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The human near-term myometrial beta3-adrenoceptor but not the beta2-adrenoceptor is resistant to desensitisation after sustained agonist stimulation


The human near-term myometrial beta3-adrenoceptor but not the beta2-adrenoceptor is resistant to desensitisation after sustained agonist stimulation



British Journal of Pharmacology 141(5): 831-841



ISSN/ISBN: 0007-1188

1 In order to compare the beta2- and beta3-adrenoceptor (beta-AR) desensitisation process in human near-term myometrium, we examined the influence of a pretreatment of myometrial strips with either a beta2- or a beta3-AR agonist (salbutamol or SR 59119A, respectively, both at 10 muM, for 5 and 15 h) on the relaxation and the cyclic adenosine monophosphate (cAMP) production induced by these agonists. 2 To assess some of the mechanisms potentially implicated in the beta-AR desensitisation process, we studied the influence of such treatment on the number of beta2- and beta3-AR binding sites, the beta2- and beta3-AR transcripts expression and the phosphodiesterase 4 (PDE4) activity. 3 Salbutamol, but not SR 59119A, concentration - response curve (CRC) was shifted by a 15 h salbutamol preincubation, with a significant difference in - log EC20 values (6.31 +/- 0.13 vs 5.58 +/- 0.24, for control and 15 h salbutamol pretreatment, respectively, P<0.05). Neither salbutamol nor SR 59119A CRCs were modified after a 15 h preincubation with SR 59119A. 4 A 15 h exposure of myometrial strips to salbutamol significantly reduced the salbutamol-induced (0.60 +/- 0.26 vs 1.54 +/- 0.24 pmol mg-1 protein, P<0.05), but not the SR 59119A-induced, cAMP production. No decrease in cAMP production was observed after a 15 h SR 59119A exposure. 5 A 15 h salbutamol exposure of myometrial strips significantly reduced the beta2- but not the beta3-AR binding site density, whereas no decrease in the number of beta2- and beta3-AR binding sites was observed after a 15 h SR 59119A treatment. 6 Neither PDE4 activity nor the beta2- and beta3-AR mRNA expression levels were affected by salbutamol or SR 59119A treatments. 7 Our results indicate that beta3-AR, but not beta2-AR, are resistant to the agonist-induced desensitisation. In our model, beta2-AR desensitisation is mediated by a decreased number of beta2-AR that was not explained by transcriptional regulation of the receptor.

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Accession: 012657945

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