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At least 217 records · Page 12Linked to original sources
PubMed1976

[Preparation and study of phytotoxic activity of anilides of the (+/-) hydratropic acid].

A series of ((+/-)-hydratropanilides variously substituted in the aniline nucleus (substances I leads to XXXIX) were prepared. The substances were studied for inhibition of the Hill reaction and for phytotoxicity. Comparison of the results of in vitro and in vivo tests did not often show strict correlation of data: in particular it seems probable that in the hydratropanilide series substances active on the isolated chloroplast are hindered in vivo in the absorption and transport phases and thus cannot reach the receptor sites.

Anilides↗
PubMed2003

Electron ionization-induced fragmentation of N-(alkoxymethyl)anilides.

Electron ionization-induced fragmentation patterns of the series of N-(alkoxymethyl)acetanilides and related formanilides and benzanilides have been studied. The main fragmentation reaction observed for all compounds studied is the loss of an alkyl radical from the N-alkoxymethyl group leading to the appropriate protonated N-acylformanilide derivatives. This reaction is accompanied by unusually high kinetic energy release. Other important fragmentations common for majority of the compounds studied are (i) loss of an aldehyde molecule derived from an alkoxyl group yielding an appropriate N-acyl-N-methylaniline, (ii) elimination of a C(n)H(2n)O(2) fragment derived from N-alkoxymethyl group and carbonyl group oxygen atom and (iii) formation of N-methyleneaniline radical cation.

Journal Article↗
PubMed1986

Experimental compound OR-K-242-HCl an anilide derivative slows conduction velocity of the heart in the conscious beagle dog.

OR-K-242-HCl is an antitussive compound. Because it resembles lidocaine structurally, one of its target organs may be the heart. In anaesthetized guinea pigs OR-K-242-HCl depressed function of the heart. The aim of the present study was to test effects of OR-K-242-HCl on the conduction velocity of the heart in the conscious beagle dog. OR-K-242-HCl was administered 6 mg/kg and 12 mg/kg i.v. and 6 mg/kg, 12 mg/kg, 24 mg/kg, and 36 mg/kg orally. The doses for lidocaine (reference substance) were 6 mg/kg, and 12 mg/kg i.v. and 6 mg/kg, 12 mg/kg, and 24 mg/kg orally. Five consecutive noisefree cycles of ECG were used before and every 15 min up to three hours after the drug administrations. For each cycle PQ-, QTC-, RR-interval, as well as, QRS-complex and heart rate were calculated. Both OR-K-242-HCl and lidocaine prolonged the conduction velocity in the atria and ventricles. After i.v. and oral administration OR-K-242-HCl induced stronger and more uniform responses than lidocaine. The oral drug administrations produced more sustained responses than the intravenous injections for both compounds.

Administration, Oral↗
PubMed1978

The pharmacokinetics and metabolism of the anilide local anaesthetics in neonates. I. Lignocaine.

The pharmacokinetics and metabolism of lignocaine in premature neonates was studied after subcutaneous administration. The collection of serial urine together with a limited number of blood samples from neonates enabled simultaneous computer fitting of data to a pharmacokinetic model. The disposition kinetics of lignocaine in four neonates were compared with similar data reported for adults. Neonates had prolonged t1/2 (neonate mean: 3.16 h; adult mean: 1.80 h), and an increased total volume of distribution (neonate mean: 2.75 l/kg; adult mean: 1.11 l/kg) compared with adults. Total plasma clearance (Cltp) normalised on body weight showed no significant difference between neonates (mean: 0.610 l/h/kg) and adults (mean: 0.550 l/h/kg). The urinary excretion of lignocaine and several of its metabolites was studied in 8 neonates and 11 adults. Neonates were shown to excrete much more unchanged lignocaine (mean: 19.67%) compared with adults (mean: 4.27%) and the proportion of the dose excreted as 4-hydroxyxylidine is considerably reduced in neonates (neonate mean: 8.89%; adult mean: 63.78%). The use of the two pharmacokinetic parameters, t1/2 and Cltp, as indices of drug elimination ability are discussed.

Adult↗
PubMed1978

Pharmacokinetics and metabolism of the anilide local anaesthetics in neonates. 11 Etidocaine.

The urinary elimination of etidocaine and several of its metabolites was investigated in neonates whose mothers had received one or more doses of etidocaine during labour. The urine collection period ranged among the neonates from 21.4 to 47.0 h post-partum. The total amounts of etidocaine and its metabolites recovered in neonatal urine represented a mean of 0.12% of the maternal dose. Some differences in the pattern of urinary metabolites were observed between neonates and adults. Mean half-life of elimination of etidocaine calculated from sigma-minus plots of the neonatal urinary data was 6.42 h. This is greater than that previously reported following intravenous administration of etidocaine to adults (2.6 h). The slower rate of elimination in neonates is probably due to an increased neonatal volume of distribution since there is evidence to show that etidocaine is extensively metabolised by the neonate.

Acetanilides↗