Drug intelligence / Profile preview

methacholine

Development stage
Approved
Lead developer
Methapharm
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Inhalation
01

Overview

Methacholine is a synthetic choline ester and parasympathomimetic bronchoconstrictor used primarily as a diagnostic agent in the methacholine challenge test to assess bronchial airway hyperreactivity, most commonly for diagnosing asthma. It acts as a non-selective muscarinic receptor agonist, stimulating muscarinic receptors (especially M3) on airway smooth muscle to induce bronchoconstriction. Methacholine does not cross the blood–brain barrier due to its quaternary ammonium structure and is relatively resistant to breakdown by acetylcholinesterases. The drug was approved by the FDA in 1986 and is marketed under the brand name Provocholine[1][2][5][8].

Brand names
Provocholine
Other names
methacholine chlorideacetyl-β-methylcholine
02

Targets

CHRM2 (M2)CHRM3 (M3)

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