Fabad Journal of Pharmaceutical Sciences, cilt.38, sa.2, ss.65-71, 2013 (Scopus)
Overactive bladder (OAB) is a common clinical syndrome with a high prevalence in geriatric population. The main symptoms of OAB such as urgency, frequency and urge incontinence result from detrusor overactivity (DO) , that is due to involuntary contractions of the detrusor smooth muscle (DSM) in the filling phase of micturition. DSM contractility is mainly regulated by cholinergic and nonadrenergic, noncholinergic (NANC) mechanisms via multiple receptors. Acetylcholine (ACh)- induced contractions mediated by M3 muscarinic receptors, adenosine triphosphate (ATP) -induced contractions mediated purinergic ion channel (P2X) receptors and Ca+2 influx are the fundamental contractile mechanisms of DSM, thus dysregulation of these contractile pathways cause DO and OAB. Trimebutine maleate (TMB), a modulator of Ca+2 and K+ channels activity, has been widely prescribed to treat functional gastrointestinal disorders. However, its activity on bladder has not been investigated. To investigate the effects of TMB on rat DSM contractions induced by ACh, by potassium chloride (KCl) and by ATP; we performed in vitro organ bath studies on rat DSM strips. We reported that TMB pretreatment inhibited DSM contractions induced by ACh, KCl, ATP. Our findings suggest that TMB may be a potent inhibitor of DO and an effective drug for OAB.