Betahistine

CAS No:
5638-76-6 Category:
  • #LGM Pharma is a Betahistine CAS# 5638-76-6 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 5638-76-6
  • AHFC code: 32:00.0
  • Synonyms:
  • ATC Code: N07CA01
  • Chemical Formula: C32H40BrN5O5
  • Molecular Weight: 136.1943
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB06698
  • SMILES: CNCCC1=CC=CC=N1
  • InChl: UUQMNUMQCIQDMZ-UHFFFAOYSA-N
  • PubChem: 2366
  • IUPAC: methyl[2-(pyridin-2-yl)ethyl]amine

Additional Details

Indication:
Pharmacodynamics:
Betahistine primarily acts as a histamine H1-agonist with 0.07 times the activity of histamine. Stimulating the H1-receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels which results in reduced endolymphatic pressure. Betahistine is believed to act by reducing the asymmetrical functioning of sensory vestibular organs as well as by increasing vestibulocochlear blood flow. Doing so aids in decreasing symptoms of vertigo and balance disorders. Betahistine also acts as a histamine H3-receptor antagonist which causes an increased output of histamine from histaminergic nerve endings which can further increase the direct H1-agonist activity. Furthermore, H3-receptor antagonism increases the levels of neurotransmitters such as serotonin in the brainstem, which inhibits the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms.
Mode of Action:
Metabolism:
Betahistine is metabolized primarily into 2-pyridylacetic acid and is subsequently excreted in the urine.
Toxicity:
Symptoms of overdose (< 640 mg) include mild to moderate nausea, dry mouth, dyspepsia, abdominal pain and somnolence. More serious complications such as convulsions, pulmonary or cardiac complications, may occur with higher intentional overdoses (> 640 mg).
General Reference:
Health Canada
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