(1) The basilar artery was the most sensitive vessel and caprate (C10) was the most potent acid with an EC50 of 49 microM.
(2) The effects of taurocholate, caprylate, and EDTA-2Na for increasing colonic pore sizes and the degree of inulin permeation were less than those of caprate, laurate, or mixed micelles.
(3) Sodium salicylate or sodium caprate in the suppository with rHuEPO also increased its absorption.
(4) Caprate also inhibited contractions elicited by KCl, serotonin, and the thromboxane analogue U46619.
(5) Caprate, laurate, and mixed micelles at 0.25% caused this radius to increase significantly, thus making it possible for inulin to permeate the everted sac from the mucosal to the serosal side.
(6) On the other hand, the concentrations following the caprate or stearate administration decreased slowly and were maintained for as long as 4 h after dosing.
(7) The linear growth phase of S. gardneri was extended through seven days by supplementing the defined medium with continuous feeds of hydrolyzed casein and methyl caprate.
(8) The pharmacokinetics of 125 mg and 250 mg CZX-S, which contained 3% sodium caprate, were also evaluated as a single administration in 9 children (aged 6 years 4 months to 12 years 0 month) and in 11 children (aged 7 years 8 months to 12 years 4 months), respectively.
(9) The pharmacokinetics of newly developed ceftizoxime suppository (CZX-S) was studied in healthy volunteers and in children, compared with that of intramuscular CZX and intravenous CZX: In 8 volunteers (aged 19 to 24 years), each of 500 mg (potency) CZX-S containing 3%, 4% and 5% sodium caprate was compared with 500 mg intramuscular CZX and 500 mg intravenous CZX as a single administration in the cross-over method.
(10) Esterase activity was strongest against caproate (C6), caprylate (C8), nonanoate (C9), and caprate (C10) substrates.
(11) We examined the enhancing effect of sodium caprate (C10) on the jejunal absorption of a poorly absorbed drug, cefmetazole, in rats, in comparison with its colonic absorption (Pharm.
(12) When laurate or caprate was added to ferric cytochrome P-450 s (3P2 and 3E2), the spectrum was converted to that of the typical high-spin type, indicating the binding of the fatty acids to the substrate site of the cytochromes.
(13) Caprate, for example, increased the n-decanoyl-containing factors from the natural level of approximately 14% to approximately 80%.
(14) The enhancing effects of 0.25% sodium caprate (C10) and sodium caprylate (C8) on the paracellular permeation of seven water-soluble nonelectrolytes (inulin, polyethylene glycol 900, mannitol, erythritol, glycerol, thiourea, and urea) across the isolated rat colonic epithelium were examined using the Ussing-type chamber technique.
(15) Colonic absorption of poorly absorbable cefmetazole was shown to increase considerably by the addition of 1% sodium caprate, sodium laurate, and mixed micelles composed of sodium oleate and sodium taurocholate.
(16) Differences in the inhibition constants (Ki) of caprate and trifluoroethanol below pH 7.8 and in the pH dependence of Ki can be explained by the substitution of neutral Gln for positively charged His.
(17) The effects of sodium salts of medium-chain fatty acids, caprylate and caprate, on the penetration of a hydrophilic compound and a macromolecular compound across rabbit corneas in vitro were examined.
(18) Methyl caprate also enhanced the penetration of vitamin D3, erythromycin, triamcinolone acetonide, testosterone, and hydrocortisone.
(19) These results suggest that caprate enhances permeability via the transcellular route through membrane perturbation.
(20) AUC of CZX-S containing 3% sodium caprate was slightly smaller than that of CZX-S containing 4% or 5% sodium caprate, but 3.1 times that of the ABPC suppository in healthy volunteers.
Ester
Definition:
(n.) An ethereal salt, or compound ether, consisting of an organic radical united with the residue of any oxygen acid, organic or inorganic; thus the natural fats are esters of glycerin and the fatty acids, oleic, etc.
Example Sentences:
(1) These effects are similar to those reported for AVP and phorbol esters, activators of protein kinase C. Forskolin and isoproterenol, which induce cAMP accumulation, activated extractable topoisomerase II (maximum 5-15 min after treatment), but not topoisomerase I. Permeable cyclic nucleotide analogs dBcAMP and 8BrcGMP selectively activated extractable topoisomerase II and topoisomerase I activities, respectively.
(2) Preincubation of human neutrophils with recombinant tumor necrosis factor alpha has previously been shown by us to enhance superoxide production of neutrophils in response to the chemotactic peptide formyl-methionyl-leucyl-phenylalanine, and the phorbol ester, phorbol myristate acetate.
(3) Tumor promoting phorbol esters (1-1000 nM) could also inhibit PGE2 stimulated cAMP production dose dependently.
(4) These products were identified to be epimers of 5,12(S)-dihydroxy-eicosatetraenoic acid methyl ester (5,12(S)-diHETE-Me) and epimers of 11,12-diHETE-Me.
(5) Benzyloxycarbonylarginine p-nitrophenyl ester and other activated esters of N-a-sustituted arginine salts may be useful reagents for introduction of trypsin-labile protecting groups into peptide fragments for purpose of polypeptide semi-synthesis.
(6) The immunodetectable PKC level in hypothyroid liver was elevated 7.7-fold, whereas the phorbol-ester binding capacity and the immunodetectable alpha-PKC level were increased 2.4- and 2.6-fold, respectively.
(7) The presence of a previously unreported dipeptide transport mechanism within blood leukocytes and the selective enrichment of the granule enzyme, DPPI, within cytotoxic effector cells of lymphoid or myeloid lineage appear to afford a unique mechanism for the targeting of immunotherapeutic reagents composed of simple dipeptide esters or amides.
(8) Incubation of membrane with DL-Hcys alone (5 X 10(-5) M), the combination of both Ad (5 X 10(-5)) and DL-Hcys (5 X 10(-5)), or S-adenosyl-L-homocysteine (SAH) (1 X 10(-6)) strongly decreased the methyl ester formation.
(9) To this purpose, the formation of DHT has been measured in rat glial cell cultures after different time of exposure to TPA, 4 alpha-Ph, an active and an inactive phorbol ester respectively, and 8-Br-cAMP.
(10) Insulin incubation of plasma membranes pretreated with protease inhibitors (leupeptin, phenylmethylsulfonylfluoride) or with exogenous trypsin, but not chymotrypsin substrates (esters of arginine and tyrosine) yields an inactive supernatant on PDH.
(11) Lymphocyte stimulation by phorbol ester for a short time induces c-fos and c-myc expression, but has no effect on [3H]thymidine incorporation.
(12) The cryptoxanthin esters varied from 5 to 10% of the total carotenoids in Valencia orange juice concentrates and from 10 to 15% of the total carotenoids in Navel orange juice concentrates.
(13) Early in the regression process, cholesterol esters are reduced at least partly by hydrolysis to yield cholesterol, some of which may crystallize and inhibit rapid regression.
(14) The kinetics of the luminescent signal with the different luciferin esters varied significantly, indicating possible differences in the rates of uptake, breakdown and enzyme inhibition.
(15) In comparison to rat pancreas, [D-Phe6]BN-(6-13)ethyl ester, Ac-GRP-(20-26)ethyl ester, [D-Phe6,Cpa14, psi 13-14]BN-(6-14), [Leu14, psi 13-14]BN, and [Leu14, psi 9,10]BN had a 10,000-, 2,940-, 1,425-, 122-, and 4-fold, respectively, weaker affinity for BN receptors.
(16) Enzymatic lability does not, however, play as important a role as lipophilicity in the corneal and conjunctival penetration of cycloalkyl and aryl ester prodrugs.
(17) To determine whether the triadimefon-induced hyperactivity is due to an action on CNS catecholaminergic systems, we evaluated the effects of combined treatment of triadimefon with either the tyrosine hydroxylase inhibitor d,l-alpha-methyl-p-tyrosine methyl ester HCl (alpha MPT) or the amine depletor reserpine.
(18) Growth of C. albicans in the presence of AGE affected the yeast lipid in a number of ways: the total lipid content was decreased; garlic-grown yeasts had a higher level of phosphatidylserines and a lower level of phosphatidylcholines; in addition to free sterols and sterol esters, C. albicans accumulated esterified steryl glycosides; the concentration of palmitic acid (16:0) and oleic acid (18:1) increased and that of linoleic acid (18:2) and linolenic acid (18:3) decreased.
(19) In comparison with native counterparts, the in vitro-formed LDL2 and HDL + VHDL were characterized by lower levels of triglyceride and cholesterol ester and higher levels of free cholesterol and lipid phosphorus.
(20) Several histidine derivatives are not susceptible to the enzyme but do inhibit the enzyme activity competitively; the most effective inhibitors are L-histidine methyl ester (Ki = 3.66 mM) and beta-imidazole lactic acid (Ki = 3.84 mM).