Interaction of selected pregna-D'-pentaranes with cytosolic receptors of myometrium and endometrium in various disease states

The relative capacities of several pregna-D'-pentaranes to combine with cytosolic receptors of the myometrium and endometrium in various disease states are investigated, and one of the compounds, 6α-methyl-16α, 17α-cyclohexanoprogesterone, is identified as holding particular promise for clinical use in replacement therapy and as a contraceptive agent. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 119, N ^o 2, pp. 163–165, February, 1995     

Sex steroids and their receptors in patients with tumors of the pancreas

A tendency toward an increase in serum content of sex steroid-binding globulin and a decrease in the total concentration of testosterone and its free and globulin-bound fractions and in the index of free androgens was observed in patients with pancreatic cancer. There were no statistically significant differences in baseline serum levels of hypophyseal hormones and prolactin in male patients and in the control. One or both types of steroid hormone receptors, the content of androgen receptors being higher than that of estrogen receptors, varying in a wide range were detected in 71% of the patients with malignant neoplasms. The occurrence of steroid hormone receptors was higher in adenocarcinomas, while their content was significantly higher in normal pancreatic tissues. The occurrence of androgen receptors was higher in male patients at the early stages of the disease, predominantly in highly differentiated adenocarcinomas located in the body of the pancreas. The content of androgen receptors was higher in male patients, in metastasizing tumors, in adenocarcinomas located in the body of the pancreas, and in patients without clinical and laboratory evidence of the mechanical jaundice syndrome. The content of androgen receptors positively correlated with the maximum size of the tumor. Translated fromByulleten' Eksperimental'noi Biologii, I Meditsiny, Vol. 126, No. 8, pp. 197–200, August, 1998     

Comparative analysis of progesterone and estradiol reception in human myoma

Cytosolic and plasma membrane receptors for progesterone and estradiol are studied in myomatous nodes (MN) and in histologically unaltered myometrium (HUM) against the background of myoma. The level of cytosolic receptors for both hormones is higher in the myoma cells than in the essentially healthy myometrium. In the plasma membranes the progresterone reception is reduced and the estradiol reception is unchanged compared with HUM. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 118, N ^o 7, pp. 33–34, July, 1994     

Relative binding capacity of pentarane substances with plasma membrane receptors of uterine cells of oophorectomized rats

The relative capacity of substances of the pentarane group for binding with progesterone receptors of the plasma membranes of uterine cells of oophorectomized rats is studied. Introduction of an extra carbocycle D' in the progesterone molecule at the 16α and 17α sites and further modification of the molecule cause an increase of the relative binding capacity of these compounds. Analysis of the findings identifies substance III, showing the highest activity toward all the discussed parameters and a promising candidate for further preclinical studies. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol., 118, N ^o 7, pp. 31–32, July, 1994     

Immunohistochemical identification of androgen receptors in the liver of pubertal male rats

Androgen receptors in the liver of pubertal male rats are identified by an indirect immunoperoxidase method. Hepatocyte nuclei predominate among positively stained structures. The intensity of staining varies from hepatocyte to hepatocyte and does not depend on its position in the liver lobule. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 122, No. 8, pp. 193–196, August, 1996     

Autostimulation of prolactin receptors in adrenal cortex of guinea pigs

Prolactin injected to male guinea pigs for 7 days considerably enhanced binding of¹²⁵I-prolactin by adrenal cortex microsomes. Scatchard analysis showed that this rise is due to an increase in the receptor binding capacity but not in their affinity. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 123, No. 5, pp. 548–550, May, 1997     

Effect of immune “sessile” receptors on the choline receptors of the lymphocyte membrane in mice immunized with certain antigens

Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 115, N ^o 2, pp. 384–386, April, 1993     

Central opioid receptors in the pathogenesis of adrenal arrhythmias

The effect of intraventricular administration of opioid peptides on the frequency and severity of ventricular arrhythmias is studied after intravenous injection of epinephrine. It is found that the selective μ-agonist DAGO and the nonselective σ-agonist DADLE decrease the frequency and severity of arrhythmias. On the other hand, the selective σ-agonist DSLET and the κ-agonist dinorphine A 1–13 potentiate adrenal arrhythmias. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 118, N ^o 9, pp. 241–243, September, 1994 Presented by R. S. Karpov, Member of the Russian Academy of Medical Sciences     

Androgen receptors in the cytosolic fraction of malignant prostatic tumors and their clinical significance

The occurrence and mean content of androgen receptors in the cytosolic fraction of prostatic adenocarcinoma depend on the age of patients, stage of tumor anaplasia, tumor differentiation, type of therapy, and the concentration of androgen receptors. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 122, No. 10, pp. 432–436, October, 1996     

Involvement of central and peripheral cannabionoid receptors in the regulation of heart resistance to arrhythmogenic effects of epinephrine

Intravenous injection of the selective cannabinoid receptor agonist HU-210 in doses of 0.05 and 0.25 mg/kg increased heart resistance to arrhythmogenic effects of epinephrine, while intracerebroventricular infusion of this substance had no effect on the incidence of epinephrine-induced arrhythmia. The selective antagonist of type I cannabinoid receptors SR141716A in a dose of 3 mg/kg and ganglion blocker hexamethonium in a dose of 10 mg/kg did not modify the antiarrhythmic effect of HU-210. This effect of HU-210 is probably related to activation of type II peripheral cannabinoid receptors. Translated fromByulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 130, No. 11, pp. 552–554, November, 2000     

Characterization of benzodiazepine receptors of human lymphocytes

It is demonstrated that benzodiazepine binding sites on human peripheral blood lymphocytes are the peripheral type receptors. The binding sites for the selective agonist³H-Ro 5-4864, but not for the antagonist³H-PK 11195, are completely inactivated by freezing-thawing of lymphocytes. The binding of³H-Ro 5-4864 to intact lymphocytes is activated by GABA and (+)baclofen. It is shown that the selective ligands Ro 5-4864 and PK 11195 bind to different subtypes of benzodiazepine receptors on human peripheral blood lymphocytes. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 126, No. 10, pp. 405–408, October, 1998     

Typifying presynaptic M-cholinergic receptors in different structures of rat brain

Pre- and postsynaptic M-cholinergic receptors are typified by radioligand analysis with selective cholinoblockers by comparing ligand binding in homogeneous and synaptosomal fractions of different structures of rat brain. It is found that presynaptic receptors of the hemispheres belong to M₃ subtype and those of the brain stem are probably of M₄ subtype. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 122, No. 7, pp. 75–77, July, 1996     

Epidermal growth factor receptors in endometrial adenomatosis

The expression of the epidermal growth factor receptors (EGFR) and of progesterone and estrogen receptors (PR and ER, respectively) was studied in 31 women of a reproductive age with endometrial adenomatosis. The receptor phenotype EGFR+PR-ER-, indicating mainly local regulation of the proliferative processes, was detected in adenomatous endometrium three times more often than in normal endometrium. The metabolic endocrine disorders were less frequent in patients with endometrial adenomatosis with EGFR, but the disease ran a more severe course in these patients, which was proven by more numerous diagnostic scrapings performed within the same period. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 127, No. 1, pp. 45–49, January, 1999     

Role of intraosseous receptors in afferent and motor reaction modulation

Acute experiments on cats demonstrated facilitation effects of afferent reactions, and segmentary motor reactions during stimulation of sciatic nerves and inhibition of corticofugal motor reactions induced by electrical stimulation of ilium osteoreceptors. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 120, N ^o 7, pp. 40–41, July, 1995 Presented by N. A. Agadzhanyan, Member of the Russian Academy of Medical Sciences     

Dopaminergic mechanisms in the immunostimulating effect of μ-opioid receptors

Immunogenesis was appreciably stimulated in CBA mice injected the μ-opioid receptor agonist DAGO. This stimulation was prevented by transecting the pituitary peduncle. Immunoactivation induced by opioid peptide was due to interaction with the dopaminergic system, because the effect is canceled by preliminary haloperidol blocking of D₂-postsynaptic receptors. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 121, No. 4, pp. 373–375, April, 1996 Presented by V. A. Trufakin, Member of the Russian Academy of Medical Sciences     

Role of estrogens in the regulation of prolactin receptors in liver cells of female rats

Strong expression of prolactin receptors in sinusoidal domains and cytoplasmic granules of hepatocytes, which is independent of cell location in the hepatic lobule and is positively regulated by estrogens, is revealed in pubertal female rats. In estrogen-treated animals, Prolactin receptors are also exposed in the perinuclear space of some hepatocytes surrounding the central veins. Estrogens regulate the intensity of prolactin receptors expression in hepatocytes, but not the number of cells containing these receptors. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 118, N ^o 9, pp. 264–267, September, 1994 Presented by I. P. Ashmarin, Member of the Russian Academy of Medical Sciences     

Estradiol-17β receptors in cytosolic fraction of chondrosarcoma

Estradiol-17β receptors were detected in the cytosolic fraction of the majority of bone chondrosarcomas by protamine sulfate sedimentation of the hormone-receptor complex. The absolute number of receptors in tumors was higher in men than in women, but chondrosarcomas with estradiol-17β receptors more often occurred in women. The highest level of receptors was revealed in highly differentiated chondrosarcomas. No relationships between tumor location, size, type of the process, and the number of receptors was detected. We can state with assurance that the absence of estradiol-17β receptors in chondrosarcomas in women is a favorable prognostic sign with regard to metastases or local tumor relapses. Translated fromByulleten' Eksperimental'noi Biologii i Meditsiny, Vol. 129, No. 2, pp. 201–203, February, 2000