands possessed low nanomolar affinity (Ki=1.79-5.23nM) for σ2 receptors and high subtype selectivity (Ki (σ2)/Ki ...
Liang Wang, Jiajun Ye, Yingfang He, Winnie Deuther-Conrad, Jinming Zhang, Xiaojun Zhang, Mengchao Cui, Jörg Steinbach, Yiyun Huang, Peter Brust, Hongmei Jia   +10 more
openaire   +2 more sources

Development of a Tc-99m labeled sigma-2 receptor-specific ligand as a potential breast tumor imaging agent

Nuclear Medicine and Biology, 2001
A novel in vivo imaging agent, 99mTc labeled [(N-[2-((3'-N'-propyl-[3,3,1]aza-bicyclononan-3alpha-yl)(2"-methoxy-5-methyl-phenylcarbamate)(2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato] technetium(V) oxide), [99mTc]2, displaying specific binding towards sigma-2 receptors was prepared and characterized.
S R, Choi, B, Yang, K, Plössl, S, Chumpradit, S P, Wey, P D, Acton, K, Wheeler, R H, Mach, H F, Kung   +8 more
openaire   +2 more sources