6533b85dfe1ef96bd12be967
RESEARCH PRODUCT
Selective chiral inhibition of Ca2+ entry promoted by bisbenzyltetrahydroisoquinolines in rat uterus.
Julia Pérez-prietoPilar D'oconJairo SaezDiego CortesAna CercósM. Carmen Zafra-poloM. Dolores Ivorrasubject
endocrine systemStereochemistryMuscle RelaxationUterusBiologyOxytocinBenzylisoquinolinesPotassium ChlorideDiltiazemUterine ContractionAlkaloidsmedicineAnimalsheterocyclic compoundsDiltiazemRats WistarPharmacologyPapaverineAlkaloidUterusCalcium Channel BlockersIn vitroRatsmedicine.anatomical_structureOxytocinStereoselectivityFemalemedicine.symptommedicine.drugMuscle contractiondescription
Abstract The effects of diltiazem and six bisbenzyltetrahydroisoquinoline alkaloids (antioquine, 7-O-methylantioquine, dimethylantioquine, monterine, granjine and cordobimine) were studied in rat isolated uterus in order to clarify the mechanisms of their relaxant actions. All the compounds tested completely relaxed KCl-induced contractions and totally or partially inhibited oxytocin-induced rhythmic contractions. Only alkaloids with absolute configurations (1R,1′S or 1R,1′R) acted intracellularly, promoting relaxation of contractile responses induced by oxytocin in a Ca2+-free medium, as does papaverine. Alkaloids of the antioquine series (1S,1′R) selectively inhibited Ca2+ entry. The great rigidity of these structures and their stereoselective action make these alkaloids useful in studies of the conformational features of the Ca2+ channel.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1992-08-25 | European journal of pharmacology |