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[Kinetics of the proteolytic activity of intact human spermatozoa].

Seminal plasma free intact human washed spermatozoa have hydrolytic activity on N-benzoil-D-L-arginine-naftilamide (BANA). Kinetic activities of this enzymatic activity are similar to those described for acrosine. Therefore, it is likely that it would be the same enzyme. BANA- hydrolytic activity might be liberated to the medium by incubation of pH lower than 4.0 and reincorporates to the membrane after adjustment of the medium to alkaline pH. pH- dependant enzyme liberation curve is similar to titration curve of sialic acid attached to the membrane. Attachment of the enzyme to the spermatic membrane diminishes its specific activity. However, if spermatozoa are previously treated with neuraminidase, its membrane afinity is inhibited. It is thought that this enzyme in the spermatozoon is present as protein ionically bound to the membrane and that sialic acid participates in this union. It is postulated that drastic treatments such as the use of ultrasound or detergents produce redistribution of specific proteins.

2-Naphthylamine↗

[Hypotensive and antihypertensive activity of a newly synthesized derivative of 2-aminotetralin].

The report describes the hypotensive and antihypertensive activity of the compound N-(trans-3-hydroxy-1,2,3,4-tetrahydro-2-naphtyl)-N'-(3-oxo-3-phenylpropyl) piperazine dihydrochloride (P11). The work is made on normotensive cats and rats as well as on spontaneous and experimental (metacorticoid) hypertension. The studies were carried out under the conditions of acute and chronic experiment as the arteria pressure was recorded by blood and bloodless method. The compound P11 show a manifested hypotensive activity with favourable duration and therapeutic width. Its antihypertensive activity is revealed in rats with spontaneous and metacorticoid hypertension both after single and chronic applciation of the compound. The influence on the blood pressure weakens after reserpinization of the animals. The compound possesses slight ganglion-blocking action and manifested alpha and beta adreno-blocking activity: diminishes noradrenaline, adrenaline and isoprenaline responses on the arterial pressure and heart activity in anesthetised cats and rats, shifts to the right the cumulative dose-response curve of noradrenaline on vas deferens of a rat, ect. The hypotensive and antihypertensive effect of the compound P11 is discussed on the basis of its alpha and beta adrenoblocking action and its specific sedative effect.

2-Naphthylamine↗

The identification and control of occupational bladder cancer.

The recognition of an increasing number of environmental and occupational factors imvolved in cancer etiology indicates the urgent need for more effective identification and control procedures. On the evidence of experience derived from the historical example of occupational bladder cancer, it is suggested that the problems of identification and control require an integrated approach which must involve the toxicity screening of industrial materials, the environmental screening of the industrial process and the epidemiological screening of those who work in industry. Such a programme will depend for its success upon the cooperation and understanding of all concerned, and the need for consultation and the full provision of information is stressed. Benefits are indicated which might ultimately accrue from the establishment of a computerized data bank in which the results of toxicological, epidemiological and carcinogenicity investigations have been accumulated and collated under the auspices of an international agency.

2-Naphthylamine↗

[Antihistamine and antiserotonin action of 2 aminotetralin derivatives].

The authors performs studies under the conditions of whole organism in vivo and on isolatid organs in vitro and examined antihistamine and antiserotonine activity of two derivatives of 2-aminotetraline, synthesized by D. Dancev and Iv. Ivanov, namely: N-(trans-e-hydroxy-1, 2, 3, 4-tetrahydro-2-naphtyl (-N-) 3-oxo-3-phenylpropyl) piperasine dichloride and N-(trans-3-hydroxy-1, 2, 3, 4-tetrahydro-2-naphtyl (-N-) 3-oxo-3-3phenyl-2-methylpropyl (piperasine dichloride) indicated respectively as P10 and P11. The experiments on isolated ileum of a guinea pig showed that the compound P11 (in concentration of 1.10(-7), 1.10(-6), and 1.10(-5) gm/ml) and P11 (in concentration of 1.10(-6) and 1.10(-5) gm/ml) inhibited the spasomogenic effect of histamine (1.10(-8) and 1.10(-7) gm/ml) as better antihistaminev effect revealed P10. Both compounds inconcentrations of 1.10(-6) and 1.10(-5) gm/ml inhibited the spasmogenic effect of serotonine (1.10(-7) gm/ml), as more significant changes occurred under the influence of the compound P11. The compound P10, administered subcutaneously in a guinea pig in a dose of 0.5 mg/kg of body weight 30 minutes before the occurrence of histamine shock, prevented its development. The same compound inhibited also the development of enterocolitis in mice, induced by serotonine (in a dose of 1 mg/kg of body weight). Both examined compounds inhibited the development of serotonine oedema of the hind paw of a rat as better effect showed the compound P11. The established facts are discussed.

2-Naphthylamine↗

On the antiarrhythmic activity of one N-substituted piperazine derivative of trans-2-amino-3-hydroxy-1, 2, 3, 4-tetrahydroanaphthalene.

The antiarrhythmic activity of the compound N-(trans-3-hydroxy-1,2,3,4-tetrahydro-2-naphthyl)-N-(3-oxo-3-phenyl-2-methylpropyl)-piperazine hydrochloride, referred to as P11, is studied on anaesthesized cats and Wistar albino rats, as well as on non-anaesthesized rabbits. Four types of experimental arrhythmia are used--with BaCl2, with chloroform-adrenaline, with strophantine G and with aconitine. The compound P11 is introduced in doses of 0.25 and 0.50 mg/kg intravenously and 10 mg/kg orally. The compound manifests antiarrhythmic activity in all models of experimental arrhythmia used, causing greatest inhibition on the arrhythmia induced by chloroform-adrenaline (in 90 per cent) and with BaCl2 (in 84 per cent). The results obtained are associated with the beta-adrenoblocking and with the membrane-stabilizing action of the compound.

2-Naphthylamine↗

Gas-liquid chromatographic-mass spectrometric determination of alpha- and beta-naphthylamines in FD&C Red No. 2 (amaranth).

A method is described for the simultaneous quantitation of trace amounts of alpha- (alpha-NA) and beta-naphthylamines (beta-NA) with detectability in the 0.1 ppb range and sensitivity of 50 picomoles in certified food grade amaranth (FD&C Red No. 2; C.I. Food Red 9; CI 16185). The amaranth sample is extracted with benzene, and the evoporated residue is derivatized with perfluorooctanoic anhydride. The resulting derivatives are separated by gas-liquid chromatography and identified and quantitated by mass spectrometric monitoring of the m/e at 539.04. The method was used for quantitation of alpha-NA and beta-NA in randomly chosen samples of amaranth. Of 11 samples from different manufacturers, 5 were free of the beta-isomer; the remaining samples contained up to 1.2 ppb beta-NA. The concentration of alpha-NA ranged from no detectable amount to 970 ppb; the majority of the samples contained less than 7 ppb.

1-Naphthylamine↗

Differentiation of strains of Staphylococcus epidermidis biotypes 1 and 4 by aminopeptidase profiles.

Seven different strains of Staphylococcus epidermidis and one strain of S. aureus were catagorized by their aminopeptidase activity. Eight different profiles were obtained: five profiles for S. epidermidis biotype 4 (each representing a different known serotype), two profiles for S. epidermidis biotype 1 (one for each strain used) and one for the strain of S. aureus used. Despite some similarities, distinct patterns of the hydrolysis of 22 different amino acid-beta-naphthylamides were evident for each individual strain. The evaluation of aminopeptidase profiles provides another means for distinguishing between strains of the same species and can, therefore, be used advantageously and in combination with serotyping as an epidemiological tool.

2-Naphthylamine↗

Causative agents in the induction of bladder cancer.

A survey of many of the known or suspected causative agents in the etiology of bladder cancer is presented. In several instances, a comparison of the epidemiological evidence and the results of animal bioassays is made. Difficulties in the interpretation of animal studies and the extrapolation of animal data to estimate human risk is discussed. Each class of chemicals, such as the aromatic aminatic amines or the non-nutritive sweetners, presents its unique problems when attempts are made to evaluate its potential as a causative agent in the etiology of bladder cancer.

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