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Efficacy of the beta3-adrenergic receptor agonist CL-316243 on experimental bladder hyperreflexia and detrusor instability in the rat.
It is suggested that activating the beta3-adrenergic receptor in rat bladder using CL-316243 may directly inhibit smooth muscle contractility, experimental hyperreflexia and detrusor instability, and be useful for urge urinary incontinence. Expand
Inhibition of cardiac delayed rectifier K+ current by overexpression of the long-QT syndrome HERG G628S mutation in transgenic mice.
The presence of IKr in the adult mouse ventricle is established and the ability of the G628S mutation to exert a dominant negative effect on endogenous IKR in vivo is demonstrated, leading to the expected LQT2 phenotype of prolonged repolarization at the single cell level but not QT prolongation in the intact animal. Expand
Comparison of the potassium channel openers, WAY-133537, ZD6169, and celikalim on isolated bladder tissue and In vivo bladder instability in rat.
In contrast, both WAY-133537 and ZD6169 inhibited bladder hyperactivity at doses that produced minimal changes in both mean arterial blood pressure and heart rate, suggesting that both ways may be useful in the treatment of bladder instability at doses associated with minimal hemodynamic side effects. Expand
Inhibition of guinea pig detrusor contraction by NS-1619 is associated with activation of BKCa and inhibition of calcium currents.
Data indicate that NS-1619 inhibits detrusor smooth muscle contraction in a concentration-dependent manner and that the underlying mechanism of action for this effect involves inhibition of calcium current, and may also include activation of the BKCa channel. Expand
Potassium channel blockers as antiarrhythmic drugs
The rational design of selective blockers of cardiac K channels for development as antiarrhythmic drugs appears to have been relatively successful and continues to show considerable promise as a therapeutic approach. Expand
The etiology of toxic peripheral neuropathies: In vitro effects of acrylamide and 2,5-hexanedione on brain enolase and other glycolytic enzymes
The in vitro effects of the neurotoxic compounds, acrylamide and 2,5-hexanedione, on several glycolytic enzymes including enolase, phosphofructokinase (PFK), glyceraldehyde-3-phosphate dehydrogenaseExpand
Acute administration of 17 beta-estradiol inhibits calcium currents in isolated guinea pig detrusor myocytes.
The combination of effects on peak current amplitude and voltage dependence of current activation produced a significant decrease in the calcium "window current," which was characteristically "N-shaped," and after exposure to 17 beta-estradiol became flattened. Expand
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
A novel series of benzylamine, potassium channel openers (KCOs) is presented as part of the program toward designing new, bladder-selective compounds for the treatment of urge urinary incontinence, with substantial loss of in vitro activity. Expand
Antiarrhythmic peptide has no direct cardiac actions
Aside from a prolongation of time to peak force, in papillary muscle, no biologically significant effects of AAP could be determined in any, preparation, suggesting that its antiarrhythmic effects are not mediated by direct membrane actions. Expand
Inhibitory effects of pimozide on cloned and native voltage-gated potassium channels.
The results suggest that PMZD inhibits certain neuronal Kv channels in heterologous expression systems and in hippocampal neurons, and was less effective on A-type currents, presumably because its ability to block requires a prolonged opening of the K channels. Expand