Zolantidine (SK&F 95282) is a potent selective brain‐penetrating histamine H2‐receptor antagonist

@article{Calcutt1988Zolantidine9,
  title={Zolantidine (SK\&F 95282) is a potent selective brain‐penetrating histamine H2‐receptor antagonist},
  author={C. R. Calcutt and Charon Robin Ganellin and Roger Griffiths and B. K. Leigh and Jacqueline Maguire and Robert C. Mitchell and M. E. Mylek and M E Parsons and Ian R. Smith and R. C. Young},
  journal={British Journal of Pharmacology},
  year={1988},
  volume={93}
}
1 The novel benzthiazole derivative zolantidine (SK&F 95282) is a potent antagonist of histamine at H2‐receptors in guinea‐pig atrium and rat uterus. Only apparent pA2 values of 7.46 and 7.26 respectively could be calculated since the slopes of the Schild plots were significantly less than unity. 2 Zolantidine is equally potent as an antagonist at histamine H2‐receptors in guinea‐pig brain. The compound inhibited histamine stimulated adenylate cyclase (pKi 7.3) and dimaprit stimulated adenosine… 

Cardiac and gastric effects of histamine H2 receptor antagonists: no evidence for a correlation between lipophilicity and receptor affinity

Results obtained in this study showed that the discrepancies between gastric and cardiac effects observed for some H2 antagonists are not explained solely by differences in lipophilicity of compounds, and suggests that ionization has a similar influence for all the molecules on the partition between the lipophilic and aqueous phase.

Pharmacological Characterization and Autoradiographic Localization of Histamine H2 Receptors in Human Brain Identified with [125I]Iodoaminopotentidine

The widespread distribution of H2 receptors in the human brain is consistent with the alleged modulatory role of histamine mediated by this subtype of receptor.

Effects of histamine H2 receptor agonists and antagonists on the isolated guinea pig gallbladder

In conclusion, histamine H2 receptors in guinea pig gallbladder resemble those of the heart, as regards their sensitivity to zolantidine and compound SKF 92857, which, by contrast, were unable to antagonize histamine effects at gastric H 2 receptors in different experimental models.

Histamine H2‐like receptors in chick cerebral cortex: effects on cyclic AMP synthesis and characterization by [3H]tiotidine binding

Chick cerebral cortex contains H2‐like HA receptors that are linked to the cAMP‐generating system and are labelled with [3H]tiotidine, a selective H2 antagonist, and it is suggested that the studied receptors represent either an avian‐specific H 2‐like ha receptors or a novel subtype of HA receptors.

Psychomotor stimulant effects of the stereoisomers of chlorpheniramine

  • J. Bergman
  • Biology, Psychology
    Psychopharmacology
  • 2005
These findings suggest that the psychomotor stimulant effects of chlorpheniramine involve actions other than the blockade of histamine H1 or H2 receptors, and possibly mediate behavioral effects common to H1 antagonists and cocaine.
...

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