Synthesis and Structure-Activity Relationship of Some New β-Blocking Agents with Possible α-Adrenoreceptor Activity

A series of new phenoxypropanolamines with cyclic guanidine and isothiourea moieties has been prepared and investigated for non‐specific α‐ and α‐adrenoreceptor activity by receptor binding experiments on crude rat brain membrane. Some of them [9a, 10c] possess affinity for both β‐ and α‐adrenorecep...

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Veröffentlicht in:Archiv der Pharmazie (Weinheim) 1990, Vol.323 (7), p.387-391
Hauptverfasser: Bergmann, JáNos, Takács, KáLmáN
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container_title Archiv der Pharmazie (Weinheim)
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creator Bergmann, JáNos
Takács, KáLmáN
description A series of new phenoxypropanolamines with cyclic guanidine and isothiourea moieties has been prepared and investigated for non‐specific α‐ and α‐adrenoreceptor activity by receptor binding experiments on crude rat brain membrane. Some of them [9a, 10c] possess affinity for both β‐ and α‐adrenoreceptors. Synthese und Zusammenhänge zwischen Struktur und Aktivität von einigen neuen β‐Blockern mit potentieller Aktivität gegenüber α‐Adrenorezeptoren Einige neue Phenoxypropanolamine mit zyklischen Guanidin‐ und Isothioharnstoff‐Strukturelementen wurden hergestellt und gegenüber unspezifischen β‐ und α‐Adrenorezeptoren durch Rezeptorbindungsexperimente an Rattenhirn‐Membran Präparaten geprüft. Zwei Derivate [9a, 10c] zeigten Affinität gegenüber beiden Typen von Adrenorezeptoren.
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Pharm. Pharm. Med. Chem</addtitle><description>A series of new phenoxypropanolamines with cyclic guanidine and isothiourea moieties has been prepared and investigated for non‐specific α‐ and α‐adrenoreceptor activity by receptor binding experiments on crude rat brain membrane. Some of them [9a, 10c] possess affinity for both β‐ and α‐adrenoreceptors. Synthese und Zusammenhänge zwischen Struktur und Aktivität von einigen neuen β‐Blockern mit potentieller Aktivität gegenüber α‐Adrenorezeptoren Einige neue Phenoxypropanolamine mit zyklischen Guanidin‐ und Isothioharnstoff‐Strukturelementen wurden hergestellt und gegenüber unspezifischen β‐ und α‐Adrenorezeptoren durch Rezeptorbindungsexperimente an Rattenhirn‐Membran Präparaten geprüft. 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Pharm. Pharm. Med. Chem</addtitle><date>1990</date><risdate>1990</risdate><volume>323</volume><issue>7</issue><spage>387</spage><epage>391</epage><pages>387-391</pages><issn>0365-6233</issn><eissn>1521-4184</eissn><coden>ARPMAS</coden><abstract>A series of new phenoxypropanolamines with cyclic guanidine and isothiourea moieties has been prepared and investigated for non‐specific α‐ and α‐adrenoreceptor activity by receptor binding experiments on crude rat brain membrane. Some of them [9a, 10c] possess affinity for both β‐ and α‐adrenoreceptors. Synthese und Zusammenhänge zwischen Struktur und Aktivität von einigen neuen β‐Blockern mit potentieller Aktivität gegenüber α‐Adrenorezeptoren Einige neue Phenoxypropanolamine mit zyklischen Guanidin‐ und Isothioharnstoff‐Strukturelementen wurden hergestellt und gegenüber unspezifischen β‐ und α‐Adrenorezeptoren durch Rezeptorbindungsexperimente an Rattenhirn‐Membran Präparaten geprüft. 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subjects Adrenergic alpha-Antagonists - chemical synthesis
Adrenergic alpha-Antagonists - pharmacology
Adrenergic beta-Antagonists - chemical synthesis
Adrenergic beta-Antagonists - pharmacology
Animals
Chemical Phenomena
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms
Imidazoles - chemical synthesis
Imidazoles - pharmacology
In Vitro Techniques
Organic chemistry
Preparations and properties
Propanolamines - chemical synthesis
Propanolamines - pharmacology
Rats
Structure-Activity Relationship
Thiourea - analogs & derivatives
title Synthesis and Structure-Activity Relationship of Some New β-Blocking Agents with Possible α-Adrenoreceptor Activity
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