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Betazole

Betazole structure

CAS No:
105-20-4
Formula:
C5H9N3
Chemical Name:
Betazole
Synonyms:
1H-Pyrazole-3-ethanamine;Pyrazole,3-(2-aminoethyl)-;Pyrazole,3(or 5)-(2-aminoethyl)-;Ametazole;3-(2-Aminoethyl)pyrazole;Betazole;3-Aminoethylpyrazole;2-(1H-Pyrazol-3-yl)ethanamine;2-(1H-Pyrazol-5-yl)ethan-1-amine;2-(1H-Pyrazol-5-yl)ethanamine;2-(1H-Pyrazol-3-yl)ethan-1-amine;706747-90-2
Categories:
Active Pharmaceutical Ingredients > Diagnostic Agents

Description

ChEBI: Pyrazole in which a hydrogen adjacent to one of the nitrogen atoms is substituted by a 2-aminoethyl group. It is a histamine H2-receptor agonist used clinically to test gastric secretory function.

Solid

Betazole is pyrazole in which a hydrogen adjacent to one of the nitrogen atoms is substituted by a 2-aminoethyl group. It is a histamine H2-receptor agonist used clinically to test gastric secretory function. It has a role as a histamine agonist, a diagnostic agent and a gastrointestinal drug. It is a member of pyrazoles and a primary amino compound.|A histamine H2 agonist used clinically to test gastric secretory function.|Betazole is a histamine H2 receptor agonist with diagnostic application. Betazole selectively targets and binds to the H2 receptor, thereby mimicking the effect of histamine on these receptors. This may lead to an increase in gastric secretions. Betazole can be used in gastric function tests.

Betazole Basic Attributes

Molecular Weight：

111.147

Exact Mass：

111.15

EC Number：

203-278-3

UNII：

1C065P542O

DSSTox ID：

DTXSID7022675

NCI Thesaurus Code：

C65258

ATC Code：

V - Various

HScode：

2933199090

Characteristics

PSA：

54.7

XLogP3：

0.1

Appearance：

Solid

Density：

0.9902 (rough estimate)

Melting Point：

<25 °C

Boiling Point：

120.5 °C

Flash Point：

150.3ºC

Refractive Index：

1.4690 (estimate)

Water Solubility：

1.56e+02 g/L

Vapor Pressure：

0.00303mmHg at 25°C

Safety Information

Precautionary statement(s)：

P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, P501

Hazard Statements：

H315

GHS Classification：

|Warning|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Toxicity

Protein Binding：

> 99%

Drug Information

Drug Indication：

For use clinically to test gastric secretory function.

Pharmacology：

Betazole is a histamine H2 agonist used in a test for measuring maximal production of gastric acidity or anacidity. This measurement can be used to diagnose diseases such as Zollinger-Ellison syndrome, whereby the volume of gastric and basal secretions is measured following betazole administration (greater than 60% of the maximal acid secretion following betazole stimulation). In another test, gastritis can be diagnosed given late absence of gastric acid which is unresponsive to betazole stimulation. Betazole can be used as a gastric secretory stimulant instead of histamine with the advantage of not provoking side effects and thus not requiring the use of antihistaminic compounds.

MeSH：

Drugs used for their effects on the gastrointestinal system, as to control gastric acidity, regulate gastrointestinal motility and water flow, and improve digestion. (See all compounds classified as Gastrointestinal Agents.)|Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically. (See all compounds classified as Histamine Agonists.)

Absorption：

Rapid and complete.

Mechanism of Action：

Betazole is a histamine analogue. It produces the same effects as histamine, binding the H2 receptor which is a mediator of gastric acid secretion. This agonist action thereby results in an increase in the volume of gastric acid produced.

MeSH Entry Terms：

Ametazole

Betazole Use and Manufacturing

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:111.15
XLogP3:-0.4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:2
Exact Mass:111.079647300
Monoisotopic Mass:111.079647300
Topological Polar Surface Area:54.7
Heavy Atom Count:8
Complexity:64.7
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes