ABSTRACT
The aim of the present paper was to study the effect of infrared laser radiation on endocrine regulation of immunogenesis and on endogenic opioid system. For this purpose experiments on rabbits were carried out. The animals underwent transcerebral radiation with subsequent induction of the primary immune response (PIR) to thymus-dependent antigen (sheep red blood cells). The PIR suppression was revealed in all test animals. It was more graphically expressed in rabbits exposed to impulse radiation. Immunodepression was combined with the increase of glucocorticoid activity of adrenal cortex, while no significant changes in thyroid hormones were registered. The 0.08 Joles impulse radiation cause a palpable fall in opioid concentration in blood plasma, the fact, which can be possibly accounted for the rapid exhaustion of opioid synthesis after their stimulation due to laser radiation.
Subject(s)
Endorphins/radiation effects , Hypothalamo-Hypophyseal System/radiation effects , Immunosuppression Therapy/methods , Lasers , Pituitary-Adrenal System/radiation effects , Animals , Antibody Formation/radiation effects , Brain , Glucocorticoids/metabolism , Infrared Rays , Male , Rabbits , SheepABSTRACT
The distribution of (+)-[3H]SKF 10,047 binding sites and the distribution of the established plasma membrane, nuclear, mitochondrial and endoplasmic reticulum markers in subcellular fractions of rat liver have been studied. The distribution profile of (+)-[3H]SKF 10,047 binding sites coincided with that of NADPH-cytochrome c reductase, the endoplasmic reticulum marker. (+)-[3H]SKF 10,047 binding sites in rat liver are therefore suggested to be located on the endoplasmic reticulum membrane and to represent a membrane-bound enzyme.
Subject(s)
Liver/chemistry , Phenazocine/analogs & derivatives , Receptors, Opioid/analysis , Animals , Binding Sites , Cell Membrane/chemistry , Cell Nucleus/chemistry , Endoplasmic Reticulum/chemistry , In Vitro Techniques , Liver/ultrastructure , Male , Mitochondria, Liver/chemistry , NADPH-Ferrihemoprotein Reductase/analysis , Phenazocine/metabolism , Rats , Rats, Inbred Strains , Receptors, sigmaABSTRACT
Effect of synthetic analogues of atrial natriuretic factor (ANF) on proliferative response and natural cytotoxic lymphocytes of human subjects was investigated in vitro. ANF-III and ANF-IV increased blast transformation lymphocytes induced by a Con-A suboptimal dose. The increase of cells activity was comparable with the effect of interleukin-2, added at a dose of 50-100 unit/ml.
Subject(s)
Atrial Natriuretic Factor , Cytotoxicity, Immunologic , Lymphocyte Activation/drug effects , Blood Donors , Cardiomyopathy, Dilated/immunology , Cells, Cultured , Concanavalin A/pharmacology , Cytotoxicity Tests, Immunologic , Humans , Interleukin-2/pharmacologyABSTRACT
The paper is devoted to analysis of the potentialities of radionuclide renography as a method for assessment of the effectiveness of radiotherapy of bladder cancer. The results obtained suggested close correlation between change of renal function and the results of irradiation. Normal renal function was observed in 3 patients, improvement--in 16 patients, and deterioration--in 8 patients whereas a complete effect of radiotherapy brought about the following figures: 5, 11 and 3, respectively. A conclusion was made of a high significance of renography parameters in objective assessment of the results of radiotherapy of bladder cancer in conjunction with other therapeutic modalities.
Subject(s)
Carcinoma, Transitional Cell/radiotherapy , Kidney/radiation effects , Urinary Bladder Neoplasms/radiotherapy , Aged , Carcinoma, Transitional Cell/diagnostic imaging , Carcinoma, Transitional Cell/physiopathology , Humans , Kidney/diagnostic imaging , Kidney/physiopathology , Kidney Function Tests , Male , Radioisotope Renography , Urinary Bladder Neoplasms/diagnostic imaging , Urinary Bladder Neoplasms/physiopathology , UrographyABSTRACT
The paper is devoted to analysis of the potentialities of radionuclide renography as a method for assessment of the effectiveness of radiotherapy of bladder cancer. The results obtained suggested close correlation between change of renal function and the results of irradiation. Normal renal function was observed in 3 patients, improvement--in 16 patients, and deterioration--in 8 patients whereas a complete effect of radiotherapy brought about the following figures: 5, 11 and 3, respectively. A conclusion was made of a high significance of renography parameters in objective assessment of the results of radiotherapy of bladder cancer in conjunction with other therapeutic modalities.
Subject(s)
Carcinoma, Transitional Cell/radiotherapy , Kidney/diagnostic imaging , Kidney/radiation effects , Radioisotope Renography , Urinary Bladder Neoplasms/radiotherapy , Humans , Male , Treatment OutcomeABSTRACT
The content of peptide hydra morphogen (PHM) was measured for the first time in blood plasma and CSF by RIA in patients with purulent meningitides. 36 patients were examined. Blood and CSF were withdrawn in the acute period and during early convalescence. In the reference group (patients with acute respiratory diseases of virus etiology, quinsy, pneumonias), the PHM concentration in the blood was 128 +/- 62 fm/ml, that in CSF 66 +/- 14 fm/ml. In purulent meningitis of medium gravity, the content of PHM in blood plasma and CSF did not significantly differ from the control. Grave purulent meningitis was marked by a high content of PHM in blood plasma and CSF, in particular, in the acute period and during early convalescence. It was 1250.30 +/- 191 and 544.03 +/- 159 fm/ml in blood plasma and 1504.38 +/- 475 and 1811.39 +/- 375 fm/ml in CSF, respectively. In grave complicated purulent meningitis, which was mainly observed in persons over 50 years, the content of PHM in blood plasma exceeded but insignificantly the content in the control during the acute period (327.49 +/- 76 fm/ml), followed by further increase (1131.41 +/- 209 fm/ml) by days 8-12 of the disease; within the same time, the content of PHM in CSF did not significantly differ from the control (319.52 +/- 152 and 625.69 +/- 275 fm/ml, respectively). In view of the fact that hypothalamic PHM is of crucial importance in the processes of nervous tissue regeneration, the content of the latter one in CSF in patients with grave purulent meningitis may serve as a criterion for disease course tendencies.
Subject(s)
Meningitis, Meningococcal/metabolism , Meningitis, Pneumococcal/metabolism , Neuropeptides/analysis , Acute Disease , Adolescent , Adult , Aged , Convalescence , Female , Humans , Male , Middle Aged , Pyrrolidonecarboxylic Acid/analogs & derivatives , Respiratory Tract Infections/metabolism , Time Factors , Virus Diseases/metabolismABSTRACT
The effect of regulatory peptides on the functional activity of pancreatic cells and phagocytic cells of reticuloendothelial system were determined in intact dogs against the background of acute experimental pancreatitis. Assessment of the efficacy of regulatory peptides was made with the aid of scintigraphic studies in gamma chamber using for this purpose colloid 198Au and 75Se-methionine. It was established that introduction of regulatory peptides to dogs leads to inhibition of capture of labeled methionine by pancreatocytes, practically not influencing the elimination of colloid gold from circulation.
Subject(s)
Calcitonin/therapeutic use , Enkephalin, Leucine-2-Alanine/analogs & derivatives , Enkephalin, Leucine/analogs & derivatives , Pancreatitis/drug therapy , Somatostatin/therapeutic use , Sympatholytics/therapeutic use , Acute Disease , Animals , Calcitonin/pharmacology , Dogs , Enkephalin, Leucine/pharmacology , Enkephalin, Leucine/therapeutic use , Mononuclear Phagocyte System/drug effects , Pancreatitis/diagnostic imaging , Phagocytosis/drug effects , Radionuclide Imaging , Somatostatin/pharmacology , Sympatholytics/pharmacologyABSTRACT
The use of a synthetic peptide analog of LH-RH agonist--[D-Ala6, des Gly10, Pro9]-LH-RH ethylamide (surfagon) at microdoses and in short courses returned to normal the ovulatory cycle in the anovulatory condition in rats and caused luteinization of follicular cysts in rats and cows with further normalization of ovarian function. It is assumed that surfagon will be effective for the treatment of anovulatory condition and ovarian follicular cysts in women.
Subject(s)
Follicular Cyst/drug therapy , Gonadotropin-Releasing Hormone/analogs & derivatives , Hormones/therapeutic use , Ovarian Cysts/drug therapy , Animals , Anovulation/drug therapy , Anovulation/etiology , Cattle , Cattle Diseases/drug therapy , Dinoprost/therapeutic use , Drug Evaluation, Preclinical/veterinary , Female , Follicular Cyst/etiology , Follicular Cyst/veterinary , Gonadotropin-Releasing Hormone/therapeutic use , Luteinizing Hormone/blood , Ovarian Cysts/etiology , Ovarian Cysts/veterinary , Ovariectomy , Ovary/pathology , Rats , Rats, Inbred StrainsABSTRACT
It is shown in experiments on mice that injection of Hydra Peptide Morphogen in doses of 30 micrograms/kg normalizes the content of cyclic nucleotides in the liver, disturbed as a result of injury. Hydra Peptide Morphogen did not change the content of cyclic nucleotides in the injured muscle.
Subject(s)
Cyclic AMP/analysis , Cyclic GMP/analysis , Liver/injuries , Muscles/injuries , Neuropeptides/pharmacology , Animals , Female , Liver/metabolism , Male , Mice , Mice, Inbred BALB C , Muscles/metabolism , Neuropeptides/administration & dosage , Pyrrolidonecarboxylic Acid/analogs & derivatives , Time FactorsSubject(s)
Follicle Stimulating Hormone/blood , Gonadotropin-Releasing Hormone/pharmacology , Luteinizing Hormone/blood , Ovulation/drug effects , Pituitary Gland/metabolism , Animals , Female , Gonadotropin-Releasing Hormone/analogs & derivatives , In Vitro Techniques , Male , Pituitary Gland/drug effects , Rats , Rats, Inbred StrainsABSTRACT
Pap test was used to study gastric and duodenal G and D cells, blood gastrin levels, basal and stimulated acid production, clinical manifestations, and morphological characteristics of the mucosa in 39 patients with duodenal ulcer and 13 controls. The findings enable the authors to outline a special form of peptic ulcer that is characterized by gastrin cellular hyperplasia concurrent with relative pyloric D cell deficit, gastric metaplasia in the duodenum and gastric hypersecretion. Such patients have more frequently multiple ulcers, predominantly 0(I) blood group, complication-aggravated course of the disease, and ulcer history in close relatives. Moreover, it has been demonstrated that incidence of gastric metaplasia is due to gastric hypersecretion; hyperplasia of duodenal gastrin cells is associated with incidence of gastric metaplasia in patients with peptic ulcer.
Subject(s)
Duodenal Ulcer/pathology , Duodenum/pathology , APUD Cells/pathology , Adolescent , Adult , Aged , Humans , Hyperplasia , Male , Middle Aged , Stomach/pathologyABSTRACT
The radioligand-receptor method was used to assay the M-cholinereceptors and opioid binding centers in biopsy specimens of the duodenal mucosa from 40 patients with duodenal ulcer as compared with the results of subsequent therapy by means of gastrocepin (20 patients) and dalargin (20 patients). Analysis of the isothermal curve of 3H-QNB-binding with duodenal mucosa membranes within Skatchard's coordinates showed the presence of 2 subtypes of muscarinic receptors blocked (M1) and not blocked (M2) by gastrocepin. The majority of the patients in both groups demonstrated a significant decrease of the dissociation constant as compared to the control (20 patients). In patients with high receptor sensitivity to gastrocepin and dalargin, ulcer cicatrization was noted during the treatment in all the cases. Meanwhile the treatment proved little effective in patients with appreciably decreased receptor sensitivity to the drugs under consideration. The data obtained indicate the possibility of predicting the results of duodenal ulcer treatment by means of the radioreceptor analysis, providing the basis for the individualized treatment choice.
Subject(s)
Anti-Ulcer Agents/therapeutic use , Duodenal Ulcer/drug therapy , Duodenum/drug effects , Enkephalin, Leucine-2-Alanine/analogs & derivatives , Enkephalin, Leucine/analogs & derivatives , Intestinal Mucosa/drug effects , Pirenzepine/therapeutic use , Receptors, Muscarinic/drug effects , Receptors, Opioid/drug effects , Adolescent , Adult , Clinical Trials as Topic , Duodenum/analysis , Enkephalin, Leucine/therapeutic use , Female , Humans , Intestinal Mucosa/analysis , Male , Middle Aged , Radioligand Assay , Receptors, Muscarinic/analysis , Receptors, Opioid/analysisABSTRACT
The effect of several synthetic FMRF-like peptides in hemodynamics and tonus of isolated rat vessels was studied. Peptide pGlu-Aps-Pro-Phe-Leu-Arg-Phe-NH2 and its C-terminal fragment Arg-Phe-NH2 induced i.v. short-term increase in arterial blood pressure and heart rate in narcotized rats. Benzpgexonium could reduce both effects of the drug. The peptide effect on blood pressure could be neutralized by prazosin; tachycardia could be prevented by propranolol. The studied peptide and its C-end tetra-, penta- and dipeptide produced relaxation of isolated rat aorta toned by prostaglandin F2 alpha. It is supposed that hypertensive effect of FMRF-like peptides is realized through central mechanisms.
Subject(s)
Blood Pressure/drug effects , Helix, Snails , Hypertension/etiology , Neuropeptides/adverse effects , Oligopeptides/adverse effects , Tissue Extracts/adverse effects , Animals , Aorta, Thoracic/drug effects , Aorta, Thoracic/physiopathology , Culture Media , FMRFamide , In Vitro Techniques , Male , Neuropeptides/pharmacology , Oligopeptides/pharmacology , Rats , Rats, Inbred Strains , Tissue Extracts/pharmacologyABSTRACT
The biological activity of surfagon (D-Ala6-desGly10-Pro9-ethylamide), a synthetic LH-RH agonist, is dozens of times higher than that of LH-RH in the test of rat hypophyseal stimulation of gonadotropin secretion in vivo and in vitro and in the ovulation induction test. A dose of surfagon required for the stimulation of LH secretion was considerably lower than that for the stimulation of FSH secretion. It may permit the use of surfagon in clinical practice for selective stimulation of secretion either of LH or total gonadotropins--LH and FSH.
Subject(s)
Gonadotropin-Releasing Hormone/analogs & derivatives , Animals , Culture Techniques , Dose-Response Relationship, Drug , Female , Follicle Stimulating Hormone/blood , Follicle Stimulating Hormone/metabolism , Gonadotropin-Releasing Hormone/isolation & purification , Gonadotropin-Releasing Hormone/pharmacology , Luteinizing Hormone/blood , Luteinizing Hormone/metabolism , Male , Ovulation/drug effects , Pituitary Gland/drug effects , Pituitary Gland/metabolism , Rats , Rats, Inbred Strains , Time FactorsABSTRACT
Porcine liver extract inhibits (+)-[3H]SKF 10047 binding to rat liver membranes. The inhibitors of (+)-[3H]SKF 10047 binding were detected in acetone supernatant and in acid acetonated powder of the liver extract. Partial purification of the acetone supernatant revealed some characteristics of these inhibitors: low molecular weight (less than 1000), thermostability, resistance to pronase digestion, solubility in water and organic solvents.
Subject(s)
Liver/metabolism , Phenazocine/analogs & derivatives , Receptors, Opioid/isolation & purification , Acetone , Animals , Chromatography, Gel , Ligands , Phenazocine/metabolism , Radioligand Assay , Receptors, Opioid/metabolism , Receptors, sigma , SwineABSTRACT
Monoclonal antibodies (MABs) to a new drug Dalargin (Tyr-D-Ala-Gly-Phe-Leu-Arg) enhancing ulcer healing have been produced. Dalargin is a synthetic analog of Leu-enkephalin. With about 40 compounds tested in competition radioimmunoassay it has been shown that specificity of the MABs is directed against the N-terminal tetrapeptide of the molecule. The MABs are sensitive to amino acid substitutions in any of the positions of the fragment and have no cross-reactivity with endogenous opioids. Their further application in pharmacokinetic studies in humans and for characterization of opioid receptors is discussed.
Subject(s)
Antibodies, Monoclonal , Enkephalin, Leucine-2-Alanine/analogs & derivatives , Enkephalin, Leucine/analogs & derivatives , Amino Acid Sequence , Animals , Enkephalin, Leucine/immunology , Male , Mice , Mice, Inbred BALB C , Molecular Sequence Data , Peptide Fragments/immunologyABSTRACT
Bioavailability and metabolism of a peptide drug Dalargin with a chemical structure Tyr-D-Ala-Gly-Phe-Leu-Arg have been examined. Dalargin is applied for the treatment of gastric and duodenal ulcers. Bioavailability was estimated following intramuscular (i/m) and intranasal (i/n) routes of administration of 3H-dalargin in anesthetized dogs. The highest dalargin concentration was achieved about 10 min after i/m and i/n administration. Absolute dalargin bioavailability was 15% and 8%, while its elimination half-life was 23.2 min and 21.3 min, respectively. Tyrosine, N-terminated tetra- and pentapeptides were the main metabolites detected in the blood. The intranasal route of dalargin administration is concluded to be possible in the clinical practice.
Subject(s)
Anti-Ulcer Agents/pharmacokinetics , Enkephalin, Leucine-2-Alanine/analogs & derivatives , Enkephalin, Leucine/analogs & derivatives , Administration, Intranasal , Animals , Anti-Ulcer Agents/administration & dosage , Anti-Ulcer Agents/metabolism , Biological Availability , Enkephalin, Leucine/administration & dosage , Enkephalin, Leucine/metabolism , Enkephalin, Leucine/pharmacokinetics , Male , Rats , Rats, Inbred StrainsSubject(s)
Anti-Ulcer Agents/administration & dosage , Duodenal Ulcer/drug therapy , Enkephalin, Leucine-2-Alanine/analogs & derivatives , Enkephalin, Leucine/analogs & derivatives , Administration, Inhalation , Adult , Aerosols , Animals , Drug Evaluation , Drug Evaluation, Preclinical , Duodenal Ulcer/chemically induced , Enkephalin, Leucine/administration & dosage , Humans , Male , Middle Aged , Pirenzepine/administration & dosage , Rats , Rats, Inbred StrainsABSTRACT
To generate the antibodies to the transforming protein of Rous sarcoma virus (RSV) pp60src, rabbits were immunized with the peptide, corresponding to 415-421 sequence of pp60src. These antibodies immunoprecipitate pp60src in RSV-transformed chicken and mammalian cells, and also some proteins (45, 85 and 120 kDa), which could be autophosphorylated in vitro. It was shown that 415-421 sequence of pp60src is not recognized by the antibodies to pp60src from RSV-induced tumour bearing rabbits (TBR serum). In contrast to TBR serum, antibodies, generated against synthetic peptide, corresponding 415-421 sequence of pp60src couldn't be phosphorylated in vitro, when [gamma-32P]ATP is added to the immune complex. The antipeptide antibodies, bound to pp60src did not block phosphorylation of TBR immunoglobulins, added to this immune complex. Hence, 415-421 sequence of pp60src RSV containing the major tyrosine phosphorylation site does not take part in the kinase reaction in vitro.