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PubMed1993

Inhibition of the nicotinic acetylcholine receptor by barbiturates and by procaine: do they act at different sites?

1. The effects of three barbiturates and the local anesthetic procaine on the ion channel function of mouse nicotinic acetylcholine receptor (nAChR) muscle subtype expressed in Xenopus laevis oocytes were examined by whole-cell voltage-clamp technique. 2. A concentration-response curve for the specific nicotinic agonist dimethylphenylpiperazinium iodide (DMPP) was first determined. This agonist produced increasing whole-cell currents up to a concentration of 100 microM (EC50 = 13 microM), then decreased responses at higher concentrations. 3. The barbiturates (amobarbital, secobarbital, pentobarbital) and procaine produced reversible inhibition of DMPP-induced currents at clinically used concentrations. The two classes of drugs differed in the voltage dependence of the inhibition: procaine-induced inhibition was increased at more negative transmembrane holding potentials (-90 vs. -45 mV); whereas amobarbital-induced inhibition did not vary at different transmembrane potentials. 4. Mutant forms of the nAChR, containing single amino acid changes in the M2 regions of alpha and beta subunits, showed increased sensitivity to procaine but no change in sensitivity to amobarbital-induced inhibition. 5. These electrophysiologic studies provide further evidence that barbiturates and local anesthetics produce inhibition of the nAChR at different sites.

Allosteric Site↗
PubMed1998

Current usefulness of procaine penicillin in the treatment of pneumococcal pneumonia.

The aim of this study was to determine whether procaine penicillin could be used in the treatment of suspected pneumococcal pneumonia of mild to moderate severity in an area with a high prevalence of penicillin resistance. Forty-nine patients were treated with 1.2 x 10(6) U of i.m. procaine penicillin every 12 h. By intent-to-treat analysis, 40 of 49 patients were cured and no patient died. Streptococcus pneumoniae could be demonstrated in 17 patients; 5 of 17 isolates were resistant to penicillin (MICs 0.25-4 microg/ml). Fifteen of 17 patients were cured with procaine penicillin, one presented allergy, and one was a therapeutic failure. Mean penicillin serum levels were 2.39 +/- 1.16 microg/ml (peak) and 0.61 +/- 0.38 microg/ml (trough). The results suggest that procaine penicillin may still be useful in the empirical therapy of suspected pneumococcal pneumonia.

Adolescent↗
PubMed1993

Cocaine-like discriminative stimulus effects of procaine, dimethocaine and lidocaine in rats.

The discriminative stimulus effects of several local anesthetics and (+)-amphetamine were assessed in a drug discrimination based on the psychomotor stimulant cocaine. Two groups of adult male Sprague-Dawley rats were trained in two-lever operant chambers in a cocaine versus saline discrimination, or a cocaine versus procaine or saline discrimination, using a fixed ratio 20 schedule of food reinforcement. Cocaine, (+)-amphetamine and dimethocaine all dose-dependently substituted for the training dose of cocaine (10 mg/kg) in both procedures. While procaine and lidocaine showed partial substitution in the cocaine versus saline procedure, much less substitution occurred in the cocaine versus procaine or saline discrimination. These data demonstrate that it is possible to train rats to discriminate between cocaine and another local anesthetic procaine, resulting in an increased pharmacological specificity of cocaine discrimination. The fact that dimethocaine fully substituted for cocaine in both procedures indicates that this local anesthetic has more cocaine-like effects than others so far tested, which is consistent with results from other behavioral and neurochemical studies with this compound.

Aminobenzoates↗
PubMed1977

The interaction of hepatocyte plasma membranes with an azide derivative of procaine.

A photoreactive derivative of procaine, p-azidobenzoyldiethylaminoethanol hydrochloride, has been synthesized and used as a site-directed probe to label hepatocyte plasma membranes. The procaine derivative was shown to have membrane binding and Ca2+ displacement characteristics quite similar to that of procaine. Photolysis of the derivative in the presence of hepatocyte plasma membranes resulted in the covalent incorporation of the probe into both the protein and lipid fractions. Analysis of the labeled membranes by sodium dodecyl sulfate-polyacrylamide gel electrophoresis indicated that one membrane protein was significantly labeled with a molecular weight of 21 400 in addition to membrane lipids. Both binding and labeling could be inhibited in the presence of an excess of procaine. The labeled membrane components may be involved in the binding of Ca2+ to the membrane system.

Animals↗
PubMed1987

NMR investigation of the influence of procaine and its metabolites on the water exchange through human erythrocyte membranes.

The effect of procaine hydrochloride and its metabolites on the diffusional water exchange through erythrocyte membranes was investigated at 37 degrees C and at concentrations ranging between 5 X 10(-5) M and 5 X 10(-1) M by using the NMR manganese doping method. Procaine hydrochloride and 2-diethylaminoethanol have a moderate stimulating effect on the water exchange, of up to 20% at concentrations ranging between 10(-3) and 10(-2) M, while an increasing inhibitory effect was found at higher concentrations. The p-aminobenzoic acid has no effect on the water exchange up to 10(-2) M and, at higher concentrations, and apparent decreasing inhibition was noticed which is thought to be an artefact due to the uptake of Mn2+ by the cells. The temperature dependence studies suggest that procaine HCl enhances the uptake of Mn2+ by the cells. An opposite effect was found for rigid erythrocytes. The p-aminobenzoic acid and 2-diethylaminoethanol appeared to be more effective than procaine hydrochloride in increasing the uptake of Mn2+.

4-Aminobenzoic Acid↗
PubMed1987

Intravenous procaine as a probe of limbic system activity in psychiatric patients and normal controls.

Evidence from animal and human studies suggests that procaine hydrochloride may selectively activate limbic system structures and suppress neocortical structures. We administered a series of intravenous bolus doses of procaine hydrochloride to 31 subjects (7 with affective disorders, 17 with borderline personality disorder, and 7 healthy normal volunteers). Dose-related cognitive and sensory distortions and illusions were observed; affective experiences ranged widely from euphoric to dysphoric. Topographic electroencephalogram (EEG) analysis indicated selective increases in fast activity (26-45 Hz) over the temporal lobes; the degree of increase in this activity correlated with degree of dysphoria experienced. Procaine was associated with increases in secretion of cortisol, adrenocorticotrophic hormone (ACTH), and prolactin, but not with growth hormone. These preliminary data are consistent with the possibility that procaine might serve as a clinically useful probe of psychosensory, affective, electrophysiological, and endocrine effects referable to the limbic system.

Adrenocorticotropic Hormone↗
PubMed1994

Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons.

Previous studies have shown that local anesthetics block voltage-dependent Na+ channels and nicotinic acetylcholine receptors. The present study investigated the effect of the local anesthetic, procaine on another ligand-gated ion channel, the 5-HT3 receptor, in rat nodose ganglion neurons. Procaine (0.01-100 microM) inhibited the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. The inhibition was fully reversible, concentration-dependent but not sensitive to changes in membrane potential. Concentration-response curves indicated that procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM. These observations suggest that one of the actions of procaine in nervous system is on 5-HT3 receptors.

Animals↗
PubMed1984

Effects of procaine on the oxidative phosphorylation of brain mitochondria from senescent rats.

Senescence affects cerebral metabolic functions. Various drugs have been tested to counteract the effects of aging on the brain. In this paper, we studied the influence of treatment using procaine, 1 mg per 100 g body weight, injected over a period of 3 days, to both young and old rats, on the phosphorylative oxidation properties of cerebral mitochondria. Respiratory activity decreased significantly in the brain of old rats. This reduction of oxygen consumption measured in the presence of glutamate, reached 31% in state 4, 25% in state 3 and, in the presence of succinate, 23% in state 4 without significant changes in state 3. The injection of procaine into young rats induced a significant increase of oxygen consumption rate with both glutamate and succinate as substrates. The same treatment administered to old rats was followed by a rise in respiratory activity, with values close to those observed in young control rats. Although the mechanism of action of procaine is not yet clear, there is some evidence that it interacts with membrane phospholipid sites. Therefore, it may be concluded that procaine facilitates oxygen transport towards the mitochondrial matrix by modifying the membrane structure in both old and young rats, although, in the latter case, this increase is not intended to improve the energetic properties of the mitochondrion.

Aging↗
PubMed1982

Locomotor activity of rats in open field after microinjection of procaine into superior colliculus or underlying reticular formation.

Whereas large lesions of the superior colliculus in rats increase locomotor activity in the open field, bilateral collicular microinjections of muscimol (an agonist of the inhibitory neurotransmitter GABA) have been reported to reduce open-field activity. This difference might be due to muscimol's acting on a subpopulation of collicular neurones, or to some feature of the microinjection technique. The issue was investigated by observing open-field behavior after reversible lesions produced by bilateral microinjections of the local anaesthetic procaine (10-300 micrograms in 0.5 microliter) into midbrain sites. Injections of procaine into the superior colliculus produced effects similar to those reported after muscimol injections: both locomotor activity and other exploratory responses were suppressed, with the rats spending much of their time motionless in an alert posture. In contrast, animals with injections of procaine into the mesencephalic reticular formation (MRF) ventral to the superior colliculus resembled rats given large collicular lesions: they showed very striking increases in locomotor activity, while their rearing and exploratory head movements were reduced. It is suggested that in some experiments large collicular lesions may have increased locomotor activity in the open field because they invaded underlying MRF. However, it is also possible that in rodents the acute effects of collicular inactivation, as assessed by microinjection of muscimol or procaine, are different from the chronic effects that are observed in experiments with electrolytic or radiofrequency lesions.

Animals↗
PubMed1993

The effects of delay of reinforcement and dose on the self-administration of cocaine and procaine in rhesus monkeys.

Delays of reinforcement were imposed while three rhesus monkeys intravenously self-administered either cocaine or procaine to determine whether the magnitude of delay-induced reductions in infusion frequency were dose- or drug-dependent. Drug-maintained baselines demonstrating the greatest resistance to change under delay conditions might be conceptualized as involving the greatest strength of responding and include drug reinforcers with the greatest efficacy. Under baseline conditions, cocaine or procaine was infused contingent upon lever pressing according to fixed ratio 10 schedules during daily, 1-h experimental sessions. Under delay conditions, a 120-s delay of reinforcement was inserted between the completion of each fixed ratio contingency and infusion delivery. Tests under baseline and delay conditions alternated until several doses of cocaine (3, 10, 33, 100, and 300 micrograms/kg), and subsequently, of procaine (33, 100, 300, 1000, and 3000 micrograms/kg) were tested. The results indicated that during both baseline and delay conditions increases in dose of either drug resulted in increases followed by decreases in the number of infusions obtained. Introducing delays of reinforcement resulted in decreases in the number of infusions obtained at a given dose. Generally, however, when reinforcement delays were imposed the decreases in infusion number, as a percentage of baseline number, were less at the higher doses of both drugs. The doses of procaine which were maximally effective as reinforcers (i.e. during which infusion number was minimally reduced by delay) were as effective as the maximally effective doses of cocaine.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1988

Effect of procaine on cultivated human WI-38 fibroblasts.

Procaine is a local anesthetic, also used in experimental gerontology and has been tested in cultivated human WI-38 fibroblasts. This molecule was found to enhance growth rate and cell densities in actively dividing cultures. As the cells aged, however, this stimulatory effect diminished and finally vanished. In a long term experiment the enhancement of growth of procaine treated cultures was finally replaced by a toxic effect even at low concentration. The amount of the thermolabile enzyme found in phase III cells did not change when procaine was added to the culture medium. In this cellular aging model, procaine behaved like a metabolic stimulator of actively dividing cells but not as an "antiaging" molecule as it is sometimes assumed.

Cell Division↗
PubMed1987

The effects of procaine, strychnine and penicillin on nociceptive neurons in leech segmental ganglia.

Procaine, strychnine and penicillin selectively depolarized the membrane potential and prolonged the action potential recorded in the lateral but not the medial nociceptive (N) cell in the hirudinid leech Macrobdella decora. In contrast, procaine did not differentiate between medial and lateral N cells in two other hirudinid leeches Hirudo medicinalis and Haemopis marmorata. In these species, the drug equally decreased the amplitude of action potentials in both types of N cells without effecting their resting membrane properties. In the nociceptive neurons of the glossiphoniid leech Haementeria ghilianii which possesses only one type of N cell, procaine produced a depolarization and prolonged the action potential. This finding indicates that the single pair of N cells in Haementeria is of the lateral type. The results suggest that the lateral type N cell in Macrobdella and Haementeria share a unique Na+-dependent conductance which is selectively opened by the local anesthetics procaine and strychnine as well as by penicillin. This conductance is either not present or insensitive to the drugs in the homologous N cells in the two other leech species examined.

Animals↗
PubMed1993

Procaine effects on single sarcoplasmic reticulum Ca2+ release channels.

The effects of the Ca(2+)-induced Ca2+ release blocker procaine on individual sarcoplasmic reticulum Ca2+ release channels have been examined in planar lipid bilayers. Procaine did not reduce the single channel conductance nor appreciably shorten the mean open times of the channel; rather, it increased the longest closed time. These results indicated that procaine interacted selectively with a closed state of the channel rather than with an open state. Gating of the sarcoplasmic reticulum Ca2+ release channel was described by a modified scheme of Ashley and Williams (1990. J. Gen. Physiol. 95:981-1005), including an additional long-lived closed state. Computer simulations determined that procaine was more likely to interact with this long-lived Ca(2+)-bound closed state of the channel rather than with other states of the channel. Simulations with the same model were also able to reproduce a prominent Ca(2+)-sensitive transition between "random" and "bursting" forms of gating of the channel, variations of which may account for "gearshift" behavior reported in studies with this and other single channels.

Animals↗
PubMed2003

Procaine-induced enhancement of fluid-phase endocytosis and inhibition of exocytosis in human skin fibroblasts.

Local anaesthetics are often applied directly onto the skin, and for this reason the effect of some local anaesthetics upon morphology and cytoskeleton organisation in human skin fibroblasts was investigated. In this paper the authors report that procaine (p-aminobenzoic acid diethylamino-etyl ester hydrochloride) induced vacuolisation of cytoplasm and great enhancement of neutral red accumulation in human skin fibroblasts cultured in vitro. Procaine-induced vacuolisation of cell's cytoplasm was observed to be associated with the enhanced uptake and inhibited release of fluid taken by endocytosis. All these effects appeared fully reversible. The cell vacuolisation cannot be prevented by 3-methyadenine, brefeldine A, and cytochalasine D. On the other hand, nocodazole and caffeine prevent cytoplasm vacuolisation induced by procaine. These observations suggest that procaine-induced formation of great vacuoles is due to an impairment of membrane traffic between endosomes. The authors' results also demonstrate that neutral red uptake assay, if used as a cell viability test, must be interpreted with great caution.

Cells, Cultured↗
PubMedDate not supplied

Changes in the flow properties of phospholipid dispersions induced by procaine hydrochloride. Effect of pH and temperature.

Since local anaesthetics are known to interact with membrane lipids, we have examined the changes taken place by procaine hydrochloride in lipid matrices as a function of pH. Rheological methods might give useful information on the association of this anaesthetic with soybean lecithin. The procaine interacted with negatively charged phospholipid polar head groups at pH 4. This system exhibits a loosening in the tight arrangement of phospholipid molecules caused by the addition of procaine as a function of this anaesthetic's concentration. The flow enthalpy values as a function of procaine-lipid ratio shows biphasic behaviour and suggests a phase transition when the anaesthetic concentration goes from 10 to 14 mM and temperatures dip below 10 degrees C.

Chemical Phenomena↗
PubMed2001

Retention behaviour and fluorimetric detection of procaine hydrochloride using carboxymethyl-beta-cyclodextrin as an additive in reversed-phase liquid chromatography.

The retention behaviour of procaine hydrochloride on an Alltima octadecyl silica (C18) column, with a mobile phase containing negatively charged carboxymethyl-beta-cyclodextrin (CM-beta-CD), influenced by a combination of hydrophobic and electrostatic interactions was systematically investigated. Various factors affecting the retention of procaine on the C18 column such as the concentration of CM-beta-CD, pH and the methanol percentage in the mobile phase, were studied. An equation was applied to estimate the apparent binding constant of the CM-beta-CD-procaine inclusion complex as an aid for understanding the retention mechanism. The first analytical application of CM-beta-CD as a mobile phase additive for the determination of procaine was developed. The calibration curve was linear in the range 22-1360 ng ml(-1) with an RSD of 2.1%. The detection limit based on 3sigma was 1 ng ml(-1) with fluorimetric detection at the excitation and emission wavelengths of 305 nm and 350 nm, respectively. The limit of quantitation based on 10sigma was 22 ng ml(-1). The proposed method has been successfully applied to real sample analysis.

Chromatography, Liquid↗
PubMed1994

Intracavernous injection of prostaglandin E1 plus procaine in the treatment of erectile dysfunction.

Despite the availability of prostaglandin E1 for more than 7 years as a diagnostic and therapeutic tool in patients with erectile dysfunction, the problem of penile discomfort after prostaglandin E1 application has remained unsolved. In a randomized, double-blind, crossover study we investigated the effect of 2 different prostaglandin E1-procaine concentrations on 24 patients suffering from pain following intracorporeal injection of prostaglandin E1 alone. Intracavernous injection of 20 micrograms. prostaglandin E1 with 10 mg. procaine (study 1) failed to improve local painful sensations. The combination of 20 micrograms. prostaglandin E1 with 20 mg. procaine (study 2) decreased the incidence of local pain significantly (p < 0.01). These preliminary results show that the combination of prostaglandin E1 plus procaine represents a beneficial alternative in patients with penile pain due to the single substance.

Adult↗
PubMed2002

Procaine into the VMH inhibits IBAT activation caused by frontal cortex stimulation in urethane-anesthetized rats.

This experiment tested the effect of procaine injection into the ventromedial hypothalamus on the sympathetic and thermogenic activation induced by frontal cortex stimulation. Oxygen consumption, firing rate of the sympathetic nerves to interscapular brown adipose tissue (IBAT), along with IBAT and colonic temperatures were monitored in fasted male Sprague-Dawley rats before and during 25 min after an electrical stimulation of the frontal cortex. The same variables were monitored in rats with administration of procaine into the ventromedial hypothalamus. The results show that cortical stimulation increases oxygen consumption, sympathetic firing rate, IBAT and colonic temperatures. The increase in sympathetic firing rate was reduced by procaine injection, and the increase in IBAT and colonic temperatures as well as oxygen consumption was fully inhibited by procaine. These findings suggest that the ventromedial nucleus plays an important role in the sympathetic and thermogenic changes induced by cortical stimulation.

Action Potentials↗