Drug intelligence / Profile preview

beta-Isosparteine

Development stage
Discontinued
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
Oral
01

Overview

beta-Isosparteine is a naturally occurring quinolizidine alkaloid found in several Fabaceae species including Lupinus (lupin), Spartium (broom), and Cytisus. It is a C2-symmetrical diastereoisomer of sparteine. Historically it has been used as an oxytocic agent to stimulate uterine contractions and as an anti-arrhythmic agent for cardiac arrhythmias. Its mechanism of action is not fully characterized but may be similar to sparteine—potentially involving sodium channel blockade in cardiac tissue. It has also been studied as a probe for CYP2D6 genotype due to its metabolism by this enzyme[1][2][5][6].

Other names
Isosparteine(-)-beta-Isosparteine7,14-Methano-2H,6H-dipyrido(1,2-a:1',2'-e)(1,5)diazocine, dodecahydro-, (7S-(7alpha,7abeta,14alpha,14abeta))-24915-04-6
02

Targets

SCN5A (Sodium channel protein type 5 subunit alpha)

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