RESUMEN
The protective action of enzymatically stable analogue of Leu-enkephalin (D-ala-2-leu5-arg6), injected intraperitoneally, in the course of stress- and epinephrine induced myocardial damage was demonstrated in animal (129 white rats) experiments. Two effect of enkephalin were sufficient for the cardiac protection: enkephalin-stimulated prostacyclin biosynthesis and simultaneous inhibition of thromboxane production.
Asunto(s)
Leucina Encefalina-2-Alanina/análogos & derivados , Encefalina Leucina/análogos & derivados , Epinefrina/toxicidad , Corazón/efectos de los fármacos , Miocardio/metabolismo , Prostaglandinas/metabolismo , Estrés Psicológico/tratamiento farmacológico , Animales , Reacción de Prevención/efectos de los fármacos , Condicionamiento Clásico/efectos de los fármacos , Conflicto Psicológico , Evaluación Preclínica de Medicamentos , Estabilidad de Medicamentos , Encefalina Leucina/farmacología , Encefalina Leucina/uso terapéutico , Epoprostenol/metabolismo , Ratas , Estrés Psicológico/metabolismo , Tromboxanos/metabolismoRESUMEN
The possibility of transversion of low-reacting mice into high-reacting ones evaluated by the application of the natural immunostimulators. L-tyrosine and thymic polypeptides (taktivin) were compared by their ability for the phenotypical correction of the immune response of the oppositely reacting mice. It was established that under the application of L-tyrosine to oppositely reacting mice the phenotypical correction of the immune response is possible. The dramatic increase in AFC and the AFC-SI secreting IgM is observed in the mice, low-reacting to SRBC in comparison with the high-reacting lines.
Asunto(s)
Adyuvantes Inmunológicos/farmacología , Reacciones Antígeno-Anticuerpo/efectos de los fármacos , Eritrocitos/inmunología , Tirosina/farmacología , Animales , Células Productoras de Anticuerpos/efectos de los fármacos , Células Productoras de Anticuerpos/inmunología , Inmunización , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Endogámicos CBA , Péptidos/farmacología , Fenotipo , Ovinos/inmunología , Bazo/efectos de los fármacos , Bazo/inmunología , Extractos del Timo/farmacologíaAsunto(s)
Antiulcerosos/administración & dosificación , Úlcera Duodenal/tratamiento farmacológico , Leucina Encefalina-2-Alanina/análogos & derivados , Encefalina Leucina/análogos & derivados , Administración por Inhalación , Adulto , Aerosoles , Animales , Evaluación de Medicamentos , Evaluación Preclínica de Medicamentos , Úlcera Duodenal/inducido químicamente , Encefalina Leucina/administración & dosificación , Humanos , Masculino , Persona de Mediana Edad , Pirenzepina/administración & dosificación , Ratas , Ratas EndogámicasAsunto(s)
Endorfinas/sangre , Choque Hemorrágico/sangre , Choque Traumático/sangre , Nucleótidos de Adenina/sangre , Animales , Evaluación Preclínica de Medicamentos , Endorfinas/uso terapéutico , Encefalina Leucina/uso terapéutico , Femenino , Masculino , Ratas , Choque Hemorrágico/tratamiento farmacológico , Choque Traumático/tratamiento farmacológico , betaendorfina/uso terapéuticoRESUMEN
The experiments on 24 dogs with experimental hemorrhagic pancreonecrosis showed that contrykal and 5-fluorouracil insignificantly decrease the area of the damaged parenchyma, fail to cease progression of the pancreas destruction. The peptide drug dalargin in these conditions increased the antitryptic activity and normalized BAEE esterase activity. Dalargin abolished erythrostasis and microthromboses in the vessels of the microcirculation, restored the blood supply throughout the area of the exocrine parenchyma, limited necrotic foci and suspended the development of pancreonecrosis.
Asunto(s)
Aprotinina/uso terapéutico , Leucina Encefalina-2-Alanina/análogos & derivados , Encefalina Leucina/análogos & derivados , Fluorouracilo/uso terapéutico , Pancreatitis/tratamiento farmacológico , Animales , Modelos Animales de Enfermedad , Perros , Evaluación Preclínica de Medicamentos , Encefalina Leucina/uso terapéutico , Hemorragia/tratamiento farmacológico , Hemorragia/fisiopatología , Necrosis , Páncreas/efectos de los fármacos , Páncreas/enzimología , Páncreas/metabolismo , Pancreatitis/fisiopatologíaRESUMEN
The role and possible clinical use of regulatory peptides, a new type of regulatory substances, is discussed. Special attention is paid to the opioid peptides and their analogues. The new drug dalargin has been developed on the basis of the endogenous opioid peptide leucine-encephalin. Its action has been studied using experimental models. It has been established that the optimal dose (10 micrograms/kg) of dalargin is effective in preventing ulceration in the cystamine duodenal ulcer rat model and the development of stomach erosive lesions in immobilization stress, reducing the degree of liver degeneration in CCl4 poisoning, etc. With an increase of the dose of dalargin the effect "escapes". Dalargin is primarily bound by delta-receptors, it produces no analgetic effect and does not enter the brain. Dalargin exhibits a pronounced cytoprotective and regeneratory action and may take an important place in treating the internal organ diseases.
Asunto(s)
Leucina Encefalina-2-Alanina/análogos & derivados , Encefalina Leucina/análogos & derivados , Animales , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Células Cultivadas , Modelos Animales de Enfermedad , Perros , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Úlcera Duodenal/inducido químicamente , Úlcera Duodenal/tratamiento farmacológico , Encefalina Leucina/farmacología , Encefalina Leucina/uso terapéutico , Hemorragia/tratamiento farmacológico , Hemorragia/etiología , Humanos , Linfocitos/efectos de los fármacos , Ratones , Necrosis , Páncreas/patología , Ratas , Receptores Opioides/efectos de los fármacos , Úlcera Gástrica/tratamiento farmacológico , Úlcera Gástrica/etiologíaRESUMEN
Experiments on unrestrained rats were carried out to study the effect of intraventricularly injected met- and leu-enkephalins and their synthetic analog Tyr-dAla-Cly-Phe-NH2 on analgesia induced by electrical stimulation of the central gray. It was shown that subanalgesic doses of enkephalins and their synthetic analog facilitated the appearance of analgesic action on subthreshold antinociceptive-brain stimulation and potentiated the analgesic effect of threshold central gray stimulation. Subanalgesic and low analgesic doses of the peptides increased antinociceptive effect of electroacupuncture. The data obtained are discussed from the standpoint of the implication of the peptidergic mechanisms in the realization of acupuncture and stimulation analgesia.
Asunto(s)
Analgesia/métodos , Endorfinas/farmacología , Encefalinas/farmacología , Manejo del Dolor , Terapia por Acupuntura , Animales , Tronco Encefálico/fisiopatología , Terapia por Estimulación Eléctrica , Encefalina Leucina , Encefalina Metionina , Masculino , Dolor/fisiopatología , RatasRESUMEN
Intracisternal administration of leu- or met-enkephalins in a dose of 100 micrograms into unanesthetized cats evoked a short-lasting elevation of arterial pressure and tachycardia. After 1.5-2 minutes the blood pressure returned to normal and bradycardia developed (heart rate = 86 +/- 3.4% of initial). Alterations in the arterial pressure and heart rate were prevented by naloxon in a dose of 50-100 micrograms administered into the 4th ventricle. Leu-enkephalin inhibited the sensitivity of the baroreceptor reflex and increased by 69% the pressor reactions evoked by hypothalamus stimulation. Met-enkephalin was half as potent with respect to the baroreceptor reflex and exerted no effect on the hemodynamic reactions evoked by hypothalamus stimulation.