当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Conformational effects on the activity of drugs. 5. Pharmacological properties of 2-(p-nitrophenyl)-4-isopropylmorpholine, a cyclic analog of INPEA.

Conformational effects on the activity of drugs. 5. Pharmacological properties of 2-(p-nitrophenyl)-4-isopropylmorpholine, a cyclic analog of INPEA.

Abstract：

:2-(p-Nitrophenyl)-4-isopropylmorphine (V), an analog of 1-(p-nitrophenyl)-2-isopropylaminoethanol (INPEA, I) in which the OCHCHN chain of I is locked in a morpholine ring, loses the beta-receptor blocking activity of I on various isolated preparations. The same ineffectiveness is observed in the O-methyl (II), N-methyl (III), and N,O-dimethyl analog (IV) of I. However, some other properties which are present in I, such as inhibitory effect on acetylcholine or on 5-HT, intrinsic alpha-sympathomimetic activity, and potentiation of catecholamines, are maintained; this demonstrates a complete dissociation of these effects from beta-receptor blockade. The interactions with the alpha-adrenoceptors and with the uptake mechanism are discussed on the basis of the structure-activity relationship between I and its analogs II-V.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Del Tacca M,Bertelli A,Mazzanti L,Stacchini B,Balsamo A,Crotti P,Macchia B,Macchia F

doi

10.1021/jm00242a016

keywords:

subject

Has Abstract

pub_date

1975-08-01 00:00:00

pages

836-8

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

18

pub_type

杂志文章

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