Therapeutic Potential of 1-(2-Chlorophenyl)-6,7-dimethoxy-3-methyl-3,4-dihydroisoquinoline

The synthesized compound 1-(2-chlorophenyl) 6-7-dimethoxy-3-methyl-3,4-dihydroisoquinoline (DIQ) was investigated as a biological agent. Its potential to affect muscle contractility was predicted through in silico PASS analysis. Based on the in silico analysis, its capabilities were experimentally investigated. The study aimed to investigate the effects of DIQ on the ex vivo spontaneous contractile activity (CA) of smooth muscle (SM) tissue. DIQ was observed to reduce the strength of Ca<sup>2+</sup>-dependent contractions in SM preparations (SMP), possibly by increasing cytosolic Ca<sup>2+</sup> levels through the activation of a voltage-gated L-type Ca<sup>2+</sup> channel. DIQ potently affected calcium currents by modulating the function of muscarinic acetylcholine receptors (mAChRs) and 5-hydroxytryptamine (5-HT) receptors at a concentration of 50 μM. Immunohistochemical tests showed a 47% reduction in 5-HT<sub>2A</sub> and 5-HT<sub>2B</sub> receptor activity in SM cells and neurons in the myenteric plexus (MP), further confirming the effects of DIQ. Furthermore, a significant inhibition of neuronal activity was observed when the compound was co-administered with 5-HT to SM tissues. The conducted experiments confirm the ability of the isoquinoline analog to act as a physiologically active molecule to control muscle contractility and related physiological processes.

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Publication Details

Journal
Molecules
Published
2024-08-11
DOI
https://doi.org/10.3390/molecules29163804
Citations
1
Primary Topic
Chemical synthesis and alkaloids
Type
article
Field-Weighted Citation Impact
0.25
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article

Therapeutic Potential of 1-(2-Chlorophenyl)-6,7-dimethoxy-3-methyl-3,4-dihydroisoquinoline

Mina Pencheva, Vera Gledacheva, Miglena Milusheva, Iliyana D. Stefanova et al.
1 citations
Molecules
Chemical synthesis and alkaloids
0.25
article

Therapeutic Potential of 1-(2-Chlorophenyl)-6,7-dimethoxy-3-methyl-3,4-dihydroisoquinoline

Mina Pencheva, Vera Gledacheva, Miglena Milusheva, Iliyana D. Stefanova, Stoyanka Nikolova, Valeri Slavchev
article en
1 citations

Abstract

The synthesized compound 1-(2-chlorophenyl) 6-7-dimethoxy-3-methyl-3,4-dihydroisoquinoline (DIQ) was investigated as a biological agent. Its potential to affect muscle contractility was predicted through in silico PASS analysis. Based on the in silico analysis, its capabilities were experimentally investigated. The study aimed to investigate the effects of DIQ on the ex vivo spontaneous contractile activity (CA) of smooth muscle (SM) tissue. DIQ was observed to reduce the strength of Ca<sup>2+</sup>-dependent contractions in SM preparations (SMP), possibly by increasing cytosolic Ca<sup>2+</sup> levels through the activation of a voltage-gated L-type Ca<sup>2+</sup> channel. DIQ potently affected calcium currents by modulating the function of muscarinic acetylcholine receptors (mAChRs) and 5-hydroxytryptamine (5-HT) receptors at a concentration of 50 μM. Immunohistochemical tests showed a 47% reduction in 5-HT<sub>2A</sub> and 5-HT<sub>2B</sub> receptor activity in SM cells and neurons in the myenteric plexus (MP), further confirming the effects of DIQ. Furthermore, a significant inhibition of neuronal activity was observed when the compound was co-administered with 5-HT to SM tissues. The conducted experiments confirm the ability of the isoquinoline analog to act as a physiologically active molecule to control muscle contractility and related physiological processes.

MoleculesVol. 29(16)
Plovdiv University (BG), Bulgarian Academy of Sciences (BG), Medical University Plovdiv (BG), Institute of Electronics (BG)
Clean water and sanitation
Openalex Percentile: Top 49%
Chemical synthesis and alkaloids
0.25
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