Estudios sobre estructura-actividad con ligandos del receptor histamina H3

Authors

  • C. R. GANELLIN
  • A. FKYERAT

Abstract

Analogues of thioperamide have been synthesised and tested in vitro on rat cerebral

cortex to explore structure-activity relationships with the intention of designing compounds

which do not possess the thiourea group of thioperamide and which may have improved

brain penetration. Compounds derived from histamine and having an aromatic nitrogencontaining

heterocyc1e on the side-chain amino group have been found to act as H3

-

antagonists. These have served as leads to provide aryloxyethyl- and aryloxypropylimidazoles

which are potent H3 antagonists of histamine.

Structure-activity relationships for agonists are brief1y reviewed. Analogues of the

very potent and selective agonist, imetit (S-[2-imidazol-4-yl)ethyl]isothiourea) have been

studied to explore the transition between agonist, partial agonist and antagonist. The

isosteric isourea is also a potent agonist. N,N' -Dibutyl-[S-[3-(imidazol-4-yl)propyl]isothiourea

is a very potent antagonist having K¡=1.5 nM.

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References

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Published

1995-09-20

How to Cite

1.
GANELLIN CR, FKYERAT A. Estudios sobre estructura-actividad con ligandos del receptor histamina H3. Ars Pharm [Internet]. 1995 Sep. 20 [cited 2024 May 18];36(3):455-68. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/21887

Issue

Vol. 36 No. 3 (1995)

Section

Original Articles

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