Quinacrine

Quinacrine. Quinacrine (7), C23H2QCIN2O, is an acridine derivative. It is used in the form of the dihydrochloride dihydrate,... 

This dmg was used prior to the availabiUty of niclosamide and is considered less satisfactory for the treatment of tapeworms than niclosamide (24). It causes more side effects and produces severe nausea. Quinacrine, however, is preferred by some clinicians for the treatment of Taenia solium infection because, unlike niclosamide, it expels the worms intact, thus reducing the theoretical risk of cysticercosis (25). 

Quinacrine concentrates in the scolex of the parasite and causes the muscles needed for holding onto the intestinal wall to relax. The worms are stained yellow and pass from the body, still aUve. Quinacrine can intercalate with DNA and inhibit nucleic acid synthesis. It creates fluorescent bands in deoxyadenylate—deoxythmidylate-rich regions of DNA and has been used as a stain in the study of human genetics. 

The dmg is readily absorbed from the gastrointestinal tract and may persist in human tissues for two months after adrninistration. Quinacrine is given as a single dose for the treatment of tapeworms it is manufactured by Winthrop-Breon of New York, New York. 

Quinacrine (49) is an acridine that was used extensively from the mid-1920s to the end of World War 11. It acts much like chloroquine and is reasonably effective. Because it causes the skin to turn yellow and, in high doses, causes yellow vision, the dmg is no longer in use as an antimalarial. Pyronaridine (77), a 1-azaacridine developed in China, appears to be effective against mefloquine-resistant, but not entirely against chloroquine-resistant, strains of P falciparum. 

Quaternary ammonium compounds biocidal activity mechanism, 1, 401 toxicity, 1, 124 Quaternization heterocyclic compounds reviews, 1, 73 ( )-Quebrach amine synthesis, 1, 490 Queen substance synthesis, 1, 439 4, 777 Quercetin occurrence, 3, 878 pentamethyl ether photolysis, 3, 696 photooxidation, 3, 695 Quercetrin hydrolysis, 3, 878 Quinacetol sulfate as fungicide, 2, 514 Quinacridone, 2,9-dimethyl-, 1, 336 Quinacridone pigments, 1, 335-336 Quinacrine... 

The packaging of nucleoproteins within chromatids is not random, as evidenced by the characteristic patterns observed when chromosomes are stained with specific dyes such as quinacrine or Giemsa s stain (Figure 36-6). 

FIG. 7 The quinacrine-dependent changes in cyclic voltammograms of the DNA-immobilized An electrode. Experimental conditions are the same as those in Fig. 5. 

Figure 9 summarizes the electrode responses toward a variety of DNA-binding substrates [14c]. For intercalators (quinacrine, acridine orange, and safranin) and groove binders (spermine and spermidine), a steep rise followed by a saturation of the concentration response curve is commonly observed. If one compares the specific concentration which gives a 50% response in the increment of the cathodic peak current (A/p ) for each substrate, a selectivity order of quinacrine acridine orange > spermine > spermidine > safranin can be estimated. The binding constants measured in aqueous media for the affinity reaction with ds DNA are as follows quinacrine, 1.5 x 10 (38 mM NaCl)... 

Quinacrine 100 mg three times in adults or 5 mg/kg per day in pediatric patients for 5 to 7 days, is available from a specialized pharmacy (e.g., Ponorama Compounding Pharmacy).3... 

Acridine dyes such as the antimalarial agent quinacrine (Atabrine) shown next are large planar aromatic compounds that intercalate or sandwich themselves between the stacked bases of the helix. 

On replication, insertion or deletion of bases may occur. Chain scission and chromosome breaks are also possible. Quinacrine is useful in human cytogenetics, since it intercalates significantly into the heterochromatin of the Y chromosome, making it fluoresce and rendering it identifiable cytologically. Detection of the Y chromosome is important in prenatal sex determination. Other dyes present in our environment are potentially mutagenic. For example, some hair dyes were shown to be mutagenic for E. coli. 

In some cases, a given drug may be highly bound to proteins. In such cases, the Vi is very high. The drug quinacrine has a Vd of 50,000 L where as the Vd of tolbutamide is less than 10 L. 

Primaquine phosphate [63-45-6] (148)/ Quinacrine hydrochloride hydrate 2942C I(2)864B, N(2)741A VA9660000, USP... 

Quinacrine hydrochloride hydrate [6151-30-0]/ 3020C I(2)877A, N(2)751D AR7875000, USP... 

The FPA experiment can also be performed by exciting into the S2band of ethidium using 315-nm radiation and detecting at 630 nm (J. H. Shibata, J. C. Thomas, and J. M. Schurr, unpublished results). Substantial cancellation of the two main relaxing terms (n = 1, 2) in r(t) considerably diminishes the statistical accuracy of the best-fit a., but nevertheless it remains the same as found for excitation into S, which provides a reassuring check. Using intercalated quinacrine as the probe dye, Fan et al. recently obtained a... 

A related observation is that fully relaxed supercoiled DNA/dye complexes are somehow different from nicked circular DNA/dye complexes in the presence of the same concentration of free dye, where the binding ratios should be the same. This is readily seen in gel electrophoresis in the presence of sufficient dye concentration so that at least one, but not all, of the topoisomers is positively supercoiled. The slowest moving, presumably fully relaxed, topoisomer migrates significantly faster than the nicked circle, and this difference increases with the amount of dye present. This is not observed with chloroquine, perhaps because the effect is too small. However, it is readily apparent in the original gels of Keller0 61) in which ethidium was used to unwind the topoisomers. We have confirmed this effect for ethidium and have observed similar behavior for proflavine, 9-aminoacridine, and quinacrine. 

Griinhagen HH, Iwatsubo M, Changeux JP. 1977. Fast kinetic studies on the interaction of cholinergic agonists with the membrane-bound acetylcholine receptor from Torpedo marmorata as revealed by quinacrine fluorescence. Fur J Biochem 80 225-242. 

Rowley JD. Tetter A new consistent chromosomal abnormality in chronic myelogenous leukaemia identified by quinacrine fluorescence and Giemsa staining. Nature 1973 243 290-293. 

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