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1-(alkylamino)isochromans: hypotensives with peripheral and central activities.

Abstract：

:A series of 1-[1-(3,4-dimethoxy-1H-2-benzopyran-1-yl)alkyl]-4-arylpiperazines that shows hypotensive activity in the conscious rat has been investigated. Structure-activity relationships are described. A typical example that was investigated in greater detail is 1-[2-(3,4-dihydro-6,7-dimethoxy-1H-2-benzopyran-1-yl)ethyl]-4-(4-fluorophenyl)piperazine. This compound decreases sympathetic nerve activity recorded from the external carotid and splanchnic nerves of baroreceptor-denervated cats and, therefore, has a central component to its mechanism of action. It also blocks pressor effects of norepinephrine and phenylephrine and is thus an alpha-adrenergic antagonist. Binding data characterize this as alpha 1-adrenergic receptor blockade.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

McCall JM,McCall RB,TenBrink RE,Kamdar BV,Humphrey SJ,Sethy VH,Harris DW,Daenzer C

doi

10.1021/jm00343a015

subject

Has Abstract

pub_date

1982-01-01 00:00:00

pages

75-81

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

25

pub_type

杂志文章

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