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I Simpson

Publications and source records attributed to I Simpson.

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Permeability of the cell-to-cell membrane channels in mammalian cell juncton.

The channels in the junctions of various mammalian cell types--primary cultures and lines--were probed with a series of linear fluorescent amino acid and peptide molecules of different size and charge. Permeability is limited by probe size and electronegativity, these two factors apparently being related reciprocally. In respect to both factors, mammalian junctional channels are more restrictive than insect channels; hence the mammalian channels are narrower, more polar, or both. The channels of the various mammalian cell types differed slightly from each other; in some types the serum of the culture medium affected the channel permeability.

Animals↗

Size limit of molecules permeating the junctional membrane channels.

The permeability of the cell-to-cell membrane channels in salivary gland cell junction (Chironomus thummi) was probed with fluorescent-labeled amino acids and synthetic or natural peptides. Molecules up to 1200 daltons pass through the channels with velocities depending on molecular size. Molecules of 1900 daltons or greater do not pass. This passage failure seems to reflect the normal size limit for junctional channel permeation; the channels continue to be permeated by the molecules up to 1200 daltons when these are mixed with the nonpermeant molecules. From this size limit a channel diameter of 10 to 14 angstroms is estimated.

Animals↗

Thiolester substrates for transamidating enzymes: studies on fibrinoligase.

Esters of thiocholine were shown to inhibit the crosslinking of fibrin clots by the transamidating enzyme, fibrinoligase (thrombin-activated fibrin-stabilizing factor or activated Factor XIII). Inhibition depended on the nature of the acylating group with the phenylpropionyl, phenylbutyryl, and trans-cinnamoyl esters being most effective of the compounds tested so far. Use of the thiolesters made it possible for the first time to study the reactions of fibrinoligase in fully synthetic substrate systems. Enzyme-catalyzed acyl-group transfers from the thiol-esters to a fluorescent amine [N-(5-aminopentyl) - 5 - dimethylamino - 1 - naphthalenesulfonamide] could be readily demonstrated and measured.Trans-cinnamoylthiocholine reacted with fibrinoligase in a totally calcium-dependent manner in the absence of any added amine, thus providing the first evidence for an esterolytic pathway for this enzyme. Spectral qualities, as well as appreciable extent of solubility in water, would seem to make trans-cinnamoylthiocholine a specially suitable substrate for further studies.

Acylation↗

Humans and hospitals.

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Attitude of Health Personnel↗

Effect of nizatidine and ranitidine on 24 hour intragastric pH, pepsin, prostaglandin E2 and serum gastrin concentrations in healthy volunteers.

In order to achieve possible greater therapeutic efficacy, ranitidine 300 mg bid (R2) may be given rather than 300 mg qhs (R1), or nizatidine 300 mg bid (N2) may be given rather than 300 mg qhs (N1). A randomized placebo-controlled crossover study was performed in six healthy volunteers (four males, two females) who ranged in age from 23 to 43 years, comparing R1, R2, N1 and N2 versus placebo (P), measuring 24 h intragastric pH by the aspiration technique, gastric juice pepsin and prostaglandin E2 (PGE2) concentrations, as well as serum gastrin concentrations. In all treatment groups, 24-h intragastric pH was higher than with P; the 24 h and daytime (0800-2200 h) pH was higher with N2 than with N1, but not with R2 versus R1. The percentage pH > or = 3 was greater with N2 than with N1 during the daytime. Night-time (2200-0800 h) and 24 h pepsin concentrations were higher in R2 than in R1, were similar in N1 and N2, and were lower in these treatment groups than in P. The gastric juice PGE2 concentration at night-time, but not at daytime, was increased in the four treatment groups compared with P. Despite the higher pH values at night-time in the treatment groups, the night-time concentrations of serum gastrin were unchanged, and yet during the daytime the higher values of pH were associated with increased gastrin concentrations when R2 or N2 were given, but not with R1 and N1. There was a negative correlation between intragastric juice pH and pepsin concentration during the daytime, and a positive correlation between pH and PGE2 concentration during the night-time. The slopes and y-axis intercepts between pH and pepsin or PGE2 concentrations differed between the placebo and the treatment groups, suggesting that these H2-receptor antagonists may have an effect on lowering pepsin and raising PGE2 concentrations in addition to their effects on pH. As the percentage of time over the 24 h period and night-time periods when the pH was greater than 3 was not different between ranitidine and nizatidine, the two regimens will likely have similar clinical efficacy.

Adult↗