Functional Role of <i>β</i>3‐Adrenoreceptors in the Bladder

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<jats:p>The detrusor muscle contains β‐adrenoceptors (β‐AR) and three subtypes, such as β1‐AR, β2‐AR, and β3‐AR, which have been identified in most species. There is a predominant expression of β3‐AR messenger RNA in human bladder tissue when compared with the β1‐AR and β2‐AR subtypes. Moreover, the presence of β1, β2, and β3‐AR in the human urothelium has been identified. It has also been demonstrated in animals that relaxation mediated through βs‐AR is achieved solely by cAMP‐dependent mechanisms in non‐contracted detrusor muscles, whereas in KCl precontracted detrusor muscles, cAMP‐dependent and ‐independent mechanisms by way of calcium‐activated K <jats:sup>+</jats:sup>(BK <jats:sub>Ca</jats:sub>) channels may be involved in β‐adrenergic relaxation. In addition, a recent phase II proof‐of‐concept study using a novel selective β3‐adrenoceptor agonist (YM178) has shown clinical efficacy in the treatment of overactive bladder (OAB) symptoms, suggesting that β3‐AR should be used as a therapeutic target for the treatment of OAB disorders.</jats:p>

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