Suppressive effects of the antiandrogen agent, chlormadinone acetate and the 5alpha-reductase inhibitor, dutasteride on prostate weight and intraprostatic androgen levels in rats.

The objectives of this study were to investigate whether chlormadinone acetate (CMA, Prostal, CAS 302-22-7) more markedly decreased ventral prostate and seminal vesicle weights and exerted more beneficial effects on intraprostatic androgen levels than dutasteride (DUT, CAS 164656-23-9) in rats. Dose-dependent inhibiting effects on prostate and seminal vesicle enlargement were observed after the 14-day administration of CMA (30, 100 mg/kg/day) and DUT (0.3, 1 mg/kg/day).

Phosphodiesterase type 9 (PDE9) in the human lower urinary tract: an immunohistochemical study.

Objectives: To examine the roles of the one of the cyclic guanosine monophosphate (cGMP)-specific phosphodiesterases (PDEs), PDE9, in human lower urinary tract (LUT), we performed immunohistochemistry (IHC) using autopsy specimens. To demonstrate the potential functional differences between PDE5 and PDE9 in human LUT, the localization of PDE5 and PDE9 was also compared using laser-capture microdissection (LCM)/reverse transcriptase-polymerase chain reaction (RT-PCR) method.

Materials And Methods: •  We immunolocalized PDE9 in human bladder (60 cases) and prostate (40) specimens using IHC.

Pharmacological properties of 3-amino-5,6,7,8-tetrahydro-2-[4-[4-(quinolin-2-yl)piperazin-1-yl]butyl]quinazolin-4(3H)-one (TZB-30878), a novel therapeutic agent for diarrhea-predominant irritable bowel syndrome (IBS) and its effects on an experimental IBS model.

3-Amino-5,6,7,8-tetrahydro-2-[4-[4-(quinolin-2-yl)piperazin-1-yl]butyl]quinazolin-4(3H)-one (TZB-30878) is a novel compound with both 5-hydroxytryptamine (5-HT)(1A) agonism and 5-HT(3) antagonism effects. We hypothesized that TZB-30878 might have benefits from these dual effects as a medication for diarrhea-predominant irritable bowel syndrome (d-IBS), and these studies were designed to confirm the pharmacological properties of TZB-30878 and its efficacy in an IBS-like animal model. The binding assays demonstrated that [(3)H]TZB-30878 selectively binds to human 5-HT(1A) and 5-HT(3) receptors, with K(d) values of 0.