Refine
Has Fulltext
- yes (45)
Is part of the Bibliography
- yes (45)
Year of publication
- 1982 (45) (remove)
Document Type
- Journal article (45) (remove)
Keywords
- Anorganische Chemie (4)
- Chemie (4)
- Biochemie (3)
- Organische Chemie (3)
- Differential effects of stressors (2)
- Healthy subjects (2)
- Physiologische Chemie (2)
- Psychologie (2)
- Tranquillizer (2)
- X-ray (2)
- structure-activity relationships (2)
- 0 antigen (1)
- Activation (1)
- Amphibian oocytes (1)
- Anxiolysis (1)
- Archäologie (1)
- Bordeiella pertussis (1)
- Carcinogenesis (1)
- Covalent binding index - Diethylstilbestrol (1)
- DNA binching (1)
- Dextran sulphate (1)
- Electron microscopy (1)
- Estrogen (1)
- Eukaryoten (1)
- Examination (1)
- Group dynamics (1)
- Hormone (1)
- Lampbrush chromosomes (1)
- Lebendgebärende Zahnkarpfen (1)
- Macrophage (1)
- Medizin (1)
- Mouse (1)
- Neurobiologie (1)
- Physiologie (1)
- Protein-Tyrosin-Kinasen (1)
- Salmonella typhimurium (1)
- Schwertkärpfling (1)
- Social stress (1)
- Social stress situations (1)
- Telemetry (1)
- Telemetry Activation (1)
- Toxicity ; plasmids (1)
- Toxikologie (1)
- Transcription units (1)
- adenosine (1)
- conformational anaylses (1)
- curare-lik activity (1)
- gene-cloning (1)
- histamine release (1)
- human lung (1)
- mast cells (1)
- pharmacological activity (1)
- sila-analogues of Nifedipine derivatives (1)
- silicon compounds (1)
Institute
- Theodor-Boveri-Institut für Biowissenschaften (13)
- Institut für Anorganische Chemie (10)
- Institut für Psychologie (bis Sept. 2007) (5)
- Institut für Organische Chemie (4)
- Institut für Molekulare Infektionsbiologie (3)
- Neurochirurgische Klinik und Poliklinik (3)
- Institut für Pharmakologie und Toxikologie (2)
- Institut für Altertumswissenschaften (bis Sept. 2007) (1)
- Institut für Psychologie (1)
- Klinik und Poliklinik für Allgemein-, Viszeral-, Gefäß- und Kinderchirurgie (Chirurgische Klinik I) (1)
The potentially curare-like silicon compounds 8a- 8f were synthesized and investigated with respect to their structure-activity relationships. The conformations of the compounds in the solid state and in solution were studied by X-ray diffraction analysis (8a- 8e) and IR NMR spectroscopy (8a- 8f), respectively. The muscle relaxing properties of 8a- 8f were investigated on the mouse. The observed structure-activity relationships are not in accordance with the classical "14 Å model" for neuromuscular blocking agents.
In the course of systematic studies on sila-substituted drugs the nifedipine-like 1.4-dihydropyridine derivatives 4a, 4b and 4c were prepared and investigated with respect to sila-substitution effects. By X-ray diffraction analyses 4a, 4b and 4c were found to be isostructural. The C/Si-analogues exhibit similar spasmolytic activities (in vitro, guinea pig ileum), comparable with that of nifedipine. However, the compounds differ substantially in their in vivo activity, as measured by the antihypertensive effect on the renal-hypertensive rat. The experimental results are discussed with respect to the carbon/silicon exchange.
The actions of adenosine on histamine release of human lung fragments were investigated. Histamine release was stimulated either with the calcium ionophore A 23187 orwith concanavalin A. Adenosine and its analogue 5'-N-ethylcarboxamidoadenosine alone had no significant effect on basal release or on the release elicited by A 23187 or concanavalin A. However, in the presence of the adenosine receptor antagonist 8-[4-[[[[(2-aminoethyl)amino]-carbonyl] methyloxy]-phenyl]-1,3-dipropylaxanthine (XAC), which itself did not affect the release, adenosine increased the stimulated histamine release. On the other hand, in the presence of the nucleoside transport inhibitor S-(p-nitrobenzyl)-6-thioninosine (NBTI), adenosine caused a reduction in stimulated histamine release. NBTI itself caused a stimulation of release. Thus, a stimulatory effect of adenosine was seen in the presence ofXAC, whereas an inhibitory effect was unmasked by NBTI. From these data it is concluded that adenosine exerts two opposing effects on histamine release in the human lung which neutralize each other: it inhibits release via a si te antagonized by XAC, which presumably represents an A2 adenosine receptor, and it stimulates release via a mechanism that is blocked by NBTI, suggesting that adenosine needs to reach the interior of cells to exert this effect. The slight stimulatory effect of NBTI alone demonstrates that trapping intracellularly formed adenosine inside mast cells leads to sufficient concentrations of adenosine to stimulate histamine release. These findings suggest an important bimodal role of adenosine in regulating histamine release in the human lung.
The expression in eukaryotes of a tyrosine kinase which is reactive with pp60v-src antibodies
(1982)
All specimens of Eumetazoa and Parazoa, ranging from mammals, birds, teleosts, sharks, lampreys, amphioxus, insects, down to sponges showed the pp60c-src associated kinase activity, indicating that c-src, which is the cellular homologue of the oncogene v-src of Rous sarcoma virus (RSV) is probably present in all multicellular animals. Protozoa and plants did not show pp60c-src: kinase activity.
The degree of c-src expression depends on the taxonomic rank of the Eumetazoa tested, and is organ-specific with nervaus tissues displaying the highest kinase activities. In the central nervous system of mammals and birds we found a high c-src expression, and in that of the lampreys, amphioxus, and insects the lowest. Unexpectedly, total extracts of sponges showed an amount of pp60c-src kinase activity similar to that of brain cell extracts of mammals and birds. These findings suggest that pp60c-src is a phylogenetic old protein that might have evolved together with the multicellular organisation of Metazoa, and that might be of importance in proliferation and differentiation of nontransformed cells.
Prostag1andin F\(_{2\alpha}\) (PGF\(_{2\alpha}\)) is one of the most common metabo1ites of arachidonic acid (M) in rat brain. When administered intracerebroventricularly (i.c.v.) to rats, both AA and PGFal exert dose-related hypertensive, tachycardic and hyperthermic effects. Metabolie alterations in the endogenaus formation of some prostaglandins in the brain-stem of spontaneously hypertensive rats (SHR) have been reported. Therefore the central effects of AA and PGF \(_{2\alpha}\) on blood pressure, heart rate and body temperature were studied both in SHR and nonootensive Wistar rats (NR) under urethane-anaesthesia. The hypertensive effect of AA i.c.v. (0.01-100 \(\mu\)g/rat) was larger in magni tude in SHR than in NR, but there was no significant difference in the M-induced changes of heart rate and body temperature between the groups. Pretreatment of NR wi th soditm1 :meclofenamate (1 mg/rat i.c.v.) antagonised the central effects of M indicating that these effects are not due to M itself but to its conversion to prostaglandins. Unlike the effects of AA, the central hypertensive, tachycardic and hyperthennic responses to PGF\(_{2\alpha}\) (0.5-50 l-lg/rat i.c.v .) were significantly attenuated in SHR. The present results obtained with M are conpatible with the previous assumption that the synthesis of prostaglandins in the brain of SHR might differ from that in NR. The results also demonstrate that the central effects of PGF\(_{2\alpha}\) are reduced in SHR.