Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors¶
Smit. (1996). Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proceedings of the National Academy of Sciences.
Cited by¶
1 citation across 1 artifact.
Each citation links to the sentence it supports in the citing article.
Domain-specific¶
- Inverse Agonist
- Cimetidine's suppression of basal gastric-acid secretion via stabilization of the inactive H2 receptor conformation and the antihistamine cetirizine's inverse agonist activity at H1 receptors are the canonical substrate examples
This sourceEvidence that cimetidine and ranitidine act as inverse agonists at histamine H2 receptors with spontaneous agonist-independent activity, upregulating those receptors. The proposal that H2-antagonist-induced receptor upregulation (via inverse agonism) explains the development of tolerance on prolonged clinical use.
Supported in partVerified against the publisher's abstract
“Cimetidine and ranitidine, which both induce H2 receptor upregulation, actually functioned as inverse agonists in those cell lines displaying spontaneous agonist-independent H2 receptor activity.”
- Cimetidine's suppression of basal gastric-acid secretion via stabilization of the inactive H2 receptor conformation and the antihistamine cetirizine's inverse agonist activity at H1 receptors are the canonical substrate examples
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