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At least 145 records · Page 8Linked to original sources
PubMed2002

Characterization and comparative evaluation of a novel PAI-1 inhibitor.

Plasminogen activator inhibitor-1 (PAI-1), the primary physiological inhibitor of both tissue-type plasminogen activator and urokinase-type plasminogen activator in plasma, is a well established risk factor in thrombotic diseases. Reduction of active PAI-1 levels may lead to a decreased tendency of thrombosis. Compounds that can suppress pharmacologically active PAI-1 levels are therefore considered as putative drugs. In the present study, we describe the PAI-1 neutralizing properties and mechanism of a newly selected compound (i.e. fendosal, HP129) in comparison to four previously reported compounds (i. e. AR-H029953XX, XR1853, XR5118 and the peptide TVASS) using different assays. The inhibitory effect of these compounds on active PAl-1 was analyzed by a plasmin-coupled chromogenic assay (Coaset t-PA), direct chromogenic assays (t-PA, u-PA) and quantification of complex formation by ELISA, SDS-PAGE and surface plasmon resonance. Comparative evaluation of the obtained IC50 values reveals large differences [i.e. IC50 of 15 microM (HP129) vs. >1000 microM (XR5118) determined at 37 degrees C using SDS-PAGE] between the compounds studied. Importantly, the relative potency of the various compounds is also dependent on the method used (10 to 170-fold differences in IC50 values). Characterization of the PAI-1 forms (i.e. active, non-reactive and substrate) generated upon inactivation reveals that the newly described compound HP129 induces a unique pathway (i.e. active to non-reactive conversion via a substrate-behaving intermediate) of inactivation compared to the other compounds. Taken together, these data strongly suggest that the various compounds act through different mechanisms. In addition, the results stress the necessity for a careful selection of the method used for the evaluation of PAI-1 inhibitors, preferably requiring a panel of screening methods.

Anticoagulants↗
PubMed1999

[Rapid method for determination of chlordimeform residue in honey].

In the present work. TLC was used as a rapid method for determination of chlordimeform in honey. Twenty gram of sample was extracted by n-hexane in alkali solution, re-extracted by acidic aqueous solution, then hydrolyzed in NaOH solution for 10 min on boiling water bath. The hydrolyzed products were extracted by methylene chloride. After passing through the Na2SO4 column for dehydration, the methylene chloride should be evaporated to less than 70 degrees C to 0.5 mL spot 50 microL sample solution on the silica gel plate, develop the plate about 8 cm from the surface of developing solvent V(benzene):V(chloroform):V(ethyl acetate) = 5:5:1. The plate was kept in the atmosphere (NaNO2 + HCl) for 10 min and 5% N-(1-naphthyl) ethylendiamine dihydrochloride was sprayed on it. Put it into a dark room for 20 min and then observe and estimate the amount of chlordimeform in the sample. The limit of determination is 10 ng. The experiment could be completed in 3 h for a sample without large equipment and special reagent.

Chlorphenamidine↗
PubMedDate not supplied

[The results of laboratory and field trials of the action of ektomin on the taiga tick].

Laboratory and field trials of 60% concentrated ectomin emulsion have been conducted. Laboratory experiments on the contact of hungry female individuals of Ixodes persulcatus (Acarina, Ixodidae) with pesticide in the envelopes made of impregnated filter paper have established high imago sensitivity to the preparation--LD50 after a 4-hour contact was 1.10(-6) micrograms/cm2. In field experiments ectomin ensured a 100% effect of hungry Ixodes persulcatus elimination 1-2 days later, with the preparation expenditure no more than 0.05 kg/hectare. The effect was retained throughout one whole season of I. persulcatus activity.

Animals↗
PubMed1990

[The effect of pesticides-CDM and AMZ on inhibition of the binding of 3H-clonidine to alpha 2-adrenoreceptor in rat forebrain tissue].

Chlordimeform (CDM) and Amitraz (AMZ) are two formamidine pesticides. CDM and AMZ inhibited the binding of 3H-Clonidine, 3H-Yohimbine to Alpha 2-adrenoreceptor of rat forebrain tissue in vitro with IC50 values of 62-68 mumol/L (CDM) and 95-110 mumol/L (AMZ). In vivo the administration of CDM and AMZ by ip showed the effect of inhibition on the binding and significant correlation of dose-effect r = 0.995 (CDM), 0.884 (AMZ). Time course test indicated that the lasting inhibition effect of CDM following exposure was shorter than AMZ. Similar results were observed with plasma in vitro. Comparing inhibition effects on rat forebrain tissue, directly induced by CDM and AMZ at different doses, with the results from the plasma of treated rats in vitro, there was a significant correlation r = 0.973 (CDM), 0.909 (AMZ). It showed that the inhibition effect of both CDM and AMZ was linked to the concentration of compounds chemical and their metabolites in blood. Time course and washing test indicated that the inhibition effect by CDM and AMZ was reversible.

Amidines↗
PubMed1987

Assessment of potential acute health effects in agricultural workers exposed during the application of chlordimeform.

Agricultural workers exposed to chlordimeform (Cdf) used as a pesticide on cotton in Imperial County, California, were monitored during the 1982 application season. Cdf metabolites were found in the urine of 132 workers and were positively correlated with the length of exposure and nature of job activity. Persons mixing and loading and engaged in miscellaneous tasks such as cleaning and maintenance of equipment had the greatest exposure. There was no evidence of urinary tract irritation by microscopic analysis of the urine, nor were significant differences found between preseason and postseason serum chemistry results. Despite the use of protective clothing and closed system transfer devices, Cdf was absorbed by workers as evidenced by urinary metabolite excretion.

Agricultural Workers' Diseases↗
PubMedDate not supplied

Acute and sub-acute effects of deltamethrin and chlordimeform on schedule-controlled responding in the mouse.

The effects of deltamethrin (0.03-3 mg/kg) and chlordimeform (0.3-56 mg/kg) were examined on schedule-controlled responding in the mouse. The response (interruption of a photocell beam) was maintained under a fixed-interval (FI) 60-sec schedule of milk delivery. Acute doses of deltamethrin larger than 0.1 mg/kg decreased responding in a dose-related manner. The ED50 was approximately 1 mg/kg; 3 mg/kg abolished responding. Repeated administration of 3 mg/kg (once daily for 10 days) did not result in a change in the rate-decreasing effects of that dose; however, daily (pre-injection) control response rates decreased about 50%. When dosing was discontinued, rates of responding failed to completely return to pre-drug control levels. Acute doses of chlordimeform larger than 10 mg/kg decreased responding in all mice, but in mice not previously receiving drugs lower doses had a greater rate-decreasing effect. The ED50 was between 10-30 mg/kg; 56 mg/kg abolished responding. Repeated administration of 3 and 10 mg/kg had little effect. Repeated administration of 30 and 56 mg/kg abolished daily (pre-injection) control performances completely after 5-6 days. Responding gradually returned to control levels after dosing was discontinued. The behavioral toxicity of both chlordimeform and deltamethrin was augmented by repeated administration.

Amidines↗
PubMed1977

[Monoamine oxidase activity of the brain of Locusta migratoria in normal conditions and after intoxication by two insecticides: chlordimeform and dieldrin].

Our investigations have shown up an MAO activity in locust brain, by the use of a radio-isotopic method, as much at larval as at adult stage. This MAO activity is in a sample of 34,3 dpm/mg of brain tissue (wet weight). Investigations have also been undertaken on effects of dieldrin and chlordimeform poisoning on this MAO activity. Even at sublethal dosages, chlordimeform causes a significant inhibition of MAO activity in vivo. This finding is in accordance with Beeman and Matsumura's work in vitro. Moreover, acute poisoning by dieldrin produces more than 60% of inhibition of MAO, 3 hours after administration of 115 microng of this insecticide by injection in the hoemocelian cavity.

Amidines↗
PubMed1979

The influence of chlordimeform on calcium and glucose homeostasis.

The effects of single and repeated administration of chlordimeform on calcium and glucose homeostasis were examined in the rat. A single injection of chlordimeform (100 mg/kg, i.p.) produced a rapid 15 percent decrease in plasma calcium and a 64 percent rise in plasma glucose. The administration of chlordimeform (75 mg/kg, i.p., twice daily) over a period of 7 days caused an 8 percent reduction in plasma calcium, a 50 percent decrease in duodenal calcium transport and a 20 percent decrease in body weight.

Amidines↗