Opioid and sigma receptor studies. New developments in the design of selective sigma ligands

2001 ◽  
Vol 73 (9) ◽  
pp. 1499-1509 ◽  
Author(s):  
Giuseppe Ronsisvalle ◽  
Agostino Marrazzo ◽  
Orazio Prezzavento ◽  
Alfredo Cagnotto ◽  
Tiziana Mennini ◽  
...  
Keyword(s):  
Racemic Mixture ◽  
Trans Isomers ◽  
New Developments ◽  
In Vivo Test ◽  
Inhibiting Effect ◽  
D1 And D2 Receptors ◽  
Selective Ligand ◽  
Sigma Ligands ◽  
Very High

New racemic and chiral methyl 2-{[4-(4-chlorophenyl)-4-hydroxypiperi-din-1-yl]methyl}-1-phenylcyclopropanecarboxylate derivatives were synthesized in order to obtain sigma ligands with increased affinity and selectivity compared to (+)-MPCB and haloperidol. The cis-(±)-7 racemic mixture showed a better binding affinity and selectivity than the (±)-8 trans isomers. Between the two cis enantiomers, (+)-7, with configuration (1R,2S), showed a very high affinity and the best selectivity for s1. All compounds synthesized (7­9) showed a reduced or negligible affinity for opioid and dopaminergic D1 and D2 receptors. Nociceptive in vivo test confirms that (+)-7 (namely MR200), such as non-selective antagonist haloperidol, increased the analgesic effect induced by the k opioid selective ligand U50,488H and reversed the inhibiting effect of (+)-pentazocine on analgesia.

Defibrotide Inhibits Platelet Activation by Cathepsin G Released From Stimulated Polymorphonuclear Leukocytes

1992 ◽  
Vol 67 (06) ◽  
pp. 660-664 ◽  
Author(s):  
Virgilio Evangelista ◽  
Paola Piccardoni ◽  
Giovanni de Gaetano ◽  
Chiara Cerletti
Keyword(s):  
Platelet Activation ◽  
Polymorphonuclear Leukocytes ◽  
Direct Interaction ◽  
Cathepsin G ◽  
In Vivo Test ◽  
Cell Functions ◽  
Test Models ◽  
Antithrombotic Effects

SummaryDefibrotide is a polydeoxyribonucleotide with antithrombotic effects in experimental animal models. Most of the actions of this drug have been observed in in vivo test models but no effects have been reported in in vitro systems. In this paper we demonstrate that defibrotide interferes with polymorphonuclear leukocyte-induced human platelet activation in vitro. This effect was not related to any direct interaction with polymorphonuclear leukocytes or platelets, but was due to the inhibition of cathepsin G, the main biochemical mediator of this cell-cell cooperation. Since cathepsin G not only induces platelet activation but also affects some endothelial cell functions, the anticathepsin G activity of defibrotide could help to explain the antithrombotic effect of this drug.

Effects of Heparin Oligosaccharides with High Affinity for Antithrombin III in Experimental Venous Thrombosis

1982 ◽  
Vol 47 (03) ◽  
pp. 244-248 ◽  
Author(s):  
D P Thomas ◽  
Rosemary E Merton ◽  
T W Barrowcliffe ◽  
L Thunberg ◽  
U Lindahl
Keyword(s):  
Antithrombin Iii ◽  
Specific Activity ◽  
High Specific Activity ◽  
Factor Xa ◽  
Blood Levels ◽  
Thrombin Time ◽  
High Affinity ◽  
Very High

SummaryThe in vitro and in vivo characteristics of two oligosaccharide heparin fragments have been compared to those of unfractionated mucosal heparin. A decasaccharide fragment had essentially no activity by APTT or calcium thrombin time assays in vitro, but possessed very high specific activity by anti-Factor Xa assays. When injected into rabbits at doses of up to 80 ¼g/kg, this fragment was relatively ineffective in impairing stasis thrombosis despite producing high blood levels by anti-Xa assays. A 16-18 monosaccharide fragment had even higher specific activity (almost 2000 iu/mg) by chromogenic substrate anti-Xa assay, with minimal activity by APTT. When injected in vivo, this fragment gave low blood levels by APTT, very high anti-Xa levels, and was more effective in preventing thrombosis than the decasaccharide fragment. However, in comparison with unfractionated heparin, the 16-18 monosaccharide fragment was only partially effective in preventing thrombosis, despite producing much higher blood levels by anti-Xa assays.It is concluded that the high-affinity binding of a heparin fragment to antithrombin III does not by itself impair venous thrombogenesis, and that the anti-Factor Xa activity of heparin is only a partial expression of its therapeutic potential.

Comparative Evaluation of In Vitro and In Vivo Assays for the Detection of Avian Infectious Bronchitis Virus as a Contaminant of Live Poultry Vaccines

1998 ◽  
Vol 26 (5) ◽  
pp. 629-634
Author(s):  
Emiliana Falcone ◽  
Edoardo Vignolo ◽  
Livia Di Trani ◽  
Simona Puzelli ◽  
Maria Tollis
Keyword(s):  
Infectious Bronchitis Virus ◽  
Serological Response ◽  
Avian Infectious Bronchitis Virus ◽  
Animal Testing ◽  
Rt Pcr ◽  
Pcr Assay ◽  
In Vivo Test ◽  
Infectious Bronchitis

A reverse transcriptase polymerase chain reaction (RT-PCR) assay specific for identifying avian infectious bronchitis virus (IBV) in poultry vaccines, and the serological response to IBV induced by the inoculation of chicks with a Newcastle disease vaccine spiked with the Massachusetts strain of IBV, were compared for their ability to detect IBV as a contaminant of avian vaccines. The sensitivity of the IBV-RT-PCR assay provided results which were at least equivalent to the biological effect produced by the inoculation of chicks, allowing this assay to be considered a valid alternative to animal testing in the quality control of avian immunologicals. This procedure can easily be adapted to detect a number of contaminants for which the in vivo test still represents the only available method of detection.

scholarly journals Wafer-Scale Fabrication and Assembly Method of Multichannel Microelectrode Arrays for ECoG Application

Electronics ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 316
Author(s):  
Cong Wang ◽  
Yu-Chen Wei ◽  
Ho-Kun Sung ◽  
Alok Kumar ◽  
Zhong-Liang Zhou ◽  
...  
Keyword(s):  
Printed Circuit Boards ◽  
Electrochemical Impedance ◽  
Microelectrode Arrays ◽  
Absence Seizure ◽  
Curing Conditions ◽  
Wafer Scale ◽  
In Vivo Test ◽  
Assembly Method ◽  
Signal Recording

High density electrocorticography (ECoG)-based microelectrode arrays (MEAs) are fabricated to timely record the neural activities to provide the fundamental understanding in neuroscience and biomedical engineering. This paper aims to introduce a device-based concept and wafer-scale fabrication process for MEAs. Flexible and biocompatible polyimide is applied on MEAs to bear all possible stress and strain. Detailed fabrication key techniques, including surface treatment, polyimide stability measurement, evaporation process, and curing conditions, have been discussed thoroughly. Moreover, the fabricated polyimide-based MEAs are surface-mounted on well-packaged printed circuit boards (PCBs) via a slot-type connector without any additional wire bonding to make the signal recording process easier. An absence seizure was recorded during the in vivo test, which shows the availability of signal recording based on the presented MEAs. The proposed MEAs could be remained at the skull, while the connector and PCBs can be disassembled apart. Therefore, the testing sample will get less suffering. To verify the robustness of the fabricated MEAs, the impedance properties were characterized using electrochemical impedance spectroscopy. The measured results indicate an average impedance of 12.3 ± 0.675 kΩ at 1 kHz. In total, 10 groups of MEAs were sample tested, and over 90% of the total 60 channels per 1-MEAs operated efficiently.

scholarly journals Defect structures of sodium and chloride co-substituted hydroxyapatite and its osseointegration capacity

2021 ◽  
Vol 56 (9) ◽  
pp. 5493-5508
Author(s):  
Dong Su Yoo ◽  
Jung Sang Cho ◽  
Yong-Chae Chung ◽  
Sang-Hoon Rhee
Keyword(s):  
Binding Energies ◽  
Dissolution Behavior ◽  
Total System ◽  
Carbonate Apatite ◽  
In Vivo Test ◽  
Co Substitution ◽  
Constituent Elements ◽  
Low Crystalline ◽  
Charged Point

AbstractA defect structure and osseointegration capacity of sodium and chloride co-substituted hydroxyapatite (NaClAp) were newly studied. The NaClAp was prepared by reacting H3PO4 and Ca(OH)2 with NaNO3 and NH4Cl followed by sintering; pure hydroxyapatite (HAp) was synthesized as a control. After sintering, the co-substitution of Ca and OH with Na and Cl, respectively, produced charged point defects at Ca and PO4 sites. Also, OH molecules partially adopted a head-on structure. The calculated total system energy of NaClAp was higher, whereas the binding energies between each constituent elements and system were lower than those of HAp. These results suggest that NaClAp was less stable than HAp, due to the formation of various defects by co-substitution of Na and Cl. Indeed, NaClAp exhibited higher dissolution behavior in simulated body fluid (SBF) compared with HAp. Accordingly, this increased the capability to produce low crystalline hydroxyl carbonate apatite, likely due to the increasing degree of apatite supersaturation in SBF. Besides, the NaClAp granules showed noticeable improvements in osseointegration capacity four weeks after in vivo test compared with HAp. Collectively, these results imply that the defects made by multiple ion substitutions are useful to increase osseointegration capacity of hydroxyapatite.

scholarly journals Expression and Characterization of the Flocculin Flo11/Muc1, a Saccharomyces cerevisiae Mannoprotein with Homotypic Properties of Adhesion

2007 ◽  
Vol 6 (12) ◽  
pp. 2214-2221 ◽  
Author(s):  
Lois M. Douglas ◽  
Li Li ◽  
Yang Yang ◽  
A. M. Dranginis
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Biofilm Formation ◽  
In Vitro System ◽  
Glycosylphosphatidylinositol Anchor ◽  
Fungal Adhesion ◽  
Very High ◽  
Molecular Weight Form

ABSTRACT The Flo11/Muc1 flocculin has diverse phenotypic effects. Saccharomyces cerevisiae cells of strain background Σ1278b require Flo11p to form pseudohyphae, invade agar, adhere to plastic, and develop biofilms, but they do not flocculate. We show that S. cerevisiae var. diastaticus strains, on the other hand, exhibit Flo11-dependent flocculation and biofilm formation but do not invade agar or form pseudohyphae. In order to study the nature of the Flo11p proteins produced by these two types of strains, we examined secreted Flo11p, encoded by a plasmid-borne gene, in which the glycosylphosphatidylinositol anchor sequences had been replaced by a histidine tag. A protein of approximately 196 kDa was secreted from both strains, which upon purification and concentration, aggregated into a form with a very high molecular mass. When secreted Flo11p was covalently attached to microscopic beads, it conferred the ability to specifically bind to S. cerevisiae var. diastaticus cells, which flocculate, but not to Σ1278b cells, which do not flocculate. This was true for the 196-kDa form as well as the high-molecular-weight form of Flo11p, regardless of the strain source. The coated beads bound to S. cerevisiae var. diastaticus cells expressing FLO11 and failed to bind to cells with a deletion of FLO11, demonstrating a homotypic adhesive mechanism. Flo11p was shown to be a mannoprotein. Bead-to-cell adhesion was inhibited by mannose, which also inhibits Flo11-dependent flocculation in vivo, further suggesting that this in vitro system is a useful model for the study of fungal adhesion.

In vitro and in vivo acetylcholinesterase-inhibiting effect of new classes of organophosphorus compounds

1999 ◽  
Vol 18 (2) ◽  
pp. 241-246 ◽  
Author(s):  
Murat Ozmen ◽  
Sadiye Sener ◽  
Ahmet Mete ◽  
Hasan Kucukbay
Keyword(s):  
Organophosphorus Compounds ◽  
Inhibiting Effect

Matching Therapists' Predicates: An in Vivo Test of Effectiveness

1983 ◽  
Vol 57 (1) ◽  
pp. 207-210 ◽  
Author(s):  
E. Thomas Dowd ◽  
Ann G. Hingst
Keyword(s):  
Neurolinguistic Programming ◽  
Representational System ◽  
In Vivo Test ◽  
Interview Situation ◽  
Rating Form ◽  
Interview Condition ◽  
Student Volunteers ◽  
Counselor Rating ◽  
Evaluation Inventory

The theory of neurolinguistic programming predicts that a therapist's matching of a client's primary representational system, as expressed in the client's predicates, should result in increased therapist's rapport and social influence. This hypothesis was tested in an actual interview situation. Six relatively inexperienced therapists, two each in predicate matching, predicate mismatching, and predicate no-matching conditions, conducted a 30-min. interview with nine undergraduate student volunteers each, for a total of 54 subjects. After the appropriate interview condition was completed, subjects rated their therapists on the Counselor Rating Form and the Counseling Evaluation Inventory. No significant differences among the three conditions on any of the measures were found. Results are compared with those of previous research on assessment and primary representational system matching in analogue situations.

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