urethra

Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a K_b value of 2-3 nM higher than in ear artery and aorta with a K_b value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction .

ABT-866 is an α_1A-adrenoceptor agonist and an antagonist at the α_1B- and α_1D-adrenoceptor subtypes. ABT-866 has an EC₅₀ of 0.60 μM for the α_1A in the rabbit urethra. ABT-866 has a pA₂ value of 5.4 for the α_1B in the rat spleen. ABT-866 has a pA₂ value of 6.2 for the α_1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence .

PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.

Upidosin (Standard) (Rec 15/2739 (Standard)) is the analytical standard of Upidosin (HY-106954). This product is intended for research and analytical applications. Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction .

Deacetylmoxisylyte is an orally active metabolite in plasma of the prodrug Moxisylyte. Deacetylmoxisylyte exhibits similar affinity and selectivity for rabbit corpus cavernosum and urethra. Deacetylmoxisylyte has IC₅₀ values of 400 and 1200 nM for alpha-1 and alpha-2 adrenoceptors .