Drug intelligence / Profile preview

tubocurarine

Development stage
Unknown
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Tubocurarine is a naturally occurring benzylisoquinoline alkaloid and the principal active component of curare, historically used as an arrow poison. It was first isolated in 1935 and became the prototypical non-depolarizing neuromuscular blocking agent for use during surgery to induce skeletal muscle relaxation, particularly in abdominal procedures. Tubocurarine acts as a competitive antagonist at post-synaptic nicotinic acetylcholine receptors (nAChRs) at the neuromuscular junction, preventing acetylcholine from activating these receptors and thereby inhibiting depolarization and muscle contraction. This blockade is reversible by increasing acetylcholine concentrations (e.g., with anticholinesterases like neostigmine). Due to its relatively long duration of action (30–60 minutes) and significant side effects, it has been largely replaced by safer agents such as rocuronium or atracurium. Tubocurarine is rarely used clinically today but remains important in pharmacological research[1][2][3][4][6].

Brand names
Tubocurarine chloride
Other names
tubocurarin(+)-tubocurarine
02

Targets

Glycine receptorMuscle-type nicotinic acetylcholine receptorHTR3A (5-hydroxytryptamine receptor 3A)

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