Synthesis and Biological Evaluation of a Tetrahydroisoquinoline Derivative Possessing Selective β2-Adrenergic Agonist Activity

Peter F. Kador; R. Venkatraman; Dennis R. Feller; Duane D. Miller

doi:10.1021/jm00217a004

Synthesis and Biological Evaluation of a Tetrahydroisoquinoline Derivative Possessing Selective β₂-Adrenergic Agonist Activity

Peter F. Kador, R. Venkatraman, Dennis R. Feller, Duane D. Miller

Pharmaceutical Science

Research output: Contribution to journal › Article › peer-review

Abstract

This paper reports the synthesis of 4-(3,4,5-trimethoxybenzyI)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (2) and 2-(3,4-dihydroxyphenyl)-3-(3,4,5-trimethoxyphenyl)propylamine (3). The biological activity of these agents relative to that of trimetoquinol (1) in guinea pig atria and guinea pig trachea is reported. The relative activities in relaxation of guinea pig trachea is 1 > 2 > 3 while in the chronotropic response in guinea pig atria the relative order of activity is 1 > 3 ≫ 2.

Original language	English (US)
Pages (from-to)	891-894
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	20
Issue number	7
DOIs	https://doi.org/10.1021/jm00217a004
State	Published - Jul 1 1977

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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title = "Synthesis and Biological Evaluation of a Tetrahydroisoquinoline Derivative Possessing Selective β2-Adrenergic Agonist Activity",

abstract = "This paper reports the synthesis of 4-(3,4,5-trimethoxybenzyI)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (2) and 2-(3,4-dihydroxyphenyl)-3-(3,4,5-trimethoxyphenyl)propylamine (3). The biological activity of these agents relative to that of trimetoquinol (1) in guinea pig atria and guinea pig trachea is reported. The relative activities in relaxation of guinea pig trachea is 1 > 2 > 3 while in the chronotropic response in guinea pig atria the relative order of activity is 1 > 3 ≫ 2.",

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AU - Miller, Duane D.

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AB - This paper reports the synthesis of 4-(3,4,5-trimethoxybenzyI)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (2) and 2-(3,4-dihydroxyphenyl)-3-(3,4,5-trimethoxyphenyl)propylamine (3). The biological activity of these agents relative to that of trimetoquinol (1) in guinea pig atria and guinea pig trachea is reported. The relative activities in relaxation of guinea pig trachea is 1 > 2 > 3 while in the chronotropic response in guinea pig atria the relative order of activity is 1 > 3 ≫ 2.

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Synthesis and Biological Evaluation of a Tetrahydroisoquinoline Derivative Possessing Selective β₂-Adrenergic Agonist Activity

Abstract

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