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L-366,509 is an oxytocin antagonist. | [Uses]
L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists[1]. | [References]
[1] 1- (( (7,7-Dimet hyl-2( S)-(2( S)-amino-4- (met hylsulfonyl) butyramido) bicyclo[2.2.1]- heptan-l( S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor |
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