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PubMed1991

Two inward currents and the transformation of low-frequency oscillations of rat and cat thalamocortical cells.

1. The contribution of a slow, mixed Na(+)-K+, inward rectifying current (Ih) and the T-type Ca2+ current (IT) (that underlies low-threshold Ca2+ potentials) to the low-frequency oscillations observed in rat and cat thalamocortical (TC) cells in vitro was studied using current clamp and single-electrode voltage clamp recordings. 2. From a holding potential of -50 mV, voltage steps negative to -60 mV showed the presence of a slow, non-inactivating inward current, Ih. This current was unaffected by Ba2+ (1-4 mM), tetrodotoxin (0.5-1 microM) and TEA (20 mM, n = 6), reversibly blocked by Cs+ (1-3 mM), and its reversal potential (-33.0 +/- 1.2 mV) followed changes in the extracellular Na+ and K+, but not Cl-, concentration. 3. Application of Cs+ (1-3 mM) abolished the pacemaker oscillations (n = 9), while in six cells that did not show any oscillatory activity Cs+ first evoked the spindle-like oscillations that, in the continuous presence of these ions, were then transformed into the pacemaker oscillations before all activities were finally blocked: all these effects were accompanied by a hyperpolarization and a progressive decrease and final blockade of Ih. Cs+ had no effect on the 'N-methyl-D-aspartate' (NMDA) oscillations (n = 5) and Ba2+ (2 mM, n = 8) did not block the pacemaker, the spindle-like and the 'NMDA' oscillations. 4. In ten cells that showed the pacemaker oscillations selective activation of beta-adrenoceptors by 10-50 microM-noradrenaline (in the presence of alpha-noradrenergic antagonists) or by 20 microM-isoprenaline first transformed the pacemaker oscillations into the spindle-like oscillations that, in the continuous activation of beta-receptors, were finally abolished: all these effects were accompanied by a depolarization and a progressive increase of Ih. 5. In TC cells that showed the pacemaker oscillations application of 1-octanol (50-100 microM), an antagonist of T-type Ca2+ currents, reversibly blocked this activity but concomitantly decreased (50%) the cell input resistance (n = 5). Application of Ni2+ (0.2-0.5 mM, n = 13), another antagonist of IT reversibly blocked the pacemaker, the spindle-like and the 'NMDA' oscillations. 7. In cells showing the pacemaker oscillations it was found that the current developing from the most hyperpolarized potential of an oscillation cycle was an inward relaxation whose time course differed from that of Ih evoked at the same potential.(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMed1991

A potassium current evoked by growth hormone-releasing hormone in follicular oocytes of Xenopus laevis.

1. Electrophysiological properties of the growth hormone-releasing hormone (GRH) receptor were studied in Xenopus oocytes with an intact follicle cell layer (i.e. follicular oocytes) by measuring whole-cell current using the two-electrode voltage-clamp method. 2. A slow transient outward current was elicited in oocytes, clamped at -60 mV, by the application of rat GRH but not bovine, porcine, or human GRH. 3. The response to GRH was not suppressed by blockers known to inhibit other endogenous receptors present in follicular Xenopus oocytes; blockers used were timolol (2 microM; beta-adrenergic blocker), theophylline (0.1 mM; purinergic blocker) and atropine (100 nM; muscarinic blocker). 4. The current response evoked by rat GRH occurred in a dose-dependent manner. The concentrations of GRH for threshold and maximum responses were 1 and 100 nM respectively and the estimated EC50 (half-maximal effective concentration) was approximately 7 nM. The amplitude and conductance of the response became larger and the latency, time-to-peak and half-decay time were shortened when the concentration of GRH was increased. 5. The GRH response was reversibly inhibited by a K+ channel blocker, tetraethylammonium+ (TEA+; 20 mM). The reversal potential for the GRH response was around -100 mV and was compatible with the reported value for a K+ current in Xenopus oocytes. Furthermore, a depolarizing shift of 40 mV in the reversal potential was observed when the external K+ concentration was increased from 2 to 10 mM, agreeing with the Nernst equation. In contrast, no significant shift in the reversal potential was observed by changing the external concentration of Na+ or Cl-. 6. The GRH response was not suppressed in oocytes treated with an acetoxy-methyl ester of bis-(o-aminophenoxy)-ethane-N,N,N',N'-tetraacetic acid (BAPTA/AM; 10 microM) which penetrates the cell membrane and chelates internal Ca2+. 7. The GRH response was potentiated by pre-treatment with forskolin (0.4 microM; 5 min), which stimulates adenylate cyclase and increases the internal concentration of adenosine 3',5'-cyclic monophosphate (cyclic AMP). 8. The GRH response was not obtainable when follicle cells surrounding oocytes were removed mechanically with forceps or enzymically with collagenase (i.e. denuded oocytes). The response was also suppressed when gap junctions, which electrically couple follicle cells and the oocyte, were blocked by 1-octanol (1 mM). 9. The first amino acid is considered to be important for the binding of peptide ligands to their receptors.(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMed1992

Relationships among antibacterial activity, inhibition of DNA gyrase, and intracellular accumulation of 11 fluoroquinolones.

A series of 11 fluoroquinolone antibacterial agents, including 8 newly synthesized molecules and 3 reference compounds (pefloxacin, ciprofloxacin, and sparfloxacin), were tested for their MICs against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The intracellular accumulation of fluoroquinolones by these microorganisms was measured by centrifugation through silicone oil and a fluorescence assay. The minimal effective dose (MED) was determined for all agents in a supercoiling assay with E. coli DNA gyrase. The hydrophobicities of the quinolones were determined and expressed as the logarithm of the coefficient of distribution (log D) between 1-octanol and phosphate buffer (pH 7.2). No correlation was found between MICs and cell accumulation for the quinolones studied. A correlation was found between log D and accumulation by S. aureus (r = 0.71, n = 11), and an inverse correlation was found between log D and accumulation by E. coli (r = 0.73, n = 11) and P. aeruginosa (r = 0.64, n = 10). The correlation coefficients between MICs and MED for E. coli, which were 0.60, 0.64, and 0.74 (n = 11) for E. coli, P. aeruginosa, and S. aureus, respectively, rose to 0.85, 0.74, and 0.74 (n = 11) for the same microorganisms, respectively, when the accumulation of the drug by the cell was taken into account. It was concluded that the inhibitory activity against DNA gyrase remains the most important parameter for quinolone potency, but that intracellular accumulation must be taken into account, since, for a given organism, both parameters are under the control of the physicochemical properties of the quinolones.

Anti-Infective Agents↗
PubMed1991

Carbonic acid buffer species measured in real time with an intracellular microelectrode array.

Carbonic acid buffer anions, HCO3- and CO3(2-), play an instrumental role in a host of vital processes in animal cells and tissues. Yet study of carbonic acid buffer species is hampered because no means are available to simultaneously monitor them at a cellular level in a rapid and dynamic fashion. An ion-selective cocktail, previously reported to measure changes in bicarbonate activity (alpha HCO3-), was instead shown to be principally selective for alpha CO3(2-). Ion-selective micropipettes (ISMs) based on this exchanger and consisting of a 3:1:6 (volume) mixture of tri-n-octylpropylammonium chloride, 1-octanol, and trifluoroacetyl-p-butylbenzene showed no significant interference from bicarbonate, chloride, phosphate, ascorbate, lactate, glutamate, acetate, or hydroxyl ions at concentrations expected in vivo. Intracellular and triple-barrel ISMs, consisting of a CO3(2-) sensitive, pH-sensitive, and reference barrel, were fabricated. Skeletal muscle cells (n = 17) were penetrated in vivo and showed values of 74 +/- 7 mV for membrane potential, 6.94 +/- 0.09 pHi, and 11 +/- 5 microM intracellular alpha CO3(2-), from which intracellular alpha HCO3- of 25 +/- 10 mM and CO2 tension of 120 +/- 55 Torr were calculated. All ion measurements reached a new steady state in 9 +/- 2 s after cell penetration. Thus measurements of intracellular alpha CO3(2-) and pH and associated levels of alpha HCO3(2-) and CO2 tension can be determined in biological tissues and cells with a spatial and temporal resolution previously unattainable.

Animals↗
PubMed1991

[Myeloperoxidase interaction with mixed monolayers of lecithin and cholesterol].

Interaction between myeloperoxidase and mixtures of lecithin-cholesterol monolayers were investigated. Solubility of the enzyme in 1-octanol or in octanol were tested too. It is shown that myeloperoxidase demonstrates an ability to concentrate on phase limits. The enzyme well dissolves in lipid membrane phases. It is possible to assume that myeloperoxidase penetrates and accumulates in the eye lens.

Adsorption↗
PubMed1976

Conditional spore cortex-less mutants of Bacillus sphaericus 9602.

Lysine-requiring mutants of Bacillus sphaericus 9602 were isolated and classified into three groups by their mutation site in the pathway of lysine biosynthesis. The Group I mutant lacks meso-alpha, epsilon-diaminopimelic acid (meso-Dap) decarboxylase activity, but Group II and III mutants have a normal level of Dap decarboxylase activity. A Group II mutant makes dipicolinic acid from an intermediate in the lysine pathway, but Group III mutants do not. In the absence of meso-Dap in the culture, muramic lactam content in the spore cortex of Group II and III mutants is very low, compared to the wild type content. Addition of meso-Dap to the culture causes an increase of muramic lactam content. Since meso-Dap is detectable only in the spore cortex of B. sphaericus 9602, almost all of the muramic lactam in the spore is probably also located in the cortex. Group I mutants grown in the presence of L-lysine sporulate normally. Group II and III mutants produce oval and nonrefractile spores under the same conditions but the addition of meso-Dap to the culture results in the production of round and refractile spores. Thus, the presence of cortex in the spore is essential to give the round and refractile spores in B. sphaericus. The presence of cortex is also required for the accumulation of dipicolinic acid in the sporulating cells. Furthermore, 1-octanol resistance of the spore depends only on the presence of cortex but both cortex and dipicolinic acid are required for heat resistance of the spore.

Bacillus↗
PubMed1991

Effect of 1-alkyl- or 1-alkenylazacycloalkanone derivatives on the penetration of drugs with different lipophilicities through guinea pig skin.

The percutaneous penetration-enhancing effects of 1-dodecyl- (azone), l-geranyl-, and 1-farnesylazacycloheptan-2-one were investigated using seven penetrants having a wide range of n-octanol-water partition coefficients. The penetration of the drugs from water vehicle (aqueous system) and ethanol vehicle (ethanolic system) through excised guinea pig skin was increased by pretreatment with the enhancers. Large enhancement was observed for the drugs, such as 5-fluorouracil and 6-mercaptopurine, with n-octanol-water partition coefficients of approximately unity. The penetration profiles were analyzed based on a one-layer skin model. Two parameters corresponding to the drug diffusivity and partitioning into the skin were obtained. In the aqueous system, the partitioning of drugs into the skin was increased by pretreatment with the enhancers. This led to an increase in drug penetration and accumulation in the skin; diffusivities were little affected. From these parameters, the drug amounts in the vehicle and the skin were well estimated for drugs having partition coefficients of less than 1. In the ethanolic system, the enhancement was far less than that observed in the aqueous system.

1-Octanol↗
PubMed1992

Electrochemical determination of partition coefficients of drugs.

An electrochemical method for the determination of partition coefficients of drugs that can exist as ions in aqueous solutions is presented. The method involves cyclic voltammetry at the polarizable interface between two immiscible electrolyte solutions. Because n-octanol is an unsuitable solvent for electrochemical purposes, 1,2-dichloroethane, which has electronic properties similar to those of n-octanol, was used in the measurements. The values obtained could be correlated with the values for n-octanol-water partition taken from the literature by an approach based on the linear solvation relationship: log P1 = a log P2 + b; in this relationship, a and b are constants and P1 and P2 correspond to the two different organic and aqueous phase partition equilibria. Furthermore, aqueous diffusion coefficients of drugs were determined from voltammograms.

1-Octanol↗
PubMed1991

Evidence that interfacial transport is rate-limiting during passive cell membrane permeation.

The octanol to water overall transfer rate constants (k'ow), the octanol/water partition coefficients (Kpc) and the diffusion coefficients in octanol (Do) and water (Dw) were measured for 36 compounds. A plot of Do/k'ow as a function of Do.Kpc/Dw was shown to fit a straight line for compounds having a high Kpc, and from the slope of this line, the thickness of the unstirred layer in the water phase was found to be 9.1 microns. Using this value and the data provided by compounds having a low Kpc, an estimate of 1.2 microns was obtained for the thickness of the unstirred layer in the octanol phase. This provided estimates for the true interfacial rate constants, kow (for movement of a compound from octanol into water) and kwo (for movement in the opposite direction), which were corrected for the effects of the unstirred layers. kow proved to be constant to within one order of magnitude for a series of compounds whose Kpc values ranged over three orders of magnitude, while kwo for these same compounds varied directly as Kpc. Assuming that octanol has solvent properties similar to those of the lipid bilayer present in natural membranes, the permeability of these membranes to a given compound can be shown to be equal to kwo/2. Comparing the permeabilities calculated in this way to measured permeabilities of natural membranes showed them to be of the same order or smaller. These data are consistent with a proposal that the rate-limiting step in passive membrane permeation is not the rate of diffusion within the membrane itself, but rather, transfer of the permeant across the interfaces separating the lipid phase of the cell membrane from the aqueous phases on either side of it.

1-Octanol↗
PubMed1992

Reduced cell-cell communication between mitotic and nonmitotic coupled cells.

The effects of mitosis on gap junctional intercellular communication (GJIC) were quantified in a clonal cell line of spontaneously immortalized rat granulosa cells (SIGC) using a fluorescence recovery after photobleaching assay. Reduction of GJIC was associated with the process of mitosis and was first apparent at the onset of prophase. Resumption of GJIC between newly divided cells and surrounding cells occurred slowly, requiring several hours following cytokinesis before reestablishment of maximal rates. Mitotic rates of GJIC in SIGC were comparable to values obtained in interphase cells partially uncoupled by 0.5 mM octanol. Limited studies of other cell lines generalized the mitotic-associated reduction of GJIC observed in SIGC. The data suggest that mitosis is one process which alters GJIC. This could be of significance when there is a change in the rate of proliferation, such as in the acquisition of immortalization, an early stage of transformation.

1-Octanol↗
PubMed1992

Modulation of cell-to-cell coupling between myometrial cells of the human uterus during pregnancy.

OBJECTIVE: The purpose of this study was to investigate changes in cell-to-cell coupling of human myometrium during pregnancy to assess the presence and permeability of gap junctions. STUDY DESIGN: To evaluate the coupling, input resistance was measured and intercellular spread of Lucifer yellow was observed with microelectrode techniques in intact myometrial preparations from four nonpregnant women, 13 women not in labor, and three women in labor. Octanol, isoproterenol, and dibutyryl adenosine 3',5'-cyclic monophosphate were applied to the preparations to assess their effects on cell-to-cell coupling. RESULTS: Input resistance of myometrial cells was decreased (p less than 0.001) and intercellular spread of Lucifer yellow was increased during pregnancy. Octanol, isoproterenol, and dibutyryl adenosine 3',5'-cyclic monophosphate rapidly and reversibly increased input resistance (p less than 0.001 for all these agents) and blocked Lucifer yellow spread in tissues from pregnant patients. CONCLUSIONS: Cell-to-cell coupling between human myometrial cells is spontaneously improved during pregnancy because of the presence of gap junctions. The coupling is rapidly and reversibly decreased by octanol, isoproterenol, and dibutyryl adenosine 3',5'-cyclic monophosphate as a result of decreased permeability of gap junctions. These two methods of modulation of gap junctions are suggested to be major mechanisms for control of myometrial contractile activity in the human uterus during pregnancy.

1-Octanol↗
PubMed1979

n-Alkanols potentiate sodium channel inactivation in squid giant axons.

The effects of n-octanol and n-decanol on nerve membrane sodium channels were examined in internally perfused, voltage-clamped squid giant axons. Both n-octanol and n-decanol almost completely eliminated the residual sodium conductance at the end of 8-ms voltage steps. In contrast, peak sodium conductance was only partially reduced. This block of peak and residual sodium conductance was very reversible and seen with both internal and external alkanol application. The differential sensitivity of peak and residual conductance to alkanol treatment was eliminated after internal pronase treatment, suggesting that n-octanol and n-decanol enhance the normal inactivation mechanism rather than directly blocking channels in a time-dependent manner.

1-Octanol↗
PubMed1991

Anesthetic inhibition of firefly luciferase, a protein model for general anesthesia, does not exhibit pressure reversal.

The surprising observation that pressures of the order of 150 atmospheres can restore consciousness to an anesthetized animal has long been central to theories of the molecular mechanisms underlying general anesthesia. We have constructed a high-pressure gas chamber to test for "pressure reversal" of the best available protein model of general anesthetic target sites: the pure enzyme firefly luciferase, which accounts extremely well for animal potencies (over a 100,000-fold range). We found no significant pressure reversal for a variety of anesthetics of differing size and polarity. It thus appears that either firefly luciferase is not an adequate model for general anesthetic target sites or that pressure and anesthetics act at different molecular sites in the central nervous system.

1-Octanol↗
PubMed1990

The liposome as a model membrane in correlations of partitioning with alpha-adrenoceptor agonist activities.

The apparent partition coefficients of a group of imidazoline alpha-adrenoceptor agonists in liposome/buffer systems (K'm) and in the n-octanol/buffer system (P') have been compared in quantitative structure-activity relationships (QSAR) employing biological activities and receptor binding affinities. A parabolic relationship between log K'm and log P' was found, and log K'm was greater than log P' for all liposome compositions. In liposomes, log K'm decreased in the order, negatively charged greater than neutral greater than positively charged. Overall, hyper- and hypotensive activities of these drugs correlated better with log K'm than with log P'; however, poor correlations were obtained between partition coefficients and in vitro binding affinities. Linear correlations of log K'm with hypotensive activities were obtained with negatively charged liposomes, whereas correlations with hypertensive activities were obtained using positively charged liposomes. Multiple regressions of biological activities with binding affinities showed positive correlations with hypotensive but not hypertensive activities with or without the inclusion of log K'm or log P'. Thus, the liposome represents a more selective model membrane system than a bulk oil phase for predicting the biological activities of imidazoline alpha-adrenoceptor agonists.

1-Octanol↗
PubMed1991

Actions of n-alcohols on nicotinic acetylcholine receptor channels in cultured rat myotubes.

1. The actions of the n-alcohols from pentanol to dodecanol on nicotinic acetylcholine receptor (nAChR) channels were investigated by recording single ACh-activated channel activity from inside-out membrane patches isolated from cultured rat myotubes. Alcohols were applied to the cytoplasmic side of the membrane; aqueous concentrations ranged from 11.7 mM-pentanol to 0.02 mM-dodecanol. 2. The intermediate-chain alcohols (pentanol to octanol) caused channel currents to fluctuate between the fully open and closed state level so that openings occurred in bursts interrupted by brief gaps. Closed time distributions were fitted well with two exponential components, the fast component representing the closures within a burst. The number of gaps within a burst was dependent on alcohol concentration whereas gap duration was independent of concentration but increased with increasing chain length of the alcohol up to octanol. 3. Nonanol and decanol reduced the mean duration of bursts of openings but did not cause an increase in the number of short closed intervals within a burst. Beyond decanol there was a decline in the ability of the n-alcohols to affect channel function. A saturated solution of undecanol (0.07 mM) reduced the mean open time by 33 +/- 17%, whereas a saturated solution of dodecanol had no significant effect. 4. The current integral per burst was reduced by all the n-alcohols between pentanol and undecanol. The IC50S were as follows: hexanol, 0.53 +/- 0.14 mM; heptanol, 0.097 +/- 0.02 mM; octanol, 0.04 mM and nonanol, 0.16 +/- 0.035 mM. 5. The results were analysed in terms of an open channel block model with a long-lived closed-blocked state beyond the blocked state. Over the range of concentrations tested this describes the effects of all the n-alcohols (C5 to C12) on channel gating reasonably well. 6. Blocking rate constants (k+B) for pentanol through to nonanol were calculated to be between 2.8 and 5.7 X 10(6) M-1 S-1. These values are based on the assumption that the concentration of the alcohols at their site(s) of action was equal to the aqueous concentration applied to the membrane. 7. Equilibrium dissociation constants (KD), calculated from the blocking and unblocking rate constants (KD = k-B/k+B), decreased with increasing chain length from 8 mM for pentanol to 0.15 mM for octanol. The standard free energy per methylene group for adsorption to the site of action was calculated to be about -3.3 kJ mol-1.(ABSTRACT TRUNCATED AT 400 WORDS)

1-Octanol↗
PubMedDate not supplied

Effect of nanoparticles on transdermal drug delivery.

The purpose of the present study was to assess by in vitro means the effect of poly (methylmethacrylate) nanoparticles and poly (butylcyanoacrylate) nanoparticles on transdermal drug delivery. Methanol and octanol were chosen as test permeants. In order to distinguish between thermodynamic effect and those due to biological consequences, two different membranes were employed, i.e., full thickness hairless mouse skin and silicone elastomer sheeting (175 microns). It is evident that poly (methylmethacrylate) nanoparticles and poly (butylcyanoacrylate) nanoparticles increase the permeability of methanol through hairless mouse skin by a factor of 1.2-2. The permeability of lipophilic octanol is either unaffected by nanoparticles or decreases as a function of nanoparticle concentration depending on the lipophilicity of the polymer material.

1-Octanol↗
PubMed1991

Alcohols protect Escherichia coli against cold shock.

Alcohols protect Escherichia coli against cold shock, and the concentration of alcohol which provided optimal protection declined with increasing hydrophobicity of the alcohol. The rate of loss of viability after the chilling transition was decreased by n-octanol, even when it was added after that chilling transition. Cold-shocked cells exhibited a sensitivity toward dioxygen, seen as greater enumeration on anaerobic, rather than on aerobic, trypticase-yeast extract agar plates, and addition of catalase or antioxidants, such as alpha-tocopherol or probucol, to the agar plates did not lessen this dioxygen sensitivity. Respiratory capacity was diminished by cold shock, and cyanide-sensitive respiration was more affected than was cyanide-resistant respiration. Discharging the proton gradient, with the uncoupler carbonyl cyanide trifluoromethoxy-phenylhydrazone, did not change sensitivity to cold shock. There was no evidence for minimal medium recovery after cold shock. The data presented, as well as that already in the literature, are explained on the basis of membrane damage caused by patches of ordering transitions in one membrane leaflet, unmatched by comparable transitions in the mating leaflet.

1-Octanol↗
PubMed1991

Evaluation of potential aluminum chelators in vitro by aluminum solubilization ability, aluminum mobilization from transferrin and the octanol/aqueous distribution of the chelators and their complexes with aluminum.

Representative amino acids, carboxylic acids, a ketone, hydroxamic acids, 3-hydroxypyridinones and a linear catecholcarboxyamide were tested in vitro to estimate their aluminum (Al) chelation potential. Their ability to solubilize Al from insoluble Al borate in a previously described octanol/aqueous (o/a) system was tested. Salicylhydroxamic acid, rhodotorulic acid, the 3-hydroxypyridin-4-ones and a sulfonated linear polycatecholcarboxamide significantly increased solubilized Al, suggesting Al chelation potential. Some of the above compounds and some compounds previously shown to solubilize Al in the o/a system were tested for their ability to mobilize Al from the Al plasma binding protein transferrin. Chelators solubilizing Al in the o/a system were comparably effective in mobilizing Al from transferrin, supporting the utility of the o/a system as a screening method. The o/a distribution coefficient of each chelator was determined, when possible, to assess its hydrophilicity. When compared with the suggested desirable hydrophilicity of effective chelators, the o/a distribution coefficient of many of the 3-hydroxypyridin-4-ones and a sulfonated linear polycatecholcarboxamide suggest that they might be able to chelate intracellular Al. The o/a distribution coefficient of each Al-chelator complex was determined, when possible, to predict the likelihood of redistribution within or excretion from the intact animal of this complex. Complexation of chelators with Al usually increased chelator hydrophilicity. The results suggest several compounds that warrant further investigation as potential alternatives to desferrioxamine in the treatment of Al accumulation and toxicity.

1-Octanol↗