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1.
Biomed Khim ; 69(6): 353-370, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38153051

RESUMEN

A1-adenosine receptors (A1AR) are widely distributed in the human body and mediate many different effects. They are abundantly present in the cardiovascular system, where they control angiogenesis, vascular tone, heart rate, and conduction. This makes the cardiovascular system A1AR an attractive target for the treatment of cardiovascular diseases (CVD). The review summarizes the literature data on the structure and functioning of A1AR, and analyzes their involvement in the formation of myocardial hypertrophy, ischemia-reperfusion damage, various types of heart rhythm disorders, chronic heart failure, and arterial hypertension. Special attention is paid to the role of some allosteric regulators of A1AR as potential agents for the CVD treatment.


Asunto(s)
Enfermedades Cardiovasculares , Agonistas del Receptor Purinérgico P1 , Humanos , Enfermedades Cardiovasculares/tratamiento farmacológico
2.
Biomed Khim ; 69(2): 112-124, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37132493

RESUMEN

The cardioprotective effects of new derivatives of glutamic acid (glufimet) and GABA (mefargin) were studied in rats exposed to acute alcohol intoxication (AAI) under conditions of selective blockade of inducible NO-synthase (iNOS). AAI induced a pronounced decrease in the contractile function of the myocardium during exercise tests (load by volume, test for adrenoreactivity, isometric exercise), caused mitochondrial dysfunction and increased processes of lipid peroxidation (LPO) in heart cells. A decrease in NO production during iNOS inhibition and AAI improved the respiratory function of mitochondria, a decreased the level of LPO products, and increased mitochondrial superoxide dismutase activity of heart cells. This led to an increase in myocardial contractility. The studied compounds, glufimet and mefargin, caused a statistically significant increase in the rates of myocardial contraction and relaxation, left ventricular pressure, and also reduced NO production. This was accompanied by a decrease in the intensity of LPO processes and an increase in the respiratory control ratio (RCR), reflecting the coupling between respiration and phosphorylation processes during activation of the respiratory chain complexes I and II. The decrease in NO concentration during selective blockade of iNOS and administration of the studied substances was less pronounced than without blockade of the enzyme. This suggests the putative effect of new derivatives of neuroactive amino acids on the NO system.


Asunto(s)
Intoxicación Alcohólica , Cardiotónicos , Corazón , Animales , Ratas , Ácido gamma-Aminobutírico/farmacología , Ácido Glutámico/farmacología , Contracción Miocárdica , Miocardio/metabolismo , Cardiotónicos/farmacología
3.
Artículo en Ruso | MEDLINE | ID: mdl-35485072

RESUMEN

OBJECTIVE: To study an effect of neuroactive amino acids derivatives glufimet and mefargin on the psychoemotional state of rats after chronic alcohol intoxication (CAI). MATERIAL AND METHODS: The study was carried out on 10-month-old female Wistar rats. CAI was modeled by replacing drinking water with a 10% solution of ethyl alcohol sweetened with sucrose (50 g/l) for 6 months. Animals (age - 16 months) were divided into groups at the end of alcoholization: 1 (n=15) - intact group - rats without CAI; 2 (n=14) - control - females after CAI; 3 (n=11), 4 (n=14), 5 (n=11) and 6 (n=10) - experimental - females after CAI who received the GABA derivative mefargin (25 mg/kg), the glutamic acid derivative glufimet (29 mg/kg) and comparison drugs phenotropil (25 mg/kg) and heptral (100 mg/kg), respectively. Substances were administered to rats after 6 months of alcoholization intraperitoneally once a day for 14 days, the intact and control groups received physiological saline. The psychoemotional state of the animals was studied in the «Open field¼ test, «Elevated plus maze¼ test, «Marble burying¼ test and the Porsolt swim test after the treatment. RESULTS: In animals of the control group, an increase in anxiety was noted, as evidenced by a greater number of boluses in the Open Field test (3.43±0.56 vs. 1.47±0.39) compared to the intact group (p<0.05), short duration of stay in open arms (26.07±3.47 vs. 68.67±10.08) and fewer hangings from them (3.07±0.25 vs. 6.67±0.79) in the «Elevated plus maze¼ test. Rats after CAI buried more balls (8.79±1.15 versus 2.73±0.71, p<0.05), which indicated that they had compulsive behavior. In addition, females of the control group were observed to be depressed, as evidenced by a long period of immobilization in the Porsolt swim test (2.36±0.41 versus 0.87±0.31, p<0.05). CONCLUSION: Mefargin, glufimet, phenotropil and heptral restricted anxiety and manifestations of obsessive-compulsive disorder in females subjected to alcoholism (p<0.05). The antidepressant effect was observed in animals treated with phenotropil and heptral after CAI (p<0.05).


Asunto(s)
Intoxicación Alcohólica , Alcoholismo , Alcoholismo/tratamiento farmacológico , Aminoácidos/farmacología , Animales , Conducta Animal/fisiología , Femenino , Humanos , Ratas , Ratas Wistar
4.
Bull Exp Biol Med ; 168(4): 457-464, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-32146627

RESUMEN

We studied the effects of GABA derivatives on anxious and compulsive behavior of progeny of rats with experimental preeclampsia provoked by replacement of drinking water for 1.8% NaCl solution from the first day of pregnancy to delivery. In comparison with progeny of health rats, the offspring of dams with complicated pregnancy demonstrated high level of anxiety and the development of obsessive-compulsive disorder both at the early (40 and 70 days) and late (6 and 12 months) stages of ontogeny. GABA derivatives succicard, salifen, and phenibut reduced symptoms of experimental preeclampsia in offspring of various age by decreasing the level of anxiety and reducing compulsive behavior. The efficacy of the examined derivatives was similar to that of the reference drug Pantogam.


Asunto(s)
Ansiedad/tratamiento farmacológico , Agonistas del GABA/farmacología , Trastorno Obsesivo Compulsivo/tratamiento farmacológico , Preeclampsia/tratamiento farmacológico , Efectos Tardíos de la Exposición Prenatal/tratamiento farmacológico , Ácido gamma-Aminobutírico/análogos & derivados , Animales , Animales no Consanguíneos , Ansiolíticos/farmacología , Ansiedad/inducido químicamente , Ansiedad/metabolismo , Ansiedad/fisiopatología , Conducta Animal/efectos de los fármacos , Femenino , Masculino , Trastorno Obsesivo Compulsivo/inducido químicamente , Trastorno Obsesivo Compulsivo/metabolismo , Trastorno Obsesivo Compulsivo/fisiopatología , Ácido Pantoténico/análogos & derivados , Ácido Pantoténico/farmacología , Preeclampsia/inducido químicamente , Preeclampsia/metabolismo , Preeclampsia/fisiopatología , Embarazo , Efectos Tardíos de la Exposición Prenatal/inducido químicamente , Efectos Tardíos de la Exposición Prenatal/metabolismo , Efectos Tardíos de la Exposición Prenatal/fisiopatología , Ratas , Cloruro de Sodio/administración & dosificación , Tranquilizantes/farmacología , Ácido gamma-Aminobutírico/farmacología
5.
Biomed Khim ; 64(4): 334-343, 2018 Aug.
Artículo en Ruso | MEDLINE | ID: mdl-30135280

RESUMEN

Experimental chronic heart failure (CHF), caused by administration of L-isoproterenol (2.5 mg/kg twice a day intraperitoneally for 21 days), promotes uncoupling of respiration and oxidative phosphorylation. The rate of mitochondrial oxygen consumption in the metabolic state V3 by Chance in animals with CHF decreased by 53.3% (p<0.05) with malate using (as an oxidation substrate feeding сomplex I of the electron transport chain (ETC)), by 70.6% (p<0.05) with succinate using (сomplex II substrate) and by 63.6% (p<0.05) when malate and succinate were added simultaneously. The respiratory control ratio significantly decreased 2.3 times for сomplex I, 2.5 for сomplex II, and 2.6 times for the simultaneous operation of two respiratory chain complexes in mitochondria of CHF rats compared to intact animals. Mitochondrial dysfunction in experimental CHF is evidently due to the development of oxidative stress. It was revealed that the content of malonic dialdehyde (MDA) in the group of rats with experimental CHF was higher by 54.7% (p<0.05), as compared with intact animals. The activity of superoxide dismutase (SOD) and catalase was lower by 17.5% (p<0.05), and by 18.4%, respectively than in the intact group. The dense extract from herba of Primula veris L. (DEHPV) 30 mg/kg limits the development of mitochondrial dysfunction in rats with experimental CHF, as evidenced by an increase in the role of V3 respiration for the first and second respiratory chain complexes in 1.7 (p<0.05) and 2.0 times (p<0.05), respectively, the ratio of respiratory control (RCR) - 1.7 times (p<0.05) for сomplex I and 2 times (p<0.05) for сomplex II compared with the negative control. The concentration of MDA was by 15.7% (p<0.05), lower and the activity of SOD was by 56.3% (p<0.05) higher.


Asunto(s)
Insuficiencia Cardíaca/prevención & control , Mitocondrias Cardíacas/efectos de los fármacos , Miocitos Cardíacos/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Primula/química , Animales , Antioxidantes/metabolismo , Enfermedad Crónica , Modelos Animales de Enfermedad , Insuficiencia Cardíaca/metabolismo , Masculino , Mitocondrias Cardíacas/metabolismo , Miocitos Cardíacos/metabolismo , Consumo de Oxígeno/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Ratas
6.
Bull Exp Biol Med ; 164(5): 605-608, 2018 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29577203

RESUMEN

Experimental preeclampsia induced by substitution of drinking water with 1.8% NaCl during pregnancy was associated with an increase in the level of DNA damage in fetal brain and placenta measured by DNA comet assay by 35.7 and 27.8 times, respectively, in comparison with physiological pregnancy.


Asunto(s)
Ensayo Cometa/métodos , Daño del ADN/genética , Preeclampsia/genética , Encéfalo/metabolismo , Daño del ADN/efectos de los fármacos , Femenino , Humanos , Placenta/metabolismo , Embarazo , Cloruro de Sodio/farmacología
7.
Ross Fiziol Zh Im I M Sechenova ; 102(7): 833-46, 2016 Jul.
Artículo en Ruso | MEDLINE | ID: mdl-30193051

RESUMEN

Changes in the metabolism of female rats hanging by cervical dorsal skin fold within 24 hours were examined. It was found that stress exposure results in an increase of the concentration of the final nitric oxide metabolites in the blood serum and homogenates of the heart and brain of animals, intensification of processes peroxidation lipids and mitochondrial dysfunction in these organs. Thus increase of mean arterial blood pressure by 18.9 % from baseline and violation of platelet and plasma components of hemostasis. Inhibitor of neuronal NO-synthase 7-nitroindazole in the dose of 50 mg/kg aggravates of the studied parameters changes. Administration of an animal selective inhibitor of inducible NOS aminoguanidine (50 mg / kg) contributes to limiting the damaging effects of stress reaction.


Asunto(s)
Inhibidores Enzimáticos/farmacología , Hemostasis/efectos de los fármacos , Óxido Nítrico Sintasa de Tipo II/antagonistas & inhibidores , Óxido Nítrico Sintasa de Tipo I/antagonistas & inhibidores , Estrés Oxidativo/efectos de los fármacos , Estrés Psicológico/tratamiento farmacológico , Animales , Presión Arterial/efectos de los fármacos , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Encéfalo/fisiopatología , Femenino , Guanidinas/farmacología , Corazón/efectos de los fármacos , Corazón/fisiopatología , Suspensión Trasera/métodos , Indazoles/farmacología , Peroxidación de Lípido/efectos de los fármacos , Mitocondrias/efectos de los fármacos , Mitocondrias/fisiología , Óxido Nítrico/agonistas , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo I/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Ratas , Estrés Psicológico/metabolismo , Estrés Psicológico/fisiopatología
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