Literature DB >> 1338472

A simple and rapid in vitro test system for the screening of histamine H3 ligands.

R C Vollinga1, O P Zuiderveld, H Scheerens, A Bast, H Timmerman.   

Abstract

A simple and rapid functional test system for the screening of histamine H3 ligands is described. It is based on the inhibitory effect of histamine H3 agonists on electrically-evoked contractile response of isolated guinea pig intestine. Whole jejunum segments are continuously stimulated maximally (15 V) by electrical pulses with a frequency of 0.1 Hz and a duration of 0.5 msec. The resulting twitches are recorded isotonically (1.0 g) and can be completely abolished by atropine (0.1 mcM).

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Year:  1992        PMID： 1338472

Source DB:  PubMed          Journal:  Methods Find Exp Clin Pharmacol        ISSN： 0379-0355


  10 in total

1.  SLATE: a method for the superposition of flexible ligands.

Authors:  J E Mills; I J de Esch; T D Perkins; P M Dean
Journal:  J Comput Aided Mol Des       Date:  2001-01       Impact factor: 3.686

Review 2.  An update on histamine H3 receptors and gastrointestinal functions.

Authors:  G Bertaccini; G Coruzzi
Journal:  Dig Dis Sci       Date:  1995-09       Impact factor: 3.199

3.  Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea-pig ileum: evidence for H3 receptor heterogeneity?

Authors:  E Schlicker; M Kathmann; H Bitschnau; I Marr; S Reidemeister; H Stark; W Schunack
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1996-04       Impact factor: 3.000

4.  Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.

Authors:  R Leurs; M T Tulp; W M Menge; M J Adolfs; O P Zuiderveld; H Timmerman
Journal:  Br J Pharmacol       Date:  1995-10       Impact factor: 8.739

5.  Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain.

Authors:  F P Jansen; T S Wu; H P Voss; H W Steinbusch; R C Vollinga; B Rademaker; A Bast; H Timmerman
Journal:  Br J Pharmacol       Date:  1994-10       Impact factor: 8.739

6.  Novel histamine H3 receptor antagonists: affinities in an H3 receptor binding assay and potencies in two functional H3 receptor models.

Authors:  E Schlicker; M Kathmann; S Reidemeister; H Stark; W Schunack
Journal:  Br J Pharmacol       Date:  1994-08       Impact factor: 8.739

7.  Design, synthesis, and in vitro and in vivo characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H3 receptor antagonists.

Authors:  Marek Staszewski; Anna Stasiak; Tadeusz Karcz; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Katarzyna Kieć-Kononowicz; Rob Leurs; Krzysztof Walczyński
Journal:  Medchemcomm       Date:  2019-01-11       Impact factor: 3.597

8.  Non-imidazole histamine H3 ligands: part V. synthesis and preliminary pharmacological investigation of 1-[2-thiazol-4-yl- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives.

Authors:  Roman Guryn; Marek Staszewski; Krzysztof Walczyński
Journal:  Med Chem Res       Date:  2012-11-29       Impact factor: 1.965

9.  4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H₃ Receptor Antagonist: Further Structure⁻Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation.

Authors:  Beata Olszewska; Anna Stasiak; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Rob Leurs; Krzysztof Walczyński
Journal:  Int J Mol Sci       Date:  2018-04-19       Impact factor: 5.923

10.  Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines.

Authors:  Roman Guryn; Marek Staszewski; Anna Stasiak; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Rob Leurs; Krzysztof Walczyński
Journal:  Molecules       Date:  2018-02-03       Impact factor: 4.411
  10 in total

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