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Betazole

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Gastrointestinal system drug Not to be confused with Betaxolol, a selective β1-adrenergic receptor antagonist.
Betazole
Names
IUPAC name 2-(1H-Pyrazol-5-yl)ethan-1-amine
Identifiers
CAS Number
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
DrugBank
ECHA InfoCard 100.002.981 Edit this at Wikidata
IUPHAR/BPS
PubChem CID
UNII
CompTox Dashboard (EPA)
InChI
  • InChI=1S/C5H9N3/c6-3-1-5-2-4-7-8-5/h2,4H,1,3,6H2,(H,7,8)Key: JXDFEQONERDKSS-UHFFFAOYSA-N
  • InChI=1/C5H9N3/c6-3-1-5-2-4-7-8-5/h2,4H,1,3,6H2,(H,7,8)Key: JXDFEQONERDKSS-UHFFFAOYAY
SMILES
  • n1ccc(1)CCN
Properties
Chemical formula C5H9N3
Molar mass 111.145 g/mol
Pharmacology
ATC code V04CG02 (WHO)
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). ☒N verify (what is  ?) Infobox references
Chemical compound

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. 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. 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.

It is used to test the effectiveness of H2 receptor blocking drugs such as nizatidine.

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. S2CID 8990827.
  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. S2CID 37678802.
  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.
Histamine receptor modulators
H1
Agonists
Antagonists
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists
See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors
Diagnostic agents (V04)
Digestive system
Diabetes
Fat absorption
Bile duct patency
Liver functional capacity
Gastric secretion
Exocrine pancreatic function
Endocrine system
Pituitary function
Thyroid function
Fertility disturbances
Tuberculosis
Renal function


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