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, Volume 38, Issue 1–2, pp 158–164 | Cite as

Pharmacological profile of new thioperamide derivatives at histamine peripheral H1-, H2-, H3-receptors in guinea-pig

  • E. Barocelli
  • V. Ballabeni
  • A. Caretta
  • F. Bordi
  • C. Silva
  • G. Morini
  • M. Impicciatore
Allergy and Histamine


The recent availability of potent and selective ligands, namely R-(α)-methylhistamine and thioperamide, led to conclusive progresses as regards histamine H3-receptor knowledge. The aim of this work is to investigate byin vitro tests the pharmacological properties of new amino and methyl derivatives of the H3-antagonist thioperamide. Such original compounds, developed by the modulation of the thioperamide imidazolyl moiety, were assayed at guinea-pig ileal contractile H1-, atrial chronotropic H2- and enteric neuronal H3-receptors.

None of the drugs exhibited interaction with H1 or H2 sites. On electrically stimulated ileum, two of the thioperamide methyl derivatives competitively antagonized the inhibitory effect of the H3-agonist R-(α)-methylhistamine. On the basis of the Schild analysis, the more active isomer (compound IV) displayed an affinity at H3-receptors only five times lower than thioperamide. These results could contribute to elucidate further the structural features required to develop potent and selective H3-antagonists. On the other hand, to prove the hypothesized apparent heterogeneity between peripheral and central H3-sites, as emerged by pharmacological and binding studies, autoradiographic investigations are in progress.


Methyl Structural Feature Histamine Ileal Pharmacological Property 
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Copyright information

© Birkhäuser Verlag 1993

Authors and Affiliations

  • E. Barocelli
    • 1
  • V. Ballabeni
    • 1
  • A. Caretta
    • 1
  • F. Bordi
    • 2
  • C. Silva
    • 2
  • G. Morini
    • 3
  • M. Impicciatore
    • 1
  1. 1.Institute of Pharmacology and Pharmacognosy, Department of PharmacyUniversity of ParmaParmaItaly
  2. 2.Institute of Pharmaceutical Chemistry, Department of PharmacyUniversity of ParmaParmaItaly
  3. 3.Institute of Pharmaceutical Technology, Department of PharmacyUniversity of ParmaParmaItaly

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