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  • 1
    ISSN: 1365-2958
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Biology , Medicine
    Notes: The ccd locus of the F plasmid codes for two gene products, CcdA and CcdB, which contribute to the plasmid's high stability by post-segregational killing of plasmid-free bacteria. Like the quinolones, the CcdB protein is a poison of the DNA-topoisomerase II complexes, while CcdA acts as an antidote against CcdB. in addition to these poison-antipoison properties, the CcdA and CcdB proteins act together at transcription level to repress their own synthesis. In this work, we have isolated, in vivo., and characterized several non-killer CcdB mutants. All missense mutations which inactivate CcdB killer activity are located in the region coding for the last three C-terminal residues. However, the resulting mutant CcdB proteins retain their auto-regulatory properties. We conclude that the last three C-terminal residues of CcdB play a key role in poisoning but are not involved in repressor formation.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Der Onkologe 3 (1997), S. 99-104 
    ISSN: 1433-0415
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
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  • 3
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. The purpose of the present study was to test the effects of synthetic atrial natriuretic peptide (ANP) on renal haemodynamics and excretory capacities of salt and water in the rat during an ‘acute volumic stress’, which was induced by brisk disturbances of the circulatory volume.2. To this end, 29 anaesthetized male Wistar rats were rapidly injected with 1 mL of 0.85% NaCl, repeated twice at 60 s intervals. The injectates contained no ANP (n = 5) or 1 × 0.25 (n = 6), 3 × 0.25 (n = 6), 1 × 2.5 (n = 6) or 3 × 2.5 μg (n = 6) ANP, added to the first injectate only (1 ×) or to each injectate (3 ×). Renal blood flow (RBF) was continuously measured with an electromagnetic flow transducer.3. Renal blood flow increased transiently (approximately 30 s) by approximately 13% (P 〈 0.05) during each injection of saline without ANP. Addition of 0.25 or 2.5 μg ANP to the first injectate enhanced RBF by 21 and 35%, respectively (both P 〈 0.05), but did not modify the time sequence. Furthermore, addition of 0.25 μg ANP to the second and third injectate produced an almost similar change in RBF at the end of each injection (ΔRBF = 20 and 17%, respectively). In contrast, the addition of 2.5 μg ANP to the second and third injectate did not produce the same changes in RBF observed at the end of the first injection. The amplitude of the change in RBF was then similar to the increase in RBF induced by 1 mL saline without ANP. Mean arterial pressure (MAP) did not change significantly during repeated injections of saline alone or with addition of 0.25 μg ANP to the first injectate. However, MAP decreased significantly (by 5, 9 and 9 mmHg) after the injection of 3 × 0.25, 1 × 2.5 or 3 × 2.5 μg ANP, respectively.4. Sodium excretion was rapidly increased from 2.600±0.654 to 9.330±1.322 μmol/min after injection of 3 × 1 mL of 0.85% NaCl (P 〈 0.05). Thereafter, sodium excretion remained enhanced throughout the experiment, so that 70% of the sodium load injected was recovered at the end of the experiment. Atrial natriuretic peptide added to the injectates further elevated the maximal responses in diuresis and natriuresis induced by saline injections without ANP (P 〈 0.001). A maximal effect was observed after the addition of 2.5 μg ANP to the first saline solution. When the amount of sodium excreted was calculated by integrating the areas under the curve of the natriuretic responses, a relationship was established as a function of the amount of ANP added to the saline solutions. It was characterized by a threshold in the presence of 2.5 μg ANP added to the first injectate when the integration period was limited to 4 min 30 s and 14 min 30 s after starting the first injection of the varying test solutions. When the integration period was extended until the end of the experiment (2 h), the amount of sodium excreted in each group was further enhanced, especially after injection of 3 × 1 mL of 0.85% NaCl without ANP or with 1 × 0.25 and 3 × 0.25 μg ANP. Differences in sodium excretion between groups were attenuated (P 〈 0.054, ANOVA).5. In conclusion, our results demonstrate differential effects of synthetic ANP on renal vascular reactivity and excretory capacity. These effects were superimposed on changes induced by acute volumic stress. In particular, effects of saline injections on renal vascular compliance were amplified in the presence of ANP added in varying amounts to the injectates. This amplification was limited to 2.5 μg ANP.
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  • 4
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 378 (1995), S. 68-70 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Investigation of the genetics, gonads, genitalia or hormone level of transsexuals has not, so far, produced any results that explain their status1'2. In experimental animals, however, the same gonadal hormones that prenatally determine the morphology of the genitalia also influence the morphology ...
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  • 5
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] EPR-1 is an activation-dependent molecule of relative molecular mass 62,000 (Mr 62K) which participates in protease-depen-dent mechanisms of lymphocyte co-stimulation8'9. Anti-EPR-1 mAb 2E1 (ref. 8) nearly completely inhibited lymphocyte proliferation in vitro that was stimulated by soluble or ...
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  • 6
    ISSN: 1432-1912
    Keywords: Key words P2X Purinoceptor ; βγ-Methylene-L-ATP ; Rat vagus nerve ; Nodose ganglion neurones ; Rat vas deferens
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  The effects of the putative selective P2X purinoceptor agonist, β,γ-methylene-L-adenosine 5′-triphosphate (βγme-L-ATP), were determined at rat neuronal and smooth muscle P2X purinoceptors. βγMe-L-ATP had no effect on the extracellularly recorded membrane potential of the rat isolated vagus nerve preparation at concentrations up to 300 μM. In contrast, the archetypal P2X purinoceptor agonist, α,β-methylene ATP (αβmeATP; 1–100 μM), produced concentration-related depolarisation responses with a mean EC50 value of 10.8 μM. The depolarising effects of αβmeATP were not attenuated by βγme-L-ATP (100 μM). In voltage clamp experiments on single nodose ganglion neurones, ATP (100 μM), but not βγme-L-ATP (1–300 μM), evoked rapid (〈20 ms onset) inward currents when applied using a concentration-clamp method. In receptor binding studies to rat brain membranes, βγme-D-ATP and αβmeATP competed with high affinity for [3H]αβmeATP binding sites, with mean pIC50 values of 7.7 and 8.3, respectively. However, βγme-L-ATP possessed low affinity for these sites and competed only at concentrations in excess of 10 μM (mean pIC50 value 4.1). In prostatic segments of the rat vas deferens, βγme-L-ATP (1–100 μM) and αβmeATP (0.3–100 μM) each produced concentration-related contractile responses with mean EC50 values of 17.1 and 3.6 μM, respectively. βγMe-L-ATP (1–10 μM) evoked fast inward currents in freshly dispersed vas deferens smooth muscle cells, indicative of an action at ligand-gated ion channels. Binding sites in vas deferens membranes labelled using 1 nM [3H]αβmeATP exhibited high affinity for βγme-L-ATP, αβmeATP and βγme-D-ATP with mean pIC50 values of 7.7, 8.4 and 7.3, respectively. These results indicate that βγme-L-ATP exhibits neither agonist nor antagonist properties at P2X purinoceptors on rat vagal neurones and possesses only very low affinity for [3H]αβmeATP binding sites in rat brain. In contrast, βγme-L-ATP is a potent, high affinity agonist at smooth muscle P2X purinoceptors of the rat vas deferens. This selective agonist action of βγme-L-ATP suggests that P2X purinoceptors in smooth muscle and neurones are different and represent distinct P2X purinoceptor subtypes.
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  • 7
    ISSN: 1432-1912
    Keywords: P2X Purinoceptor ; βγ-Methylene-l-ATP ; Rat vagus nerve ; Nodose ganglion neurones ; Rat vas deferens
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects of the putative selective P2X purinoceptor agonist, β,γ-methylene-l-adenosine 5′-triphosphate (βγme-l-ATP), were determined at rat neuronal and smooth muscle P2X purinoceptors. βγMe-l-ATP had no effect on the extracellularly recorded membrane potential of the rat isolated vagus nerve preparation at concentrations up to 300 μM. In contrast, the archetypal P2X purinoceptor agonist, α, β methylene ATP (αβmeATP;1–100 μM), produced concentration-related depolarisation responses with a mean EC50 value of 10.8 μM. The depolarising effects of αβmeATP were not attenuated by βγme-l-ATP (100 μM). In voltage clamp experiments on single nodose ganglion neurones, ATP (100 μM), but not βγme-l.-ATP (1–300 μM), evoked rapid ( 〈 20 ms onset) inward currents when applied using a concentration-clamp method. In receptor binding studies to rat brain membranes, βγme-d-ATP and αβmeATP competed with high affinity for [3H]Lx βmeATP binding sites, with mean pIC50 values of 7.7 and 8.3, respectively. However, βγme-l-ATP possessed low affinity for these sites and competed only at concentrations in excess of 10 μM (mean pIC50 value 4.1). In prostatic segments of the rat vas deferens, βγme-l-ATP (1–100 μM) and αβmeATP (0.3–100 μM) each produced concentration-related contractile responses with mean EC50 values of 17.1 and 3.6 μM, respectively. βγMe-l-ATP (1–10 μM) evoked fast inward currents in freshly dispersed vas deferens smooth muscle cells, indicative of an action at ligand-gated ion channels. Binding sites in vas deferens membranes labelled using 1 nM [3H]αβmeATP exhibited high affinity for ββ γme-l-ATP, αβmeATP and βγme-d-ATP with mean PIC50 values of 7.7, 8.4 and 7.3, respectively. These results indicate that βγme-l-ATP exhibits neither agonist nor antagonist properties at P2X purinoceptors on rat vagal neurones and possesses only very low affinity for [3H]αβmeATP binding sites in rat brain. In contrast, βγme-l-ATP is a potent, high affinity agonist at smooth muscle P2X purinoceptors of the rat vas deferens. This selective agonist action of βγme-l-ATP suggests that P2X purinoceptors in smooth muscle and neurones are different and represent distinct P2X purinoceptor subtypes.
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  • 8
    ISSN: 1432-1912
    Keywords: Somatostatin ; BIM-23027 ; Rat colonic mucosa ; sst2 receptors ; SRIF-binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We have previously shown that the somatostatin (SRIF) sst2 receptor-selective peptide, BIM-23027, is a potent antisecretory agent in rat isolated distal colonic mucosa (RDCM) and in radioligand binding studies in RDCM membranes, it only maximally inhibited approximately 40% of [125I]-Tyr11-SRIF-14 binding (McKeen ES, Feniuk W, Humphrey PPA (1995) Naunyn-Schmiedeberg's Arch Pharmacol 352:402–411). The aim of this study was to characterise the BIM-23027-sensitive and -insensitive SRIF binding sites in more detail and to compare their properties with those of the recombinant sst2 receptor stably expressed in mouse fibroblast (Ltk−) cells. SRIF-14, SRIF-28, CGP-23996 and D Trp8-SRIF-14 abolished [125I]-Tyr11-SRIF-14 binding (pIC50 values, 8.7–9.7) but the competition curves had Hill slopes which were less than unity. Octreotide and L-362,855 inhibited binding over a wide concentration range (0.1 nM-1 μM) and inhibition of binding was incomplete at the highest concentration studied. BIM-23056 (PIC50 〈6.5) was a weak inhibitor of [125]-Tyr11-SRIF-14 binding. GTPγS decreased [125I]-Tyr11-SRIF-14 binding by 40%. Further binding experiments with [125I]-Tyr11-SRIF-14 were carried out in RDCM in the continuous presence of BIM-23027 (1 μM). Under these conditions, seglitide had no effect on [125I]-Tyr11-SRIF-14 binding at concentrations up to 10 μM, whilst SRIF-14 and SRIF-28 abolished specific [125I]-Tyr11-SRIF-14 binding in a manner which was consistent with the ligand binding to two sites. SRIF-14 and SRIF-28 displayed high affinity (pIC50 values of 9.8 and 9.3 respectively) for approximately 70% of these binding sites and low affinity (pIC50 values of 7.8 and 7.3) for the remaining sites. Octreotide, L-362,855 and BIM-23056 were weak inhibitors of [125I]-Tyr11-SRIF-14 binding (PIC50 〈6.5). [125I]-BIM-23027 labelled a single population of SRIF binding sites in RDCM membranes and mouse fibroblast (Ltk−) cells stably expressing the human recombinant sst2 receptor. There was a significant correlation between the affinitestimates of a range of SRIF analogues at inhibiting [125I]-BIM-23027 binding in RDCM membranes and binding to the recombinant sst2 receptor in Ltk− cells, suggesting that the sites labelled by [125I]-BIM-23027 in RDCM are similar to the sst2 receptor. GTPγS (100 μM) decreased [125I]-BIM-23027 binding in RDCM by 60%. The results from these studies demonstrate that [125I]-Tyr11-SRIF-14 labels a heterogeneous population of high affinity SRIF binding sites in RDCM membranes. The majority of these sites are insensitive to GTPγS and display negligible affinity for the cyclic hexapeptides, BIM-23027 and seglitide. The remaining high affinity binding sites can be selectively labelled with [125I]-BIM-23027, are sensitive to GTPγS and show similar characteristics to the recombinant sst2 receptor which appears to mediate the antisecretory effects of SRIF in the mucosa (McKeen ES, Feniuk W, Humphrey PPA (1995) Naunyn-Schmiedeberg's Arch Pharmacol 352:402–411).
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  • 9
    ISSN: 1432-1912
    Keywords: Key words Somatostatin ; BIM-23027 ; Rat colonic mucosa ; sst2 receptors ; SRIF-binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We have previously shown that the somatostatin (SRIF) sst2 receptor-selective peptide, BIM-23027, is a potent antisecretory agent in rat isolated distal colonic mucosa (RDCM) and in radioligand binding studies in RDCM membranes, it only maximally inhibited approximately 40% of [125I]-Tyr11-SRIF-14 binding (McKeen ES, Feniuk W, Humphrey PPA (1995) Naunyn-Schmiedeberg‘s Arch Pharmacol 352:402–411). The aim of this study was to characterise the BIM-23027-sensitive and -insensitive SRIF binding sites in more detail and to compare their properties with those of the recombinant sst2 receptor stably expressed in mouse fibroblast (Ltk–) cells. SRIF-14, SRIF-28, CGP-23996 and D Trp8-SRIF-14 abolished [125I]-Tyr11-SRIF-14 binding (pIC50 values, 8.7–9.7) but the competition curves had Hill slopes which were less than unity. Octreotide and L-362,855 inhibited binding over a wide concentration range (0.1 nM-1 μM) and inhibition of binding was incomplete at the highest concentration studied. BIM-23056 (pIC50 〈6.5) was a weak inhibitor of [125]-Tyr11-SRIF-14 binding. GTPγS decreased [125I]-Tyr11-SRIF-14 binding by 40%. Further binding experiments with [125I]-Tyr11-SRIF-14 were carried out in RDCM in the continuous presence of BIM-23027 (1 μM). Under these conditions, seglitide had no effect on [125I]-Tyr11-SRIF-14 binding at concentrations up to 10 μM, whilst SRIF-14 and SRIF-28 abolished specific [125I]-Tyr11-SRIF-14 binding in a manner which was consistent with the ligand binding to two sites. SRIF-14 and SRIF-28 displayed high affinity (pIC50 values of 9.8 and 9.3 respectively) for approximately 70% of these binding sites and low affinity (pIC50 values of 7.8 and 7.3) for the remaining sites. Octreotide, L-362,855 and BIM-23056 were weak inhibitors of [125I]-Tyr11-SRIF-14 binding (pIC50 〈6.5). [125I]-BIM-23027 labelled a single population of SRIF binding sites in RDCM membranes and mouse fibroblast (Ltk–) cells stably expressing the human recombinant sst2 receptor. There was a significant correlation between the affinity estimates of a range of SRIF analogues at inhibiting [125I]-BIM-23027 binding in RDCM membranes and binding to the recombinant sst2 receptor in Ltk– cells, suggesting that the sites labelled by [125I]-BIM-23027 in RDCM are similar to the sst2 receptor. GTPγS (100 μM) decreased [125I]-BIM-23027 binding in RDCM by 60%. The results from these studies demonstrate that [125I]-Tyr11-SRIF-14 labels a heterogeneous population of high affinity SRIF binding sites in RDCM membranes. The majority of these sites are insensitive to GTPγS and display negligible affinity for the cyclic hexapeptides, BIM-23027 and seglitide. The remaining high affinity binding sites can be selectively labelled with [125I]-BIM-23027, are sensitive to GTPγS and show similar characteristics to the recombinant sst2 receptor which appears to mediate the antisecretory effects of SRIF in the mucosa (McKeen ES, Feniuk W, Humphrey PPA (1995) Naunyn-Schmiedeberg‘s Arch Pharmacol 352:402–411).
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  • 10
    ISSN: 1432-1912
    Keywords: Key words45Ca2+ influx ; PC12 cells ; P2 purinoceptors ; Ion channel
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The aim of this study was to determine whether 45Ca2+ influx could be used as a quantitative measure of channel activation for functional characterisation of P2X purinoceptors in cell lines. In undifferentiated PC12 cells, grown in suspension, ATP (EC50 = 45 μM), ATPγS (EC50 = 50 μM) and 2-meSATP (EC50 = 81 μM) but not ab meATP (1 mM) stimulated 45Ca2+ influx 2–5 fold. This effect did not appear to be due to activation of P2U or P2Y purinoceptors since 1 mM UTP, ADP or ADPβS did not produce any significant effect. Similarly, the effects of ATP were not apparently mediated through activation of P2Z purinoceptors since dibenzylATP behaved as a weak (EC50 = 191 μM) partial agonist (Maximal effect 29.5% of ATP maximum) and there was no detectable ATP-stimulated ethidium bromide uptake in the PC12 cells. ATP-stimulated 45Ca2+ influx was not affected by nifedipine suggesting that it was not secondary to activation of L-type calcium channels and rather reflected influx through a P2X purinoceptor present in these cells. The ATP-stimulated 45Ca2+ influx could be reduced by monovalent cations, presumably as a result of direct competition for influx through the cation channel, with the following rank order of potency :- guanidinium (EC50 = 16 mM) 〉 sodium 〉 Tris 〉 choline 〉 N-methyl-D-glucamine = sucrose). A number of P2 purinoceptor antagonists inhibited ATP-stimulated 45Ca2+ influx. Pyridoxalphosphate-6-azophenyl-2′,4′-disulphonic acid (3–300 μM), pyridoxal 5-phosphate (3–300 μM) and d-tubocurarine (30–300 μM) produced an insurmountable antagonism of responses to ATP, with no marked change in agonist EC50. Suramin (100–300 μM) and cibacron blue (30–300 μM) produced a surmountable antagonism while DIDS (4,4′-diisothiocyanatostilbene-2,2′disulfonic acid) only antagonised responses to ATP at concentrations in excess of 300 μM. The general properties of the P2X purinoceptor population identified in these cells were consistent with them being P2X2 purinoceptors. These findings suggest that ATP-stimulated 45Ca2+ influx may be used as a reliable and quantitative functional assay for characterisation of P2X purinoceptor subtypes in cell lines.
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