A new isoquinolinone derivative with noble vasorelaxation activity

Chia Hsien Lin, Mei Shan Lin, Ying Hsiu Lin, I. Ming Chen, Pen Rong Lin, Chen Yu Cheng, Ming Cheng Tsai

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

The pharmacological effects of BDPBI (7-bromo-1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)2H-isoquinolin-3-one dihydrochloride) were tested on isolated endothelium-containing or denuded aorta of the (guinea pig. BDPBI with the formula C27H24BrCl2N3O was synthesized starting with 3-isochromanone. In the endothelium-containing preparations of the aortic rings, phenylephrine (PHE; 10 μmol/l) elicited contracture and acetylcholine (ACh; 10 μmol/l) or BDPBI (0.01-10 μmol/l) elicited relaxation effects on the PHE-precontracted preparations. The BDPBI-elicited effect on the PHE-precontracted aortic rings was not altered in the presence of adrenergic blockers (propranolol or yohimbine; 1 μmol/l) or pretreated preparations with aspirin, indomethacin (10 μmol/l) or L-NAME (1 mmol/l). However, the relaxation effects of BDPBI were blocked if the preparations were pretreated with diphenhydramine (10 μmol/l) or chloropheniramine maleate (10 μmol/l). In contrast to lower concentrations of atropine (1 μmol/l), higher concentrations of atropine (30 μmol/l) did block the effects of BDPBI on the PHE-precontracted aortic rings. HTMT dimaleate (0.01-10 μmol/l), a histamine H1 receptor agonist, also elicited relaxation effects on the PHE-precontracted preparation, and the effects were blocked if the preparations were pretreated with diphenhydramine or chloropheniramine maleate. On isolated denuded aorta of the guinea pig, BDPBI did not elicit relaxation effects on the PHE-precontracted aortic rings. These results demonstrated that the vasorelaxation effect of BDPBI on PHE-precontracted aortic rings is partly dependent on the activation of a histaminergic receptor from the vascular endothelium. We suggested that BDPBI would be an effective vasorelaxant for cardiovascular systems.

Original languageEnglish
Pages (from-to)202-210
Number of pages9
JournalPharmacology
Volume67
Issue number4
DOIs
Publication statusPublished - Mar 20 2003

Fingerprint

Diphenhydramine
Atropine
Vasodilation
Endothelium
Aorta
Guinea Pigs
Histamine Agonists
Adrenergic Antagonists
Yohimbine
NG-Nitroarginine Methyl Ester
Vascular Endothelium
Contracture
Phenylephrine
Cardiovascular System
Vasodilator Agents
Propranolol
Indomethacin
Aspirin
Acetylcholine
Pharmacology

Keywords

  • Acetylcholine
  • Aorta
  • BDPBI (7-bromo-1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)2H-isoquinolin-3-one dihydrochloride)
  • Endothelium
  • Histamine
  • Smooth muscle
  • Vasorelaxant

ASJC Scopus subject areas

  • Pharmacology

Cite this

Lin, C. H., Lin, M. S., Lin, Y. H., Chen, I. M., Lin, P. R., Cheng, C. Y., & Tsai, M. C. (2003). A new isoquinolinone derivative with noble vasorelaxation activity. Pharmacology, 67(4), 202-210. https://doi.org/10.1159/000068402

A new isoquinolinone derivative with noble vasorelaxation activity. / Lin, Chia Hsien; Lin, Mei Shan; Lin, Ying Hsiu; Chen, I. Ming; Lin, Pen Rong; Cheng, Chen Yu; Tsai, Ming Cheng.

In: Pharmacology, Vol. 67, No. 4, 20.03.2003, p. 202-210.

Research output: Contribution to journalArticle

Lin, CH, Lin, MS, Lin, YH, Chen, IM, Lin, PR, Cheng, CY & Tsai, MC 2003, 'A new isoquinolinone derivative with noble vasorelaxation activity', Pharmacology, vol. 67, no. 4, pp. 202-210. https://doi.org/10.1159/000068402
Lin CH, Lin MS, Lin YH, Chen IM, Lin PR, Cheng CY et al. A new isoquinolinone derivative with noble vasorelaxation activity. Pharmacology. 2003 Mar 20;67(4):202-210. https://doi.org/10.1159/000068402
Lin, Chia Hsien ; Lin, Mei Shan ; Lin, Ying Hsiu ; Chen, I. Ming ; Lin, Pen Rong ; Cheng, Chen Yu ; Tsai, Ming Cheng. / A new isoquinolinone derivative with noble vasorelaxation activity. In: Pharmacology. 2003 ; Vol. 67, No. 4. pp. 202-210.
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N2 - The pharmacological effects of BDPBI (7-bromo-1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)2H-isoquinolin-3-one dihydrochloride) were tested on isolated endothelium-containing or denuded aorta of the (guinea pig. BDPBI with the formula C27H24BrCl2N3O was synthesized starting with 3-isochromanone. In the endothelium-containing preparations of the aortic rings, phenylephrine (PHE; 10 μmol/l) elicited contracture and acetylcholine (ACh; 10 μmol/l) or BDPBI (0.01-10 μmol/l) elicited relaxation effects on the PHE-precontracted preparations. The BDPBI-elicited effect on the PHE-precontracted aortic rings was not altered in the presence of adrenergic blockers (propranolol or yohimbine; 1 μmol/l) or pretreated preparations with aspirin, indomethacin (10 μmol/l) or L-NAME (1 mmol/l). However, the relaxation effects of BDPBI were blocked if the preparations were pretreated with diphenhydramine (10 μmol/l) or chloropheniramine maleate (10 μmol/l). In contrast to lower concentrations of atropine (1 μmol/l), higher concentrations of atropine (30 μmol/l) did block the effects of BDPBI on the PHE-precontracted aortic rings. HTMT dimaleate (0.01-10 μmol/l), a histamine H1 receptor agonist, also elicited relaxation effects on the PHE-precontracted preparation, and the effects were blocked if the preparations were pretreated with diphenhydramine or chloropheniramine maleate. On isolated denuded aorta of the guinea pig, BDPBI did not elicit relaxation effects on the PHE-precontracted aortic rings. These results demonstrated that the vasorelaxation effect of BDPBI on PHE-precontracted aortic rings is partly dependent on the activation of a histaminergic receptor from the vascular endothelium. We suggested that BDPBI would be an effective vasorelaxant for cardiovascular systems.

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KW - Endothelium

KW - Histamine

KW - Smooth muscle

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