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Pharmaceutisch Weekblad

, Volume 12, Issue 6, pp 236–239 | Cite as

New selective histamine H1 agonists

Synthesis and pharmacology
  • J. G. Koper
  • A. Van der Vliet
  • H. Van der Goot
  • H. Timmerman
Articles

Abstract

In this article the synthesis and histaminergic H1 activity of a series of substituted 2-phenylhistamines are described. It appeared that substitution of the phenyl ring of these compounds influences the H1 activity substantially. In general, substitution inpara position causes a decrease in h1 activity. However, in themeta-substituted members both increases and decreases of H1 activity have been observed; thus themeta nitro andmeta methoxy derivatives are four times as potent as the parent 2-phenylhistamine. As far as investigated, neither H1 nor H3 activity could be established.

Keywords

Chemistry, organic Histamine Histamine H1 agonists Histamine H1 antagonists Pharmacology 2-Phenylhistamine Synthesis 

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Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1990

Authors and Affiliations

  • J. G. Koper
    • 1
  • A. Van der Vliet
    • 1
  • H. Van der Goot
    • 1
  • H. Timmerman
    • 1
  1. 1.Department of PharmacochemistryFree UniversityHV Amsterdamthe Netherlands

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