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Article

Ex Vivo and In Vivo Study of Some Isoquinoline Precursors

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Department of Bioorganic Chemistry, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria
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Department of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria
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Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria
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Department of Pharmacology and Clinical Pharmacology, Faculty of Medicine, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria
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Department of Pharmacology and Drug Toxicology, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria
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Research Institute, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria
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Author to whom correspondence should be addressed.
Academic Editor: Helen D. Skaltsa
Sci. Pharm. 2022, 90(2), 37; https://doi.org/10.3390/scipharm90020037
Received: 4 April 2022 / Revised: 21 May 2022 / Accepted: 6 June 2022 / Published: 13 June 2022
(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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. View Full-Text
Keywords: synthesis; isoquinoline precursors; in silico; smooth muscle relaxants; learning and memory processes in rats synthesis; isoquinoline precursors; in silico; smooth muscle relaxants; learning and memory processes in rats
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MDPI and ACS Style

Milusheva, M.; Gledacheva, V.; Batmazyan, M.; Nikolova, S.; Stefanova, I.; Dimitrova, D.; Saracheva, K.; Tomov, D.; Chaova-Gizdakova, V. Ex Vivo and In Vivo Study of Some Isoquinoline Precursors. Sci. Pharm. 2022, 90, 37. https://doi.org/10.3390/scipharm90020037

AMA Style

Milusheva M, Gledacheva V, Batmazyan M, Nikolova S, Stefanova I, Dimitrova D, Saracheva K, Tomov D, Chaova-Gizdakova V. Ex Vivo and In Vivo Study of Some Isoquinoline Precursors. Scientia Pharmaceutica. 2022; 90(2):37. https://doi.org/10.3390/scipharm90020037

Chicago/Turabian Style

Milusheva, Miglena, Vera Gledacheva, Margarita Batmazyan, Stoyanka Nikolova, Iliyana Stefanova, Darinka Dimitrova, Kremena Saracheva, Desislav Tomov, and Veneta Chaova-Gizdakova. 2022. "Ex Vivo and In Vivo Study of Some Isoquinoline Precursors" Scientia Pharmaceutica 90, no. 2: 37. https://doi.org/10.3390/scipharm90020037

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