Betazole

Not to be confused with Betaxolol, a selective β1-adrenergic receptor antagonist.
Betazole
Names
IUPAC name
2-(1H-pyrazol-5-yl)ethanamine
Identifiers
105-20-4 YesY
ChEBI CHEBI:59170 YesY
ChEMBL ChEMBL1201323 N
ChemSpider 7455 YesY
DrugBank DB00272 YesY
7126
Jmol interactive 3D Image
PubChem 7741
UNII 1C065P542O YesY
Properties
C5H9N3
Molar mass 111.145 g/mol
Pharmacology
ATC code V04CG02
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N verify (what is YesYN ?)
Infobox references

Betazole (also known as ametazole) is a histamine H2 receptor agonist. Betazole hydrochloride is known as gastramine and histalog.

It has been used as a gastric stimulant to test for maximal production of gastric secretion activity.[1] The test can be used in diagnosis of diseases such as Zollinger-Ellison syndrome where there is excess acid production, in this case driven by over production of gastrin. The volume of acid secretion is measured following administration of betazole, diagnosis being secretion greater than 60% of the maximal acid secretion following betazole stimulation. This procedure can lead to complications and should be avoided in subjects with coronary artery disease.[2] It is also used in diagnosis of gastritis in association with a test for secretin activity.

Betazole is used as a stimulant in preference to histamine because of its specificity for the H2 receptor and its advantage of not generating the undesirable side effects that histamine would induce. It therefore does not require concomitant use of antihistaminic compounds to block the actions of histamine at other histamine receptor types.

Its action in stimulating histamine release can be of use when testing the effectiveness of H2 receptor blocking drugs such as nizatidine.[3]

References

  1. Wruble LD Cummins AJ Goldenberg J Schapiro H (1967). "The effect of intravenous histalog on gastric secretion in man". Digestive Diseases and Sciences 12 (11): 1087–1090. doi:10.1007/BF02233873. PMID 6057052.
  2. Stoller JL Holubitsky IB Harrison RC Munro AI (1970). "Complications of the histalog test of gastric acid secretion". Digestive Diseases and Sciences 15 (7): 647–651. doi:10.1007/BF02236024. PMID 4951403.
  3. Hammond JB, Offen WW (1988). "Effect of nizatidine and cimetidine on betazole-stimulated gastric secretion of normal subjects: comparison of effects on acid, water, and pepsin.". Am J Gastroenterol. 83 (1): 32–6. PMID 2892392.
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