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Synthesis and analgesic activity of some 5-(4-hydroxyphenyl)-2-azabicyclo[3.2.1]octanes.

Abstract：

:A representative series of 5-(4-hydroxyphenyl)-2-azabicyclo[3.2.1]octanes was synthesized and evaluated in vitro, as well as in vivo, as potential analgetic agents. In general, moderate to good activity (19 twice as active as morphine) was observed in the phenylquinone writhing assay (PQW), while only marginal activity was detected by the tail-flick method. Compounds 19 and 18, being the most active in the PQW model, also demonstrated weak binding affinity for the opiate receptors labeled by [3H]naloxone in rat brain homogenates.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Ong HH,Anderson VB,Wilker JC,Spaulding TC,Meyerson LR

doi

10.1021/jm00181a005

subject

Has Abstract

pub_date

1980-07-01 00:00:00

pages

726-9

issue

7

eissn

0022-2623

issn

1520-4804

journal_volume

23

pub_type

杂志文章

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