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M L Indenbom

Publications and source records attributed to M L Indenbom.

10 recordsLinked to original sources
PubMedDate not supplied

[Cholinomimetic activity of acetylcholine and sebacinyldicholine derivatives with differing cationic group structures].

The intrinsic alpha activities and the D2 (frog, m, rectus abdominalis) concentrations were estimated for different acetylcholine and sebacinylcholine derivatives. So were also the A2 values for antagonists and the affinity constants Kc for some partial agonists. The results obtained disprove Paton's "rate-theory". The relationship between the cholinergic activity and the volume of cationic groups was studied and it could not possibly be explained by the steric hindrance alone. It is suggested that certain hydrophobic radicals of the cationic groups contact the receptor surface outside the anionic centre. Such contacts prevent the cholinoreceptor to change its conformation and thus inhibit the depolarization of the membrane. An approximate estimation of the anionic site dimensions is given.

Abdominal Muscles↗
PubMedDate not supplied

[Decurarization using the cation-anion molecular interaction of a myorelaxant and its antagonist].

In experiments on the cat neuromuscular preparation the authors investigated the anticurare action of the new compound IEM-931 having sulphonate-anionic groups 20 A apart. The new compound administered in a dose of 184 mkM/kg prevents and removes the curare effect of rythetronium which is its structural analogue. Regarding tubocurarine the antagonism is displayed, however, only from the dose of 384 mkM/kg. This indicates that efficacy of the anticurare action of IEM-931 is directly related to complimentarity of the interacting molecule structure. The experiment with regional relaxation of the cat muscles shows that the anticurare action of IEM-931 is realized both in the blood and on the cholinoreceptor. Moreover, as a result of molecular interaction the inactive complex is formed.

Animals↗
PubMedDate not supplied

[Selective action on hypophyseal gonadotropic function of a new compound from the group of aromatic series sulfur derivatives].

Chronic experiments set up on rats showed the new original drug izm-931, a sulphoderivative of the aromatic series with a rigid molecular structure, to produce, depending upon its dose and reactivity of the hypothalamus-hypophysogonads, regulation system both stimulating and inhibiting gonadotropic effect. At the same time the drug produces neither peripheral nor estrogenic and antiestogenic action on the uterus and vaginal epithelium. The drug resembles but has a number of advantages over and differences with an earlier synthetized by the authors drug sigetin, whose pharmacological properties are close to the one under consideration. The synthesis and study of compounds of this kind are aimed at the search for new effective medicinal agents with an elective type of action on the gonadotropic function of the hypophysis which are of interest for the obstetric and gynecological practice. The present investigation is a new step towards solving this urgent problem of pharmacology in dealing with neuroendocrine regulation of the reproductive function.

Animals↗