Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0847097 (acidity)
 15,165 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The purpose in developing diclofenac sodium was to synthesize a nonsteroidal anti-inflammatory drug with high activity and outstanding tolerability. Factors considered were drug transport through biologic membranes, the atomic and spatial structure of the molecule, and the electronic structure. Based on analysis of other nonsteroidal anti-inflammatory drugs, it was postulated that an effective antirheumatic agent should have the following characteristics: an acidity constant between 4 and 5, a partition coefficient of approximately 10, and two aromatic rings twisted in relation to each other. The result was diclofenac sodium, which has an acidity constant of 4.0 and a partition coefficient of 13.4. The structural elements include a phenylacetic acid group, a secondary amino group, and a phenyl ring containing chlorine atoms, which cause maximum twisting of the ring. Experimental and clinical findings obtained to date have indicated that diclofenac sodium was synthesized on well-founded principles.
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PMID:The history of diclofenac. 308 89

The effect of gastric pH on the viability and virulence of Yersinia enterocolitica O:8 after exposure to sublethal concentrations of copper and chlorine was determined in mice. Viability and injury were assessed with a nonselective TLY agar (tryptic soy broth containing lactose, yeast extract, and agar) and two selective media, TLYD agar (TLY agar plus sodium deoxycholate) and CIN agar (cefsulodin-Irgasan-novobiocin agar). Both copper and chlorine caused injury which was manifested by the inability of the cells to grow on selective media. CIN agar was more restrictive to the growth of injured cells than TLYD agar. Injury of the exposed cells was further enhanced in the gastric environment of mice. Besides injury, the low gastric pH caused extensive loss of viability in copper-exposed cells. Lethality in the chlorine-exposed cells was less extensive, and a portion of the inoculum (5.2 X 10(5) of 1 X 10(7) inoculated cells) reached the small intestine 5 min postinoculation. No adverse effect on the injured cells was apparent in the small intestine, and a substantial revival (approximately 70%) of the injury occurred in 3 to 4 h after intraluminal inoculation. The virulence of chlorine-stressed Y. enterocolitica in orally inoculated mice was similar to that of the control culture, but copper-stressed cells showed reduced virulence. Virulence was partly restored by oral administration of sodium bicarbonate before the inoculation of copper-exposed cells. Neutralization of gastric acidity had no effect on the virulence of the control or chlorine-stressed cells. The results of this study indicate that the extensive injury caused by the low gastric pH does not affect the virulence potential of chlorine-exposed cells. However, extensive cell death in the mouse stomach is responsible for the reduced virulence of the copper-stressed bacteria.
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PMID:Survival and virulence of copper- and chlorine-stressed Yersinia enterocolitica in experimentally infected mice. 366 14

Chlorine dioxide, bromine chloride and iodine were compared with chlorine as virucidal agents. Under optimal conditions all disinfectants were effective at low concentrations, but each disinfectant responded differently to acidity and alkalinity. Disinfection by chlorine was impaired by the presence of ammonia, but the other disinfectants retained much of their potency. Disinfection of poliovirus by iodine resulted in structural changes in the virions as seen by electron micrroscopy, but the other disinfectants were able to inactivate poliovirus without causing any apparent structural changes.
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PMID:A comparison of the virucidal properties of chlorine, chlorine dioxide, bromine chloride and iodine. 629 May 66

A positive correlation of the milk specific conductance (MSC) to the number of cells (r = 0.65) and to the content of chloride ions (r = 0.93) was found on the basis of an examination of 196 udder-quarter milk samples. As indicated by the closeness of the relationship to the number of cells, MSC measurement at a determination level of 41.8% has similar diagnostic effectiveness as the determination of the content of chloride ions (determination level 43.5%) and lactose content (determination level 42.8%), and much higher diagnostic effectiveness than the determination of titration acidity (determination level 23.4%). As indicated by the closeness of the relationship to the content of chloride ions, MSC measurement at a determination level of 86.7% has higher diagnostic effectiveness than the determination of lactose content (determination level 73.9%) and titration acidity (determination level 54.6%). In both comparisons, the highest diagnostic effectiveness was found in assessing the chlorine-sugar number (determination levels of 49.8% and 94.0%). The MSC value, corresponding to the cellulization of 500 . 10(3) cells per ml of milk, was determined from regression: 0.523 S . m-1. The diagnostic congruence of MSC with the number of cells in milk was 81.25%, and with the findings of mastitis test-NK only 54.0%. The variability of the measurements of MSC renders it impossible to use this measurement to indirect multi-step screening of milk cellulization. It is only realistic to distinguish two classes of the measured MSC values: negative and positive.
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PMID:[The diagnostic value of measuring the electric conductivity of milk]. 677 7

1. Unlike rhodopsin, the extracted 521-pigment of the Tokay gecko (Gekko gekko) is pH-sensitive and changes its spectral absorbance in the pH range of 4.5-7.3. The colour change is reversible and pH can be employed to adjust the spectral maximum anywhere between 490 nm and its native location at 521 nm.2. The hypsochromic shift with increasing acidity is opposite to that expected for the protonation of the Schiff base nitrogen and suggests an action on the secondary system of interacting charges that have long been postulated to adjust vertebrate visual pigment colour within the visible spectrum.3. Chloride ions modulate this pH effect in a systematic and significant manner. For the pigment extracted in the chloride-deficient state the colour change occurs in the pH range of 6.0-7.0, the midpoint being close to 6.5, suggesting the possible participation of the imidazole group of histidine as the functional moiety. With added NaCl the colour shifts to the region below pH 6.2.4. The modulating action of chloride is postulated to be a conformational change of the opsin leading to a shift of the secondary interacting site from one functional group to another or else to a change in pK of a single group due to the conformational alteration of the electrostatics of the system.5. At pH values between 7.5 and 9.0 a different mechanism becomes apparent. In this region a decrease occurs in the photopigment density as well as a shift in absorbance toward the blue. This alkaline effect is readily reversed either by adding NaCl or else by lowering the pH. Along with the other protective effects of chloride these ions serve to reduce or prevent this alkaline loss in density.6. Associated with this reversible photopigment loss is a reversible appearance of a product with a maximum at about 366 nm. The spectrum of this product is like that produced by the addition of 11-cis retinal to the extract. Acidification of the alkaline preparation leads to a restitution of the photopigment as well as to a reduction of the 366-product.7. Addition of hydroxylamine to the alkaline extract in appropriate concentration inhibits the restitution of pigment-521 with acid or NaCl, but adding 11-cis retinal to the system leads to restoration of the photopigment after acidification. All the evidence suggests that product-366 is either free 11-cis retinal or else held to the opsin in a form that does not alter its spectral absorbance. The alkaline effect is therefore a disruption of the aldimine bond of the visual pigment.8. In many respects the gecko 521-pigment behaves like the chicken cone pigment, iodopsin, suggesting that an investigation of the latter in terms of pH may be a worthy project for future study.9. With its ability to change colour with pH, with chloride, with nitrate, etc. the extractable gecko pigment offers possibilities for the investigation of mechanisms responsible for adjusting visual pigment absorbance throughout the visible spectrum. The techniques of circular dichroism, Raman spectroscopy, infra-red spectroscopy, etc. may find here a suitable material for these studies.
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PMID:The gecko visual pigment: a pH indicator with a salt effect. 733 18

1. Expression of the recombinant human excitatory amino aid transporters, EAAT1 and EAAT2, in Xenopus laevis oocytes allows electrogenic transport to be studied under voltage clamp conditions. 2. We have investigated the transport of the pharmacological substrate, L-serine-O-sulphate transport by EAAT1 and EAAT2. The EC50 values for L-serine-O-sulphate transport by EAAT2 showed a steep voltage-dependence, increasing from 152+/-11 microM at - 100 mV to 1930+/-160 microM at 0 mV. In contrast to EAAT2, EC50 values for L-serine-O-sulphate transport by EAAT1 were relatively constant over the membrane potential range of - 100 mV to 0 mV. The EC50 values for L-glutamate and D-aspartate transport, by EAAT2, were also relatively constant over this membrane potential range. 3. Chloride ions modulated the voltage-dependent changes in EC50 values for transport by EAAT2. This effect was most apparent for L-serine-O-sulphate transport, and to a lesser extent for L-glutamate and not at all for D-aspartate transport by EAAT2. 4. Extracellular sodium and proton concentrations also modulated the voltage-dependence of L-serine-O-sulphate EC50 values for EAAT2. 5. We speculate that these different properties of L-serine-O-sulphate transport by EAAT2 compared to other substrates may be due to the much stronger acidity of the sulphate group of L-serine-O-sulphate compared to carboxyl groups of L-glutamate or D-aspartate. 6. These results highlight some of the differences in the way different glutamate transporter subtypes transport substrates. This may be used to understand further the transport process and develop subtype selective inhibitors of glutamate transport.
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PMID:Serine-O-sulphate transport by the human glutamate transporter, EAAT2. 960 66

We reported the high effectiveness of electrolyzed strong acid aqueous solution (ESAAS) in cleaning hemodialysis lines. Although ESAAS has a strong bactericidal action, one concern is its strong acidity. It has a pH of 2.3-2.7, more than 1,000 mV in oxidation-reduction potential (ORP), and 10-50 ppm of available chlorine. The possibility of metal corrosion, degradation of synthetic resins, chorine gas emission, or dissolving calcium carbonate (CaCO3) deposits due to ESAAS's acidity was tested using in vitro experiments. The bactericidal and antiviral effects of various ESAAS's were also tested. Metal corrosion and synthetic resin degradation, although they occurred, were not serious. There were no problems with chlorine gas emission and dissolving of CaCO3 deposits. Each type of ESAAS showed almost the same bactericidal and antiviral effect, but in some cases differences were observed.
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PMID:The effect of electrolyzed strong acid aqueous solution on hemodialysis equipment. 1061 23

A new superacid, H(CB11H6X6) (where X = chlorine or bromine), whose conjugate base is the exceptionally inert CB11H6X6- carborane anion, separates Bronsted acidity from oxidizing capacity and anion nucleophilicity in a manner not previously achieved. Reaction of this superacid with C60 gives HC60+ as a stable ion in solution and in the solid state. In a separate experiment, an oxidant was developed such that the long-sought C60.+ ion can be synthesized in solution. The preparation of these two fullerene carbocations is a notable departure from the prevalent chemistry of C60, which is dominated by the formation of anions or the addition of nucleophiles. The H(CB11H6X6) superacid overcomes the major limitations of presently known superacids and has potentially wide application.
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PMID:Taming superacids: stabilization of the fullerene cations HC60+ and C60.+. 1088 20

The kinetics of oxidation of perchloroethylene (PCE), trichloroethylene (TCE), three isomers of dichloroethylene (DCE) and vinyl chloride (VC) by potassium permanganate (KMnO(4)) were studied in phosphate-buffered solutions of pH 7 and ionic strength approximately 0.05 M and under isothermal, completely mixed and zero headspace conditions. Experimental results have shown that the reaction appears to be second order overall and first order individually with respect to both KMnO(4) and all chlorinated ethenes (CEs), except VC. The degradation of VC by KMnO(4) is a two-consecutive-step process. The second step, being the rate-limiting step, is of first order in VC and has an activation energy (E(a)) of 7.9+/-1 kcal mol(-1). The second order rate constants at 20 degrees C are 0.035+/-0.004 M(-1) s(-1) (PCE), 0.80+/-0.12 M(-1) s(-1) (TCE), 1.52+/-0.05 M(-1) s(-1) (cis-DCE), 2.1+/-0.2 M(-1) s(-1) (1,1-DCE) and 48.6+/-0.9 M(-1) s(-1) (trans-DCE). The E(a) and entropy (DeltaS(*)) of the reaction between KMnO(4) and CEs (except VC) are in the range of 5.8-9.3 kcal mol(-1) and -33 to -36 kcal mol(-1) K(-1), respectively. Moreover, KMnO(4) is able to completely dechlorinate CEs, and the increase in acidity of the solution due to CE oxidation by KMnO(4) is directly proportional to the number of chlorine atoms in CEs.
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PMID:Oxidation of chlorinated ethenes by potassium permanganate: a kinetics study. 1156 7

The unexpected greater Lewis acidity of BCl(3) than BF(3) with respect to strong bases such as NH(3) has been the subject of much discussion. A number of explanations have been proposed, among which the most popular and most widely quoted is that stronger back-donation from fluorine than from chlorine decreases the availability of the otherwise empty 2p orbital on boron from accepting an electron pair from a base. In contrast, toward weak bases such as CO, BF(3) is a stronger Lewis acid than BCl(3). We have reinvestigated the relative acid strengths of BF(3) and BCl(3) toward Lewis bases by calculating geometries and atomic charges for the following adducts: BF(3).NH(3), BF(3).N(CH(3))(3), BF(3).OH(2), BF(3).O(CH(3))(2), BCl(3).NH(3), BCl(3).N(CH(3))(3), BCl(3).OH(2), and BCl(3).O(CH(3))(2). Our results show that the halogen ligands remain close-packed throughout the formation of an adduct and that the bond lengths increase accordingly. It takes more energy to lengthen the short strong BF bonds than the longer weaker BCl bonds and it is for this reason that BCl(3) is a stronger Lewis acid than BF(3) toward a strong base such as NH(3). In contrast, in the formation of a complex with a weak base such as CO, the BX(3) is barely distorted from planarity and so the acidity of BF(3) is greater than that of BCl(3) because the charge on boron is greater in BF(3) than BCl(3).
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PMID:Ligand Close-Packing and the Lewis Acidity of BF(3) and BCl(3). 1167 Nov 88


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