Comparative Inotropic Effects of the Some Isoquinoline Alkaloids

Jumayev, Inoyat; Usmanov, P. B.; Rustamov, Shavkat Yu.; Zhurakulov, Sherzod

doi:10.13005/bpj/1892

Cited by 8 publications

(4 citation statements)

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“…Among 1-Aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines, sedative-anxiolytic (Mirzaev et al 2017), cytotoxic (Terentyeva et al 2019), antiarrhythmic, anti-inflammatory (Rakhmanova et al 2022), atypical neuroleptic (Mirzaev et al 2020) activities, and regulating the volume of thymocytes (Terentyeva et al 2016) substances have been found within their active characteristics. Some authors have explored the inotoropy and antiarrhythmic effects of isoquinoline alkaloids on heart muscle tissue (Zhumaev et al 2020), as well as the mechanisms of action on cardiomyocyte Ca 2+ transport systems (Zhumaev et al 2019). Taking for experimental purposes 1-(2´-bromine-4´,5´-dimethoxyphenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (F-18), 3,4-dimitoxyphynilethylamine, and 2-bromine are considered as compounds synthesized on the basis of 4,5dimethoxybenzaldehyde, which is characterized by its high physiological effect on biomembranes.…”

Section: Introductionmentioning

confidence: 99%

Effects of dihydroquercetin, 1-aryltetrahydroisoquinoline, and conjugate on the functional condition mitochondrial membrane of the rat liver

Ernazarov

Pozilov

Asrarov

et al. 2023

Nova Biotechnol. Chim.

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In the current research paper, the flavonoid dihydroquercetin, 1-(2´-bromine-4´,5´-dimethoxyphenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (F-18) and 2-(3,4-dihydroxyphenyl)-6-(1-(2´-bromine-4´, 5´-dimethoxyphenyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2 (1N)-il) methyl-3. The effects of 5,7-trigidroxychroman-4-on (DHQ-11) conjugate on rat liver mitochondrial calcium megachannels and on lipid peroxidation (LPO) induced using Fe2+/citrate were investigated in vitro experiments. White male rats weighing 180-200 grams were used in the experiments. It was found that the DHQ-11 conjugate was identified to have an inhibitory effect on rat liver mitochondria to calcium megachannels and peroxidation of lipids induced by Fe2+/citrate. The inhibitory properties of DHQ-11 conjugate on hepatic mitochondrial calcium megachannels and mitochondrial membrane lipid peroxidation were identified as active against dihydroquercetin and the F-18 isoquinoline alkaloid.

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Section: Introductionmentioning

confidence: 99%

Effects of dihydroquercetin, 1-aryltetrahydroisoquinoline, and conjugate on the functional condition mitochondrial membrane of the rat liver

Ernazarov

Pozilov

Asrarov

et al. 2023

Nova Biotechnol. Chim.

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“…Isoquinolines and tetrahydroisoquinolines can serve as good anesthetics, vasodilators, and antihypertensive and antibacterial agents [13]. These compounds possess an inotropic effect through their influence on Ca 2+ modulation [14] and have significant protective activity on memory dysfunction in rats, as well as cholinesterase (ChE) inhibitor activity [15]. The relationship between drugs inhibiting PDE activity and SM relaxation in the isolated guinea-pig colon has been well-known for a long time [16,17].…”

Section: Introductionmentioning

confidence: 99%

Ex Vivo and In Vivo Study of Some Isoquinoline Precursors

et al. 2022

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This article concerns the synthesis and biological activities of some N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides as isoquinoline precursors and compounds with smooth muscle (SM) relaxant activity. Aim: find the biological activity of N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides and compare it with papaverine, an isoquinoline alkaloid that has been known as a brain and coronary vasodilator and SM relaxant. Materials and methods: In silico simulation with the PASS online program predicts SM relaxant activity for the compounds. The amides were tested on the isolated gastric SM preparations (SMPs) from rats to determine their effects on spontaneous contractile activity (CA) compared with papaverine. The in vivo effect on the learning and memory processes of rats was also assessed. Results: the data from the isometric measurements showed that one of the compounds caused ex vivo relaxation in circular SM tissues isolated from the stomach (corpus) of male Wistar rats. Conclusion: We found that the compound’s SM relaxation uses the papaverine pathway. It also has an improving effect on the cognitive functions of learning and memory processes in rats.

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“…However, the possible antiarrhythmic mechanism of BH is as a membrane surface Na + -Ca 2+ exchange inhibitor [21]. In addition, it reduces sarcoplasmic reticulum Ca 2+ release by inhibiting sarcoplasmic reticulum RyR2Ca 2+ channels [22]. BH is still undergoing preclinical studies, and its pharmacokinetic profile and metabolites have not yet been studied.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic Study and Metabolite Identification of 1-(3′-bromophenyl)-heliamine in Rats

Abdulla

Zhang

et al. 2022

Pharmaceuticals

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Tetrahydroisoquinolines have been widely investigated for the treatment of arrhythmias. 1−(3′−bromophenyl)−heliamine (BH), an anti−arrhythmias agent, is a synthetic tetrahydroisoquinoline. This study focuses on the pharmacokinetic characterization of BH, as well as the identification of its metabolites, both in vitro and in vivo. A UHPLC−MS/MS method was developed and validated to quantify BH in rat plasma with a linear range of 1–1000 ng/mL. The validated method was applied to a pharmacokinetic study in rats. The maximum concentration Cmax (568.65 ± 122.14 ng/mL) reached 1.00 ± 0.45 h after oral administration. The main metabolic pathways appeared to be phase-I of demethylation, dehydrogenation, and epoxidation, and phase II of glucuronide and sulfate metabolites. Finally, a total of 18 metabolites were characterized, including 10 phase I metabolites and 8 phase II metabolites. Through the above studies, we have gained a better understanding of the absorption and metabolism of BH in vitro and in vivo, which will provide us with guidance for future in-depth studies on this compound.

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Comparative Inotropic Effects of the Some Isoquinoline Alkaloids

Cited by 8 publications

References 0 publications

Effects of dihydroquercetin, 1-aryltetrahydroisoquinoline, and conjugate on the functional condition mitochondrial membrane of the rat liver

Effects of dihydroquercetin, 1-aryltetrahydroisoquinoline, and conjugate on the functional condition mitochondrial membrane of the rat liver

Ex Vivo and In Vivo Study of Some Isoquinoline Precursors

Pharmacokinetic Study and Metabolite Identification of 1-(3′-bromophenyl)-heliamine in Rats

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