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Biomedical subjects

P Franke

Publications and source records attributed to P Franke.

At least 127 records · Page 7Linked to original sources

[Analysis and stability of propiverine hydrochloride (Mictonorm)].

In acid, neutral and alkaline solution the hydrolytic degradation of the spasmolytic agent Mictonorm (1) was determined. As degradation products ester- and/or ether fragments (2-5), benzophenone (6) and a compound X (7) were identified. In comparison N-Methylpiperidinyl(4)-benzilate (2) and benzilic acid (3) were also investigated in the isothermal quick-assay test. The test showed that the ether bound in 1 was hydrolyzed before the ester group. The compounds 5-7 are formed also direct from 3.

Benzilates↗

[In vitro and in vivo photochemical reactivity of methaqualone-1-oxide].

Methaqualone-1-oxide (1) exhibits photochemical reactivity. By irradiation of 1 with solar light the oxaziridin 3 is formed at first, which reacts in vitro (human proteins) and in vivo (rats) with macromolecules. As result of the photochemical in vitro and in vivo reactions of 1 the photoproduct 2-acetamidobenzoic acid-2'-methylanilide (6), involved in oxidation of protic compounds, was detected and after hydrolysis of proteins it appears that the short-lived 3 was adding to proteins.

Animals↗

[Biotransformation of alimemazine].

After application of alimemazine (1) 14 phenothiazine derivatives were detected in the rat urine. The structure of 9 metabolites was elucidated (TLC detection, UV, MS), which are hydroxy, N-dealkyl, S-oxide, and sulfone derivatives of 1. The hydroxy compounds, which are the main metabolites (greater than 50%), are partly conjugated. 5-10% of sulfones were observed. Some of the metabolites were detected in the feces, too. The relationship of the excretion products in urine and feces is 75:25%.

Animals↗

[Biotransformation of Chlorphenethazin (Elroquil, Marophen)].

After application of chlorophenethazine more than 20 metabolites were detected in rat urine. The structure of 14 metabolites were elucidated (UV, MS), which are hydroxy, N-dealkyl, S-oxide, sulfone and N-oxid derivatives. The hydroxy derivatives are partly conjugated. The relative high content of the sulfone of 2-chlorophenothiazine-N-acetic acid (upto 10% of the total metabolite content) is remarkable. Main metabolites are the S-oxide of the N-dealkyl derivative and 7-hydroxy-1.

Animals↗

[Photochemical reactivity of methaqualone-1-oxide].

The photoreactivity of methaqualone-1-oxide a main metabolite of the hypnotic methaqualone has been studied in polar and apolar solvents using UV- and daylight. Five photoproducts were isolated and identified by their analytical behaviour (TLC, UV, IR, high-resolution MS). The structure of the compounds 4, 6, 7, and 8 refer to unstable, reactive intermediates (oxaziridine, biradical) during the photolysis.

Chromatography, Thin Layer↗

[Incidence of psychiatric peculiarities in females with urinary incontinence].

Psychodiagnostic studies were conducted in 100 women with urinary incontinence. The VNPI test proposed by Regel and Schulze, a neurosis screening test, was adopted. Fifty-two of the patients studied revealed test results which were either pathological or called for further elucidation. Pathological VNPI findings were obtained in 23% of the women with stress incontinence, in 48% of those with combined incontinence, and in 85% of the patients with urgency incontinence. The present study suggests that psychodiagnosis is necessary beside comprehensive somatic urinary incontinence diagnosis.

Arousal↗

[Biotransformation and pharmacokinetics of (3,4-dichloroanilino)phenylacetonitrile (H 74)].

On studying the biotransformation of the potential spasmolysant (3,4-dichloroanilino)phenyl-acetonitrile (1; H 74), the authors isolated and identified (TLC, UV, high-resolution MS) from the urine and/or the faeces of male Wistar rats, apart from 1 (greater amounts only in the faeces because of incomplete oral absorption), 7 degradation products. In this connexion, the excretion of greater amounts of 3,4-dichloroaniline (2) and the detection of an accumulation of 2 in the serum in case of long-term treatment are above all disquieting from a toxicological point of view. According to extremely poor water solubility associated with high lipophilicity, the gastrointestinal absorption of 1 extends over a relatively long period of time, is incomplete and not proportional to the dose applied. Using a gas chromatographic technique, the authors found almost dose-proportional serum levels of (3,4-dichlorophenylimino)benzaldehyde (4) after oral application of 1, which is attributable to a first-pass effect (after intravenous application, below the limit of detection). 1 is subject to intensive distribution (marked alpha phase; high Vd) and its elimination is relatively slow (slow back flow from deep compartments; high reabsorption). In contrast to this, the elimination of 4 is considerably more rapid.

Acetonitriles↗

Carp insulin: amino acid sequence, biological activity and structural properties.

The amino acid sequence of insulin of carp (Cyprinus carpio) has been determined and correlated with its biological activity in a fat-cell test and its structural properties as measured by circular dichroism and sedimentation analysis. The amino acid sequence of carp insulin displays some unusual features: the B chain is longer at the N terminus by two residues as compared with mammalian insulins and there are substitutions of the charged residues, found in most insulins at positions B21 and B22, by proline and threonine respectively. On the other hand, all amino acid residues essential for biological activity and for the association of insulin monomers are the same in carp insulin. Accordingly, the half-maximal response in a fat-cell test is reached with carp insulin at concentrations which are only three times higher than with porcine insulin and the maximal response is the same. The circular dichroism spectrum of carp insulin resembles greatly that of bovine insulin indicating that it has a similar spatial structure. Despite amino acid substitutions in the dimer-dimer contact region, carp insulin is able to form hexamers.

Adipose Tissue↗

Investigation into the species-specific deacylation of penta-acetyl-gitoxin.

Penta-acetyl-gitoxin (PAG) shows species-specific deacylation to 16-acetyl-gitoxin (16 AG; I and III) or gitoxin (II and IV) by homogenates of liver and intestinal mucosa of man (I), rabbit (II), guinea-pig (III) and rat (IV), whereas it is degraded into tri- and tetra-acetates by homogenates of guinea-pig myocardium as well as by human blood and serum. The identity of the principal and chloroform-extractable metabolities in human urine after PAG administration with 16-AG has been demonstrated by mass spectrometry.

Acetyldigoxins↗

C55-Dolichol: occurrence in pig liver and preparation by hydrogenation of plant undecaprenol.

Apart from the long-chain dolichols (C80-C110), pig liver contains also a family of much shorter polyprenols with dominating C55-polyprenol. This compound was identified as cis/trans-dihydroundecaprenol in which the OH-terminal isoprene residue was saturated. The number of internal trans isoprene residues in this compound was three in comparison with two such residues in long-chain C95-dolichol. Chemical preparation of dihydroundecaprenol with a selectively saturated OH-terminal isoprene residue from fully unsaturated plant undecaprenol is presented.

Animals↗