Methacholine

Cholinergic Receptor Agonist — VARIOUS

Key facts

Methacholine is an ofp drug in the Cholinergic Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1986. Its mechanism of action is classified as Cholinergic Agonists. DrugCentral lists 8 molecular targets, including CHRM1, Chrm2 and CHRM2. Recorded indications include Diagnostic Test for Asthma.

• Approval status: ofp (first approved 1986 by the FDA).
• Drug class: Cholinergic Receptor Agonist.
• Mechanism of action: Cholinergic Agonists.
• Molecular targets: CHRM1, Chrm2, CHRM2 and Chrm3 (8 listed in DrugCentral).
• Indications: Diagnostic Test for Asthma.
• ATC code: V04CX03 (Other diagnostic agents).
• Molecular formula: C8H18NO2+; molecular weight 160.24 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Diagnostic Test for Asthma

Contraindications (28)

• Anemia
• Anemia due to enzyme deficiency
• Blood coagulation disorder
• Body fluid retention
• Bradycardia
• Breastfeeding (mother)
• Cardiovascular event risk
• Diabetes mellitus
• Disease of liver
• Disorder of cardiovascular system
• Disorder of thyroid gland
• Epilepsy
• Factor II deficiency
• Gastritis
• Gastroesophageal reflux disease
• Gastrointestinal hemorrhage
• Gastrointestinal ulcer
• Hemophilia
• Hepatic failure
• Increased gastric tonus
• Kidney disease
• Nasal polyp
• Peptic ulcer
• Pregnancy, function
• Thrombotic thrombocytopenic purpura
• Thyrotoxicosis
• Urinary tract obstruction
• Vitamin K deficiency

Mechanism & targets

• Mechanism of action (MoA): Cholinergic Agonists
• Established pharmacologic class: Cholinergic Receptor Agonist

Molecular targets (8)

Target	Gene	Action	Activity
Muscarinic acetylcholine receptor M1	CHRM1	unknown	Ki 7.64
Muscarinic acetylcholine receptor M2	Chrm2	unknown	Ki 7.23
Muscarinic acetylcholine receptor M2	CHRM2	unknown	Ki 7.23
Muscarinic acetylcholine receptor M3	Chrm3	agonist	EC50 6.92
Muscarinic acetylcholine receptor M1	Chrm1	agonist	EC50 6.40
Muscarinic acetylcholine receptor M4	Chrm4	unknown	Ki 5.80
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 5.80
Muscarinic acetylcholine receptor M3	CHRM3	agonist	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1986-10-31	FDA	—	METHAPHARM

ATC classification

ATC code	Therapeutic hierarchy
V04CX03	VARIOUS › DIAGNOSTIC AGENTS › OTHER DIAGNOSTIC AGENTS › Other diagnostic agents

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Methacholine is on its molecule page.

• Molecular formula: C₈H₁₈NO₂+
• Molecular weight: 160.24 g/mol
• CAS number: —
• InChIKey: NZWOPGCLSHLLPA-UHFFFAOYSA-N
• PubChem CID: 1993

CC(C[N+](C)(C)C)OC(C)=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Methacholine used for?

DrugCentral lists the following indications for Methacholine: Diagnostic Test for Asthma.

How does Methacholine work?

Methacholine is classified as Cholinergic Agonists; its molecular targets in DrugCentral include CHRM1, Chrm2, CHRM2 and Chrm3 (agonist).

When was Methacholine first approved?

Methacholine was first approved by the FDA in 1986.

What drug class does Methacholine belong to?

Methacholine is in the Cholinergic Receptor Agonist class.

What is the chemical formula of Methacholine?

Methacholine has the molecular formula C8H18NO2+ and a molecular weight of 160.24 g/mol.

Sources

• DrugCentral drug card 1726 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200764 — compound record and bioactivity
• PubChem CID 1993 — chemical identifiers
• DrugBank DB06709 — drug record
• FDA UNII 03V657ZD3V — substance identity
• DailyMed: FDA labels for Methacholine — current prescribing information (label search)
• UniProt P11229 (CHRM1) — target protein
• UniProt P08172 (CHRM2) — target protein
• UniProt P08173 (CHRM4) — target protein
• UniProt P20309 (CHRM3) — target protein

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