Search results for "Biological activity"

Impairment of intracellular antiviral defense with age: age-dependent changes in expression of interferon-induced and double-stranded RNA-activated 2…

1995

The 2',5'-oligoadenylate (2-5A) system is involved in the defense of mammalian cells against virus infection. In a previous study [25], we demonstrated that the activities of the enzymes which synthesize and degrade 2-5A [2-5A synthetase (2-5OAS) and 2',3'-exoribonuclease] and of the enzyme that is activated by 2-5A (ribonuclease L) change during aging and development in different tissues of rat. The age-dependent decrease in 2-5OAS activity and increase in 2-5A nuclease activity results in a decrease in the cellular 2-5A content, suggesting that the efficiency of the antiviral 2-5A system is impaired in aged rats. Here we determined the age-dependent changes in the level of mRNA coding for…

Pharmacological intervention in age-associated brain disorders by Flupirtine: Alzheimer’s and Prion diseases

1998

Alzheimer's disease, a major form of dementia in the elderly has become an increasingly important health problem in developed countries. In vitro studies on primary neurons demonstrate that Flupirtine (Katadolon) at a concentration of 1 microg/ml, significantly reduces the neurotoxic (apoptotic) effect displayed by A beta25-35, a segment of the amyloid beta-protein precursor the etiologic agent of Alzheimer's disease. Flupirtine, which has been in clinical use since 10 years ago, prevents the toxic effect of PrP, the presumed etiologic agent of the Creutzfeldt-Jakob disease as well as the excitatory amino acid glutamate on cortical neurons. Flupirtine displays a bimodal activity. Its strong…

Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.

2009

The beta-adrenergic agonist 1 (zilpaterol) is used as production enhancer in cattle. Binding experiments of separated enantiomers on recombinant human beta(2)-adrenergic and mu-opioid receptors and functional studies showed that the (-)-1 enantiomer accounts for essentially all the beta(2)-adrenergic agonist activity and that it exhibits less affinity toward the mu-opioid receptor than (+)-1, which is a mu-opioid receptor antagonist. X-ray crystallography revealed the absolute configuration of (-)-1 to be 6R,7R.

Darstellung und H2-agonistische Aktivität alkylsubstituierter 3-(Imidazol-4-yl)propylguanidine Synthesis and H2-Agonistic Activity of Alkyl-3-(imidaz…

1987

Derivate des 3-(Imidazol-4-yl)propylguanidins mit einem Methyl- oder einem 2-(Ethylthio)ethyl-Substituenten2) an der Guanidin-Gruppe weisen am H2-Rezeptor des Meerschweinchenvorhofs nur 10–20% der Histaminaktivitat auf. Dagegen fuhrt die Substitution mit der H2-affinen 2-[(5-Methylimidazol-4-yl) methylthio]ethyl-Gruppierung zu Impromidin, einem hochpotenten H2-Agonisten.

Racemische Histamin-H1-Agonisten

1984

Es wurden racemische α- und β-methylverzweigte 2-(2-Aminoethyl)-thiazole und 2-(2-Aminoethyl)-imidazole (Isohistamine) dargestellt und auf Histamin-H1- und -H2-agonistische Aktivitat gepruft. Histamine Analogues, XXVI: Racemic Histamine H1-Agonists Racemic α or β-methylated 2-(2-aminoethyl)thiazoles and 2-(2-aminoethyl)imidazoles (isohistamines) were prepared and tested for histamine H1- and H2-agonistic activity.

Histaminanaloge, 27. Mitt. Bis (2,2′-histamine)

1985

Es wurden p-Phenylen-bis(2,2′-histamin) (6a), Ethylen-bis(2,2′-histamin) (6b), Tetramethylen-bis(2,2′-histamin) (6c) und Hexamethylen-bis(2,2′-histamin) (6d) dargestellt und auf Histamin-H1-und H2-agonistische Aktivitat untersucht. Histamine Analogues, XXVII: Bis(2,2′-histamines) p-Phenylenebis(2,2′-histamine) (6a), ethylenebis(2,2′-histamine) (6b), tetramethylenebis(2,2′-histamine) (6c), and hexamethylenebis(2,2′-histamine) (6d) were prepared and tested for histamine H1,-and H2-agonistic activity.

Biologically Active Organic Compounds, Especially Plant Promoters, in Algae Extracts and Their Potential Application in Plant Cultivation

2015

Synthesis of polyfluoroalkyl sp2-iminosugar glycolipids and evaluation of their immunomodulatory properties towards anti-tumor, anti-leishmanial and …

2019

Immunomodulatory glycolipids, among which α-galactosylceramide (KRN7000) is an iconic example, have shown strong therapeutic potential in a variety of conditions ranging from cancer and infection to autoimmune or neurodegenerative diseases. A main difficulty for those channels is that they often provoke a cytokine storm comprising both pro- and anti-inflammatory mediators that antagonize each other and negatively affect the immune response. The synthesis of analogues with narrower cytokine secretion-inducing capabilities is hampered by the intrinsic difficulty at controlling the stereochemical outcome in glycosidation reactions, particularly if targeting the α-anomer, which seriously hamper…

Histaminanaloge, 28. Mitt. 2-Aryloxyalkyl- und 2-Aminoalkylhistamine

1987

Als Histaminderivate mit H1-affinitatsvermittelnden Strukturelementen in 2-Stellung des Imidazolrings wurden 2-Aryloxyalkyl- und 2-Aminoalkylhistamine sowie das racemische 2-(1-Phenylethyl)histamin dargestellt und auf Histamin-H1-agonistische Aktivitat untersucht. Histamine Analogues, XXVIII: 2-(Aryloxyalkyl)- and 2-(Aminoalkyl)histamines As histamine derivatives with structures at position 2 of the imidazole ring, which mediate H1-receptor affinity, 2-(aryloxyalkyl)- and 2-(aminoalkyl)histamines as well as racemic 2-(1-phenylethyl)histamine were prepared and tested for histamine H1-agonistic activity.

H2-Antihistaminika, 36. Mitt. Isolamtidin und Analoge

1987

Isolamtidin (9a), ein Stellungsisomer des Lamtidins (8a), sowie die analogen N3-substituierten 1-Methyl-1H-1,2,4-triazol-3,5-diamine 9e-i, k wurden durch spezifische Synthese dargestellt und am isolierten Meerschweinchenvorhof und an der histaminstimulierten Sauresekretion der narkotisierten Ratte auf H2-antagonistische Wirkung untersucht. H2-Antihistaminics, XXXVI: Isolamitidine and Analogues Isolamitidine (9a), a position isomer of lamtidine (8a), as well as the analogous N3-substituted 1-methyl-1H-1,2,4-triazole-3,5-diamines 9e-i, k were prepared and tested for H2-antagonistic activity on the isolated guinea-pig atrium and towards the histamine-stimulated acid secretion of the anaestheti…