TY - JOUR
T1 - Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?
AU - Bardou, Marc
AU - Rouget, Céline
AU - Breuiller-Fouché, Michèle
AU - Loustalot, Catherine
AU - Naline, Emmanuel
AU - Sagot, Paul
AU - Frydman, René
AU - Morcillo, Esteban J.
AU - Advenier, Charles
AU - Leroy, Marie Josèphe
AU - Morrison, John J.
PY - 2007/6/1
Y1 - 2007/6/1
N2 - 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 β3-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.
AB - 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 β3-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.
UR - http://www.scopus.com/inward/record.url?scp=34548014518&partnerID=8YFLogxK
U2 - 10.1186/1471-2393-7-S1-S14
DO - 10.1186/1471-2393-7-S1-S14
M3 - Article
SN - 1471-2393
VL - 7
JO - BMC Pregnancy and Childbirth
JF - BMC Pregnancy and Childbirth
IS - SUPPL. 1
M1 - S14
ER -
