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At least 73 records · Page 4Linked to original sources
PubMed1993

[Local anesthetics. CX. Preparation, activity and partition coefficients of pyrrolidinoethylesters of 2-, 3- and 4-alkoxy-substituted phenylcarbamic acids].

By pyrrolidinoethylalcohol addition on 2-, 3- and 4-alkoxy-substituted phenylisocyanate in non-aqueous toluene medium a series of 30 compounds of the type Pyrrolidinoethylesters of 2-, 3- and 4-alkoxy substituted phenylcarmabim acids were prepared. Pharmacological evaluation results shown after comparing with cocaine and procaine standards that these compounds have a higher index of effectiveness in both types of local anaesthesia. The maximum effectiveness of surface anaesthesia shows Pyrrolidinoethylester of 2-octyloxy phenylcarbamic acid which is 204-times more effective as cocaine. The maximum effectiveness of infiltration anaesthesis shows Pyrrolidinoethylester of 2-heptyloxy phenylcarbamic acid which is 66-times more effective as procaine. Prepared compounds are more effective in the case of surface anaesthesia as in the case of infiltration anaesthesia and they have comparatively high values of partition coefficients P' and P' cal. Comparison of prepared compounds effectiveness and analogic piperidinoethylesters shows that in more cases they are either equal or nearer effective. The values of their P' and P' cal correlate with these results.

Anesthetics, Local↗
PubMed1990

Microinjection of cocaine into the nucleus accumbens elicits locomotor activation in the rat.

Cocaine is believed to exert its psychostimulant effects through activation of the mesocorticolimbic system. Although the nucleus accumbens, in particular, has been hypothesized as the site of action of cocaine's stimulating effects, there is no direct evidence that microinjection of cocaine into this region produces behavioral activation. The present experiments investigated the locomotor response to microinjection of cocaine (0, 10, 30, 100 micrograms/0.5 microliter) into the nucleus accumbens in rats. Cocaine elicited a pronounced, dose-dependent motor activation of approximately 60 min duration. This stimulant effect was blocked by prior administration of a dopamine (DA) receptor antagonist, cis-flupenthixol. The response to cocaine was differentiated from nucleus accumbens microinjections of procaine and lidocaine, compounds that have potent local anesthetic effects but little affinity for the dopamine-uptake site. Neither procaine nor lidocaine (0, 10, 30, 100 micrograms/0.5 microliter) had any overall effect, although activity was somewhat decreased in the initial part of the test session and increased at the end, relative to control activity. Cocaine injected into the anterior dorsal or ventrolateral striatum (100 micrograms) also increased motor activity; procaine and lidocaine had no effect. Cocaine injected into the ventrolateral striatum significantly increased stereotypy. The amplitude of motor activation following cocaine injection into nucleus accumbens was much greater than that elicited at the other striatal sites. Further, observation of the time course of motor activation following cocaine injection into the anterior dorsal and ventrolateral striatum suggested that the motor effect was due to diffusion, most likely to the nucleus accumbens.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1978

Effect of lorcainide, a new antiarrhythmic compound, on the changes in heart rhythm induced by intravenous injection of adenosine-5'-diphosphate in rats.

In rats, the intravenous injection of 1 mg/kg A.D.P. (adenosine-5'-diphosphate) results in transient thrombocytopenia, bradycardia and arrhythmias. Pre-treatment of the animals with the antiarrhythmic compounds lorcainide, aprindine, procaine (1.25, 2.5, 5 mg/kg i.v.) and xylocaine (5, 10, 20 mg/kg i.v.) before A.D.P. injection results in a reduction of bradycardia and a faster normalization of heart rate. All 4 compounds were equipotent in this respect, but the higher dose of xylocaine used should be stressed. The duration of irregular heart rhythm after A.D.P. injection was significantly shortened by all 4 compounds. Peak thrombocytopenia after A.D.P. administration is reduced only by lorcainide and the highest dose of aprindine, with two dose levels of xylocaine, but is not reduced by procaine. Suloctidyl (50 mg/kg orally) had no effect on any of the parameters registered. From this study we conclude that the normalization by the compounds of cardiac rate and rhythm disturbances after A.D.P. is due to their direct antiarrhythmic effect rather than to inhibition of platelet aggregation.

Acetamides↗
PubMed1993

[Local anesthetics. VXII. Preparation and effectiveness of dibasic alkylesters of 2-, and 3-alkoxy-substituted phenylcarbamic acids].

In a series of 24 compounds of the type of dibasic alkylesters of 2-, and 3-alkoxy substituted phenylcarbamic acids, esterified alcohols 1-dipropylamino-3-pyrrolidino (piperidino or perhydroazepino)-2-propanol were used. It follows from the results of pharmacological evaluation that these compounds possess a high index of effectiveness in surface and infiltration anaesthesia compared to the standards of cocaine and procaine. Maximum effectiveness in surface anaesthesia was shown by [1-dipropylaminomethyl)-2- (piperidino)ethyl]-ester of 3-butoxyphenylcarbamic acids whose activity is as much as 180 times higher than that of cocaine. Maximum effectiveness in infiltration anaesthesia was shown by [1-dipropylaminomethyl)-2-(pyrrolidino)ethyl] ester of pentyloxyphenylcarbamic acid achieving an activity 250 times higher than that of standard procaine. The prepared compounds are more effective in the case of infiltration than in the case of surface anaesthesia.

Anesthetics, Local↗
PubMed1992

Study of local anaesthetics. Part 98(3): Preparation and local anaesthetic activity of 4-alkylpiperazinoethyl esters of o-heptyloxyphenylcarbamic acid.

During the course of study of variations in the basic moiety of heptacainium chloride 10 derivatives of 4-alkylpiperazinoethyl esters of o-heptyloxyphenylcarbamic acid were prepared. Pharmacological investigation indicated that practically all the new compounds were several times more active than standards (cocaine and procaine). The most effective compound was 1-[2-(o-heptyloxyphenylcarbamoyloxy)ethyl]-4-butyl-piperazinium dichloride, which was 142 times more active than cocaine and 266 times more active than procaine.

Anesthetics, Local↗
PubMed1988

Treatment of rabies in mice and foxes with antiviral compounds.

Thirty four chemical compounds were injected into rabies infected mice by intramuscular (i.m.) route. Twenty four compounds such as well known therapeutic agents: amantadine, lipacids, phenol compounds, didemnin-B, procaine, nucleosides analogues (ribavirin, tiazofurin, pyrazofurin) had no effect. Two compounds had a slight effect not justifying to consider them as possible therapeutic agents: selenazofurin and an analogue of ribavirin (RTA). Eight heteropolyanions (HPA), which have a related chemical structure, were efficient providing 100% protection. Nineteen compounds were injected into rabies infected mice by the intracerebral (i.c.) route. Fourteen compounds such as ribavirin, RTA, selenazofurin, tiazofurin and 9 HPA compounds had no effect. Five other HPA compounds (HPA 23-39-46-51-56) were efficient preventing the development of clinical infection in some mice. Whatever was the treatment route, treated surviving mice developed rabies neutralizing antibodies. No proof of viral multiplication was found in their brains. As some HPA compounds did produce a therapeutic effect in mice, two of them HPA 23 and HPA 39 were administered to rabies-infected foxes. In foxes the compounds prolonged the mean survival time and increased the number of survivors. These data suggest that chemotherapy might be worthwhile when vaccination was impossible.

Animals↗
PubMed1987

Effects of TMB-8, a calcium antagonist, on transport properties of the isolated canine tracheal epithelium.

The effects of the putative intracellular Ca2+ antagonist, TMB-8 (8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate), on the canine tracheal epithelium were examined. Luminal addition reduced rapidly, but reversibly, the transmucosal potential difference and increased the resistance across the open-circuited epithelium. Under short-circuit conditions, the drug reduced stimulation by prostaglandin E2, forskolin, 8-bromo cyclic AMP, prostaglandin F2 alpha and A23187. Inhibition of prostaglandin E2 responses were accompanied by reversal of net Cl- fluxes produced by the agonist. The effects of TMB-8 were unaffected by increasing Ca2+ in the bathing solutions, and were not mimicked by procaine, nitrendipine, calmidazolium, compound 48/80 or trifluoperazine. W7 did, to a limited extent, produce similar responses, though the drug was more toxic, and the effects were irreversible.

1-Methyl-3-isobutylxanthine↗
PubMed1992

The effect of cocaine on sperm motility characteristics and bovine cervical mucus penetration.

OBJECTIVES: To determine the in vitro effects of cocaine on sperm motility and bovine mucus penetration because cocaine abuse is associated with decreased sperm motility, and related compounds, such as procaine, are known to decrease sperm motility. DESIGN: Human semen samples were exposed to a range of cocaine concentrations and the effects quantified using computer-assisted sperm analysis and the bovine mucus penetration test. SETTING: University research laboratory. PATIENTS, PARTICIPANTS: Samples were obtained from 18 healthy volunteers. INTERVENTIONS: Normal semen samples were exposed to concentrations of cocaine ranging from 10(-11) to 10(-4) M. Motility characteristics were evaluated after 2 hours, and bovine mucus penetration was evaluated after 30 minutes, 1 hour, and 2 hours. Mucus penetration by washed sperm was also evaluated. MAIN OUTCOME MEASURES: Motility characteristics were evaluated using computer-assisted sperm analysis, and functional sperm motility was evaluated using the bovine mucus penetration test. RESULTS: Cocaine exposure decreased the percentage of motile sperm in a concentration-dependent manner with a maximum decrease of 23% at 10(-4) M but had no effect on other motility characteristics. Cocaine decreased bovine mucus penetration by 12% at high cocaine concentrations (10(-4) M), but increased penetration by 69% at low concentrations (10(-9) M). Washing sperm before cocaine exposure attenuated the increased sperm penetration. CONCLUSION: The ability of cocaine to decrease the percentage of motile sperm at high concentrations may explain the decreased sperm motility associated with cocaine use. Cocaine's ability to augment sperm penetration at low concentrations suggests an interaction of cocaine with the sperm adrenergic system.

Analysis of Variance↗
PubMed2003

Pharmacological and toxicological aspects of combination of beta-lactam and aminoglycoside antibiotic, prednisolone and procaine hydrochloride on the example of Vetramycin.

Vetramycin is an injectable veterinary compound for animal use only. In veterinary medicine, it has been used for a long time as a bactericidal beta-lactam and aminglycoside antibiotics combination, extending the bactericidal spectrum of these substances. This compound, in addition to bactericidal procaine penicillin and dihydrostreptomycin (DHS), contains also prednisolone acetate and procaine hydrochloride, two biologically active substances. Prednisolone, a glucocorticoide, has an antiinflammatory, antiallergic, antiitchical and analgesic effect. Procaine hydrochloride, in turn, has a local anaesthetic effect and attenuates pain caused by irritable properties of antibiotics at the injection sites. The average dosage of, respectively, procaine benzylpenicillin (I.U./kg(-1) b.w.), DHS (microg/kg(-1) b.w.), prednisolone acetate (microg/kg(-1) b.w.) and procaine hydrochloride (mg/kg(-1) b.w.) in horses, cattle, pigs is 6000-15000, 10-11, 0.24-0.6 and 1.2-3.0; s.i.d., in sheep, foals, calves, piglets is 20000-40000, 10, 0.8-1.6 and 4-8; s.i.d., in dogs and cats is 30000-200000, 10, 0.8-1.6 and 4-8; s.i.d.. Intramammary injection dose (Vetramycin antimastitis ointment in syringe) in cows is 1000000 I.U. of procaine benzylpenicillin + 1000000 I.U. of dihydrostreptycin sulphate per quarter of udder, s.i.d., during 3 successive days.

Aminoglycosides↗