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PubMed1982

Effects of local anesthetics and related compounds on the endocytosis and catabolism of asialo-glycoproteins in isolated hepatocytes.

The effects of local anesthetics, including procaine and dibucaine, and some related amine compounds, such as dansyl-cadaverine, were studied with respect to their effects on the uptake and degradation of asialo-glycoproteins in isolated hepatocytes. 0.5 mM of either dibucaine or dansyl-cadaverine reduced the rates of uptake to 18-19% of control value; other amines were less effective. Dibucaine and dansyl-cadaverine both acted by reducing the surface binding capacity of the cells as well as by reducing the rate of internalization of surface-bound asialo-glycoprotein. All of the compounds that affected the uptake, including dansyl-cadaverine, also reduced the rate of degradation. This effect could be studied separately from their effect on uptake. The concentrations that were required in order to reduce degradation were, in general 0.5-0.25 of those which caused a reduction in the uptake. Even though dibucaine, lidocaine and dansyl-cadaverine were found to accumulate in the lysosomes, it was concluded from studies with isopycnic centrifugation in sucrose gradients that all three compounds inhibited the rate of transfer of endocytosed protein from endocytic vesicles to lysosomes. This effect could be due to a reduced rate of fusion between endocytic vesicles and lysosomes.

Anesthetics, Local↗
PubMed1988

Cocaine inhibits muscarinic cholinergic receptors in heart and brain.

(-)-Cocaine inhibits M2 muscarinic cholinergic binding measured with [3H]quinuclidinyl benzilate in heart and brain with a Ki of 18.8 microM. The cyclic nucleotide 5'-guanylylimidodiphosphate does not shift the competition curve, suggesting that (-)-cocaine is an antagonist. (-)-Cocaine also reverses the methacholine-induced inhibition of guinea pig atrial contractions at a similar concentration. Although (+)-cocaine is about 8-fold more potent than (-)-cocaine, (+)-cocaine is not present in extracts of the coca plant. Of the many compounds tested, only (-)-cocaine and lidocaine have a higher affinity at M2 muscarinic receptors than at M1 receptors; other compounds such as (+)-cocaine, norcocaine, procaine and dimethocaine are equipotent at the M1 and M2 subtypes. These results indicate that cocaine can act as an antimuscarinic agent, particularly at higher, toxic doses.

Animals↗
PubMed1993

[Preparation and pharmacologic profile of derivatives of alkoxyphenylcarbamic acid with potential effects on the cardiovascular system].

In a systematic study of the relationship between the chemical structure and beta-adrenolytic activity, eleven derivatives of the 4-alkoxysubstituted phenylcarbamic acids were prepared. The beta-adrenolytic efficiency of the compounds was studied in the isolated spontaneously beating guinea-pig atria and expressed as pA2 values against isoprenaline tachycardia. Negative chronotropic and antidysrhythmic activity were also evaluated. All of the compounds studied were local anesthetically active and their indexes of efficiency were 3-50 fold higher in comparison with standards cocaine and procaine. The acute toxicity of the compounds was within the acceptable limits.

Animals↗
PubMed1997

[Pharmaco-toxicologic evaluation of newly synthesized analogs of propafenone].

The basic pharmacological evaluation of five analogues of propafenone was the aim of the present paper. Antiarrhythmic activity of the compounds at 10(-5) mol.kg-1 was established in guinea-pigs using experimental arrhythmias induced by ouabain and aconitine. The beta-adrenolytic efficiency of the compounds was studied in the isolated spontaneously beating guinea-pig atria and expressed as pA2 values against isoprenaline tachycardia. All of the compounds studied were local-anaesthetically active and their indexes of efficiency were 1-5 fold higher in comparison with the standards cocaine and procaine. The acute toxicity of the compounds was within acceptable limits.

Adrenergic beta-Agonists↗
PubMed1985

A correlative study of internode proportions and sensitivity to procaine in regenerated frog sciatic nerves.

A comparison of regenerated and normal frog sciatic nerves showed a marked reduction in conduction velocity from 37.5 to 15.2 m/s with little change in the absolute refractory period. Changes in conduction velocity corresponded to a reduced mean axon caliber (4.8 versus 6.6 micron). Regenerated nerves also had markedly foreshortened internodes (mean of 309 versus 1236) micron) and thinner sheaths than controls. The geometric proportions of internode length/fiber caliber (l/d) was reduced to approximately one-third of normal. Regenerated nerves were more easily blocked by exposure to 3 mmol/liter procaine than controls, showing greater increase in the absolute refractory, or decreases, respectively, in the peak of the alpha-wave and the area of the compound action potential; the effect of procaine on conduction velocity was less marked. Exposure of various lengths of nerves in chambers of 1, 3, or 20 mm length revealed greater differences for the shorter chambers. The data indicated that some effects could be attributed to the foreshortening of the regenerated internodes. The main difference between normal and regenerated nerves, however, had to be attributed to changes in the nodal membrane characteristics of the latter.

Action Potentials↗
PubMed2004

Massive cell vacuolization induced by organic amines such as procainamide.

Procaine and some other basic drugs reportedly induce vacuolization of various cell types. We addressed the concentration-effect and structure-activity relationships as well as the mechanism of this effect using three cell lines. Massive vacuolization occurs over several hours in primary cultures of rabbit pulmonary artery smooth muscle cells (SMCs) and COS-1 cells in response to procaine and loosely related amine compounds (procainamide, N-acetyl-procainamide, metoclopramide, lidocaine, triethylamine, nicotine) used at 2.5 mM. Furthermore, chloroquine, propranolol, diphenhydramine, and neutral red are active in this respect at 100 to 250 microM in SMCs and COS-1 cells. Human embryonic kidney 293 cells mildly responded to triethylamine, nicotine, and propranolol only. Tetraethylammonium was uniformly inactive, as well as many other drugs in all three cell types (concentrations up to 2.5 mM). Procainamide does not induce apoptosis in SMCs treated for up to 48 h, although the vacuolization is sustained and proliferation and migration are reduced during this period. Procainamide-induced vacuolization is reversible on drug washing, largely prevented by bafilomycin A1 cotreatment, and has a tentatively identified Golgi origin (uptake of ceramide-C5). Procainamide and neutral red are concentrated in SMCs in a bafilomycin A1-sensitive manner. The preventive effect of bafilomycin A1 suggests that the vacuoles originate from the osmotic swelling of acidic organelles in which the charged basic drugs are trapped at low pH. Drug transport at the plasma membrane may be limiting for this type of response, as suggested by the cell type selectivity of agents and the inhibitory effect of some drugs such as quinidine.

Animals↗
PubMed1979

Effect of 60Co-irradiation on penicillin G procaine in veterinary mastitis products.

The effect of 60Co-irradiation on penicillin G procaine in a peanut oil-based veterinary mastitis product was examined by reversed-phase high-performance liquid chromatography (HPLC). The HPLC method is capable of separating and quantifying procaine, penicillin G, and various degradation compounds. Penicillin G recovery from a placebo formulation was 100.4% with a relative standard deviation of less than 1%. When irradiated at 4.0 Mrads, the penicillin G in two product lots decreased slightly (approximately 1-2%) with a corresponding increase in two compounds inherently present in bulk penicillin G powder. These compounds may be formed in abundance by treating penicillin G in an acidic solution. From the mass spectrometric analysis and the relative retention data with authentic compounds, these compounds were identified as benzylpenilloaldehyde and benzylpenaldic acid. Values obtained by the HPLC method on the product irradiated and stored at various temperatures correlated well with those of the microbiological assay. No significant decrease in the procaine was detected even after 4.0-Mrad irradiation. The HPLC method is applicable for analysis of other beta-lactam antibiotics.

Animals↗
PubMed2003

N-in-one permeability studies of heterogeneous sets of compounds across Caco-2 cell monolayers.

PURPOSE: The purpose of the study was to evaluate several n-in-one cocktails of heterogeneous compounds to increase the throughput of permeability studies across Caco-2 monolayers, to investigate the reliability and applicability of the method, and to develop fast and sensitive analysis for the compounds. Compounds with potential interactions in efflux and/or active transport were chosen. METHODS: Permeability experiments with verapamil, propranolol, midazolam, hydroxyzine, timolol, buspirone, procaine, naproxen, ketoprofen, and antipyrine as single compounds and in cocktails of 5-10 compounds were performed at 50 microM concentration both in the apical-to-basolateral and basolateral-to-apical direction. The compounds were quantified by liquid chromatography-electrospray tandem mass spectrometry (LC-ESI/MS/MS). Toxicity tests were performed to determine cellular damage. RESULTS: The analytical method was sensitive, accurate, and rapid. The individual permeabilities of compounds in cocktails correlated well with permeabilities as single compounds. No significant interactions between the compounds within the mixtures were observed, except for acidic compounds. The studied mixtures did not show any toxicity. CONCLUSIONS: The use of n-in-one cocktails is a suitable method to improve the capacity in routine permeability experiments and higher throughput screening of drug candidates, although potential interactions should always be borne in mind. The use of LC-ESI/MS/MS technology provides an excellent tool in fast and accurate analysis of small amounts of heterogeneous compounds.

Biological Transport↗