Literature DB >> 2942013

The influence of guanidino and isothiourea groups in histaminergic compounds on H2-activity.

G J Sterk, H van der Goot, H Timmerman.   

Abstract

Because in some alkylenediisothioureas replacement of one of the isothiourea groups by a guanidino group resulted in a strong increase in agonistic histamine H2-activity, while replacement of the guanidino group of a potent analogue of impromidine by an isothiourea group resulted in a complete loss of histamine H2-activity, it was concluded that guanidino and isothiourea groups are not bio-isosteric for the H2-receptor.

Entities:  

Mesh：

Substances：

Year:  1986        PMID： 2942013     DOI： 10.1007/bf01988004

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


  3 in total

1.  Impromidine (SK&F 92676) is a very potent and specific agonist for histamine H2 receptors.

Authors:  G J Durant; W A Duncan; C R Ganellin; M E Parsons; R C Blakemore; A C Rasmussen
Journal:  Nature       Date:  1978-11-23       Impact factor: 49.962

2.  The effects of stimulants and inhibitors of histamine receptors on acid secretion from guinea pig gastric fundus.

Authors:  M Impicciatore; G Morini; G Bertaccini
Journal:  Eur J Pharmacol       Date:  1978-04-01       Impact factor: 4.432

3.  1980 Award in Medicinal Chemistry: Medicinal chemistry and dynamic structure-activity analysis in the discovery of drugs acting at histamine H2 receptors.

Authors:  R Ganellin
Journal:  J Med Chem       Date:  1981-08       Impact factor: 7.446
  3 in total
  2 in total

1.  H3 receptor assay in electrically-stimulated superfused slices of rat brain cortex; effects of N alpha-alkylated histamines and impromidine analogues.

Authors:  J F van der Werf; G J Bijloo; A van der Vliet; A Bast; H Timmerman
Journal:  Agents Actions       Date:  1987-04

2.  Profiling of histamine H4 receptor agonists in native human monocytes.

Authors:  M Gschwandtner; B Koether; T Werfel; H Stark; R Gutzmer
Journal:  Br J Pharmacol       Date:  2013-09       Impact factor: 8.739
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.