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α1-adrenoceptor activation induces phosphorylation of β2-adrenoceptors in human prostate tissue
Department of Urology, University of Munich, Munich, Germany.
Department of Urology, University of Munich, Munich, Germany.
Department of Urology, University of Munich, Munich, Germany.
Urological Research Institute, University of San Raffaele, Milan, Italy.
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2011 (English)In: BJU International, ISSN 1464-4096, E-ISSN 1464-410X, Vol. 108, no 6, 922-928 p.Article in journal (Refereed) Published
Abstract [en]


• To test whether β1-adrenoceptor activation leads to phosphorylation of the β2-adrenoceptor in human prostate tissue.


• Prostate tissue from patients undergoing radical prostatectomy was stimulated in vitro with the α1-adrenergic agonist phenylephrine (10 µM).

• α2-adrenoceptor phosphorylation at serines 345/346 was studied using Western blot analysis with a phospho-specific antibody.

• The role of second messenger kinases was assessed by studying the effects of the protein kinase C (PKC) inhibitor Ro 31-8425 and the protein kinase A (PKA) inhibitor H89 on phenylephrine-induced phosphorylation.

• The expression of G protein-coupled receptor kinases (GRKs) 2/3 was analysed using quantitative reverse-transcriptase-polymerase chain reaction (RT-PCR), Western blot analysis and immunohistochemistry.


• Stimulation of prostate tissue with phenylephrine resulted in phosphorylation of the β2-adrenoceptor (5, 10 and 20 min after stimulation).

• This α1-adrenoceptor-induced phosphorylation of β2-adrenoceptors was resistant to inhibition of PKC and PKA.

• Changes in phosphorylation levels were not attributable to changes in receptor levels, as these remained constant during stimulation.

• RT-PCR and Western blot analysis showed expression of GRK2/3 in human prostate tissues.

• Immunohistochemical staining showed that GRK2/3 expression in human prostate tissue is located to stromal and smooth muscle cells.


• Activation of α1-adrenoceptors causes phosphorylation of β2-adrenoceptors in the human prostate. This may enhance α1-adrenergic contraction and is possibly mediated by GRK2, which is expressed in prostate smooth muscle.

• Mutual regulation between different adrenergic receptors might be involved in the therapeutic effects of α1-blockers in patients with benign prostate hyperplasia.

Place, publisher, year, edition, pages
2011. Vol. 108, no 6, 922-928 p.
Keyword [en]
prostate hyperplasia; lower urinary tract symptoms (LUTS); smooth muscle; alphal-adrenoceptor; alphal-blocker; G protein-coupled receptor kinase (GRK)
National Category
Medical and Health Sciences
URN: urn:nbn:se:liu:diva-77364DOI: 10.1111/j.1464-410X.2010.10021.xPubMedID: 21371241OAI: diva2:526548
Available from: 2012-05-14 Created: 2012-05-14 Last updated: 2012-08-17

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