Literature DB >> 2955678

Are histamine receptors involved in the stimulant activities of thiazolylethylamines supposed as cyclic models of dimaprit?

M Impicciatore, G Morini, M Chiavarini, E Barocelli, F Bordi, P V Plazzi, F Vitali.   

Abstract

A representative group of 2-aminothiazolylethylamine derivatives, in which the gastric acid secretion stimulating S-aminoalkylisothiourea moiety can be recognized, was tested. The quite different responses observed suggest that in vivo but not in vitro some events mimicking an H2-receptor agonist-like activity rather than a direct interaction with H2-receptors could take place. On the basis of structure-activity relationships, it can be speculated that the active conformation of dimaprit is not that resembled by these compounds which have been considered as cyclic models of one of its possible conformations.

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Year:  1987        PMID: 2955678     DOI: 10.1007/bf02074686

Source DB:  PubMed          Journal:  Agents Actions        ISSN: 0065-4299


  6 in total

1.  Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters.

Authors:  J M VAN ROSSUM
Journal:  Arch Int Pharmacodyn Ther       Date:  1963

2.  Chemical differentiation of histamine H1- and H2-receptor agonists.

Authors:  G J Durant; C R Ganellin; M E Parsons
Journal:  J Med Chem       Date:  1975-09       Impact factor: 7.446

3.  Acid secretion by guinea-pig isolated stomach.

Authors:  P Holton; J Spencer
Journal:  J Physiol       Date:  1976-02       Impact factor: 5.182

4.  Pharmacological activities of two new histamine analogs.

Authors:  M Impicciatore; G Morini; M Chiavarini; P V Plazzi; F Bordi; F Vitali
Journal:  Agents Actions       Date:  1986-04

5.  [Imidazole H-2 agonists. Synthesis and activity of 2-(2-amino-4-imidazolyl)ethylamine (2-aminohistamine) dihydrochloride].

Authors:  T Vitali; M Impicciatore; P V Plazzi; F Bordi; M Vitto
Journal:  Farmaco Sci       Date:  1984-01

6.  [Thiazolylalkylamines: synthesis of analogs of imidazolylethylamines and their effect on gastric secretion].

Authors:  T Vitali; M Impicciatore; P V Plazzi; F Bordi; G Morini
Journal:  Farmaco Sci       Date:  1986-06
  6 in total
  1 in total

1.  Potentiation of NF-kappaB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells.

Authors:  N S Holden; W Gong; E M King; M Kaur; M A Giembycz; R Newton
Journal:  Br J Pharmacol       Date:  2007-09-24       Impact factor: 8.739

  1 in total

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