6533b851fe1ef96bd12a98ca
RESEARCH PRODUCT
Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?
Emmanuel NalineEsteban J. MorcilloC LoustalotJohn J. MorrisonMarie-josèphe LeroyRené FrydmanCéline RougetCéline RougetCéline RougetPaul SagotMarc BardouCharles AdvenierMichèle Breuiller-fouchesubject
Muscle RelaxationMESH : Receptors Adrenergic beta-3MESH : Adrenergic beta-AgonistsUterusAdrenergic beta-3 Receptor AgonistsMESH: Adrenergic beta-AgonistsPharmacologyUterine contractionUterine Contraction0302 clinical medicineMESH: PregnancyMESH : UterusPregnancyObstetrics and GynaecologyMedicineMESH : FemaleMESH: Obstetric Labor Premature[ SDV.MHEP.GEO ] Life Sciences [q-bio]/Human health and pathology/Gynecology and obstetricsreproductive and urinary physiology0303 health sciencesMESH : MyometriumMyometriumMESH : Obstetric Labor PrematureObstetrics and GynecologyAdrenergic beta-Agonists3. Good healthmedicine.anatomical_structureMuscle relaxation030220 oncology & carcinogenesisTocolyticMESH: Uterine ContractionMyometriumMESH: MyometriumMESH: UterusFemalemedicine.symptomTocolytic agentmedicine.medical_specialtyAdrenergic receptorAdrenergic beta-3 Receptor Agonists[SDV.MHEP.GEO]Life Sciences [q-bio]/Human health and pathology/Gynecology and obstetricsMESH : Muscle Relaxation03 medical and health sciencesObstetric Labor PrematureInternal medicineHumans030304 developmental biologyMESH: Humansbusiness.industryMESH : HumansUterus[SDV.MHEP.GEO] Life Sciences [q-bio]/Human health and pathology/Gynecology and obstetricsMESH : PregnancyEndocrinologyProceedingsReceptors Adrenergic beta-3MESH: Muscle RelaxationbusinessMESH: Receptors Adrenergic beta-3MESH: FemaleMESH : Uterine Contractiondescription
International audience; The management of premature birth still remains unsatisfactory. Since the relative lack of efficiency and/or safety of current tocolytic agents have been highlighted, it is necessary to develop new uterorelaxant drugs deprived of important maternal and foetal side effects. Our work reported in this review focuses on a potential new target for tocolytic drugs, the beta3-adrenoceptor (ADRB3). This third type of ADRB is shown to be present and functional in human myometrium. We demonstrated that ADRB3 agonists are able to inhibit in-vitro spontaneous contractions of myometrial strips, via a cyclic AMP-mediated pathway. Furthermore, we established that ADRB3 is the predominant subtype over the ADRB2 in human myometrium and that its expression is increased in near-term myometrium, compared to non-pregnant myometrium. Finally, we reported that contrary to ADRB2, the human myometrial ADRB3 is resistant to long-term agonist-induced desensitisation. These compelling data confirm the clinical potential interest of ADRB3 agonists in the pharmacological management of preterm labour.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2007-06-01 |