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At least 775 records · Page 43Linked to original sources
PubMed1982

Accumulation of cimetidine by kidney cortex slices.

The mechanisms involved in the excretion of the histamine H2-receptor antagonist cimetidine are as yet incompletely understood. The purpose of this study was to examine the interaction of cimetidine with incubated slices of dog kidney cortex. The results of time and concentration-dependent experiments by using 3H-labeled cimetidine demonstrated that the drug was accumulated without metabolism against a concentration gradient by a saturable process. Inhibition of uptake by cyanide and by incubation under a nitrogen atmosphere indicated energy dependence. Uptake of cimetidine by active cationic transport was likely inasmuch as both cyanine 863 and quinine blocked accumulation. However, a probenecid-sensitive component, accounting for about 20% of steady-state accumulation, also was identified. The lack of inhibitory action of p-aminohippuric acid and the cationic nature of the cimetidine molecule suggest the probenecid-sensitivity was not related to the renal organic anion mechanism. Further, probenecid inhibition was not due to a generalized cellular toxicity because maximally inhibitory concentrations of probenecid did not interfere with uptake of the cation tetraethylammonium.

Animals↗
PubMed1981

[Anticholinesterase properties of benzo(f)quinolinium derivatives].

"In vitro" studies have demonstrated that methyl-p-toluene sulfonates of 1-methyl-(ethyl)-3-aryl-benzo(f)quinolinium are highly efficient inhibitors of cholinesterases, the inhibition constants (Ki) for acetylcholinesterase and butyrylcholinesterase being equal to 2.20 +/- 0.49 and 9.43 +/- 0.39 mkM, respectively. The effect of these inhibitors on the enzyme is of competitive - non-competitive type. A certain role in benzo(f)quinoline binding to acetylcholinesterase apparently belongs to the interaction of substituents in the phenyl nucleus with the anionic sites located outside the active surface of the enzyme.

Cholinesterase Inhibitors↗
PubMed1981

Cain's quinolinium (NSC 176319): protection of murine L1210 leukemia cells and bone marrow progenitor cells against mechlorethamine cytotoxicity and its application to combination chemotherapy.

Cain's Quinolinium; quinolinium, 6-amino-1-methyl-4[[[[[[(1-methyl-pyridinium-4-yl)amino]phenyl]amino]carbonyl]phenyl]amino] (NSC 176319), is a chemotherapeutic agent, which is equally cytotoxic in vitro to both murine L1210 leukemia cells and bone marrow progenitor cells. At non-toxic concentrations it equally protects L1210 cells and bone marrow progenitor cells against mechlorethamine cytotoxicity. However, treatment of murine L1210 leukemia bearing mice with the combination of Cain's Quinolinium and mechlorethamine at a mole ratio of 1:1 resulted in 100% long term survivors compared to 50% with Cain's Quinolinium alone or 0% with mechlorethamine alone.

Animals↗
PubMed1981

[Polarization optical investigations for the demonstration of a "sialomucin coat" at the surface of the chorionic epithelium of the rabbit placenta in relation to the stage of pregnancy].

Histological, histochemical, fluorescence optical and polarization microscopical investigations were performed in 53 placentas of rabbits from the 10th to the 35th day of pregnancy. A "sialomucin coat" could be demonstrated in all cases at the maternal surface of the metabolic barrier of the placenta. Polarization optical measurements after association with N,N'-diethylpseudoisocyanine chloride showed a lower content of sialic acid at the surface of the trophoblast in postmature placentas of rabbits in comparison to normal mature placentas. The immunological function of the placental barrier is discussed with respect to maturity.

Animals↗
PubMed1981

Chemotherapy of Babesia felis infection: efficacy of certain drugs.

The efficacy of 10 drugs was tested against Babesia felis infection in domestic cats. Primaquine phosphate administered per os or as an intramuscular injection was found to be highly effective and the obvious drug of choice when compared with conventional babesicides. The recommended dosage is 0,5 mg/kg body mass of primaquine base. Repeated treatments are well tolerated but single doses in excess of 1 mg/kg are known to cause mortality in cats.

Animals↗
PubMed1994

Using dyes and filters in a fluorescent imaging system.

The FluorImager fluorescence imaging system uses monochromatic 488-nm laser light to excite fluorochromes. It contains a built-in 515-nm long-pass filter that rejects excitation laser light, but allows emission light with wavelengths longer than 515 nm to pass through. A fluorochrome appropriate for use in the system is excitable by 488-nm light and emits at least some of its fluorescence at wavelengths longer than 515 nm. Two types of optical filters, long-pass and band-pass, are used in the system. Long-pass filters reject shorter wavelengths and transmit longer wavelengths. The number in the filter name denotes the cutoff wavelength (midpoint of the transition between rejected and transmitted light) for the filter. Band-pass filters transmit a band of wavelengths and reject both shorter and longer wavelengths. The numbers in the filter name denote the center wavelength of the passed band and the width of the band at half maximum transmission. Generally, when scanning for a single fluorochrome, only the built-in 515-nm long-pass filter is needed. An interchangeable filter can be added to decrease the contribution from a broad-spectrum background signal and to attenuate strong fluorochrome signals.

Calcium↗
PubMed1994

Some new properties of DNA-YOYO-3 homodimer complexes revealed by electrophoresis and fluorescence lifetime measurements.

The DNA bis-intercalator oxazole homodimer (YOYO-3: 1,1'-(4,4,7,7-tetramethyl-4,7-diazaundecamethylene)-bis-4-[3-methy l- 2,3-dihydro-(benzo-1,3-oxazole)-2-methylidene]-quinolinium tetraiodide) specifically alters the electrophoretic pattern of covalently closed circular (CCC) DNA molecules. Thus, YOYO-3 seems to remove the CCC DNA supercoils and induces the appearance of additional bands by changing the linking number. It also promotes an unusual "star" activity for the restriction enzyme Hind III. Fluorescence lifetime measurements indicate that YOYO-3 is capable of binding to DNA by bis- and mono-intercalation.

Benzoxazoles↗
PubMed1994

Three drugs inhibit phospholipase A2-induced high permeability of endothelial monolayers.

The permeability of aortic endothelial monolayers to fluid and albumin increased 13.5 and 16.1 times respectively after pretreatment with phospholipase A2 (PLA2, 100 U.ml-1) for 30 min. 1-(p-Chlorobenzoyl)-5-methylindole-3-acetic acid (1.16 mmol.L-1), SRI 63-441 (30 nmol.L-1), and 1,25-dihydroxycholecalciferol (0.1 mumol.L-1) decreased PLA2-induced high permeability. PLA2 did not damage the endothelial cells significantly. Our results indicate that the action of PLA2 to increase the permeability of endothelial monolayers is mainly due to PLA2-induced lipid mediators released from endothelial cells.

Animals↗
PubMed1995

In vivo renal production and tubular secretion of tyramine.

Para-tyramine (p-TYM) is a predominant urinary amine in humans, rabbit, rat and dog, and its urinary excretion rate may reflect central nervous system pathophysiology. However, the source of urinary p-TYM is not known, nor have the mechanisms regulating its excretion been characterized. The present study, by using renal clearance techniques, examined the sources of urinary p-TYM and the mechanism of excretion in anesthetized rabbits. In all studies, the renal clearance of p-TYM was compared with that of norepinephrine (NE). Base-line delivery to the kidney of p-TYM in plasma was 8.6 +/- 1.6 ng/min (mean +/- S.E.M., n = 16), whereas the mean urinary excretion rate of p-TYM was 26.5 +/- 3.6 ng/min during the same period (P < .001 vs. delivery). In three separate series of experiments, either vehicle (n = 5) or a specific inhibitor of renal tubular organic cation secretion, cyanine 863 (6 mg/kg, n = 7), or a specific inhibitor of aromatic-amino acid-decarboxylase, alpha-mono-fluoromethyldopa (FMD, 4 mg/kg, n = 5), were infused i.v., Mean arterial pressure, glomerular filtration rate, renal plasma flow and urine flow rate were unchanged in all studies. The renal clearances of p-TYM (Cp-TYM) and NE (CNE) were unchanged only after vehicle. After cyanine 863, Cp-TYM was decreased to 36% of control (P < .01), whereas CNE decreased to 21% of its base-line value (P < .01). After FMD Cp-TYM was reduced to 2% of control (P < .05), whereas CNE decreased by 44% (P < .01).(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1994

P2Z adenosine triphosphate receptor activity in cultured human monocyte-derived macrophages.

The present study shows that human mononuclear phagocytes express a P2Z-like purinergic membrane receptor activity. Extracellular adenosine triphosphate (ATP) induces the formation of nonselective membrane pores in human mononuclear phagocytes that allow the entry of otherwise membrane impermeant fluorescent dyes (YO-PRO-1 or Lucifer yellow) into the cytoplasm of these cells. The percentage of mononuclear phagocytes that was permeabilized by ATP increased as monocytes matured into macrophages. Their response to ATP was inhibited by Mg2+ and oxidized ATP. Benzoylbenzoic-ATP (BzBzATP) was approximately 60% as effective as ATP and adenosine-5 -O-(thiophosphate) (ATP gamma S) was less than 20% as effective as ATP in permeabilizing human macrophages to YO-PRO-1 or Lucifer Yellow. Thus, the human P2Z-like receptor differs from its murine counterpart because BzBzATP, ATP, and ATP gamma S are equally efficacious in permeabilizing murine macrophage-like J774 cells to these dyes. UTP, GTP, and CTP were ineffective in permeabilizing human or murine macrophages to YO-PRO-1. Taken together, these data indicate that human monocyte-derived macrophages express a P2Z-like activity that is pharmacologically distinct from that expressed by their murine counterparts and that expression of these receptors is developmentally regulated in human mononuclear phagocytes.

Adenosine Triphosphate↗
PubMed1994

Use of thiazole orange homodimer as an alternative to ethidium bromide for DNA detection in agarose gels.

Detection of polymerase chain reaction-amplified DNA fragments is commonly accomplished by visualizing the products in electrophoretic agarose beds with the use of ethidium bromide under ultraviolet light. However, ethidium bromide is mutagenic, and special handling and disposal precautions must be used. We report the use of a nonmutagenic dye, thiazole orange dimer (TOTO), which can be substituted for ethidium bromide. The excitation maximum for TOTO under ultraviolet light is 488 nm, and the absorption maximum is 510 nm, necessitating photographic filters different from those used for ethidium bromide for optimal results. Of particular importance in TOTO's use is the quantity used for each gel lane, since excess TOTO will cause unacceptable product mobility retardation. TOTO is only slightly more expensive than ethidium bromide. Overall, this stain provides very good visualization of polymerase chain reaction--amplified DNA bands in agarose gels. We believe the use of this safer reagent will become more widespread with increased regulation of laboratory activities.

Base Sequence↗