Vasorelaxant effect of the potassium channel activator, RWJ 29009, is tissue selective

Pharmacological basis for the medicinal use of <i>Morus alba</i> in gut and airways disorders

“…Tissue selective behavior of M. alba could be due to K + gates activating component(s), as KATP channels are known to be heterogeneous (Rudy, 1988;Aguilar-Bryan et al, 1998;Jenkinson, 2006) and some KATP channel openers are tissue selective. For example, a second generation KATP channel activator, rilmakalim is bronchial smooth muscle selective, while most of the first generation molecules, such as lemakalim and bimakalim seem to exhibit a greater potency in the vasculature (Weston and Edwards, 1992;Jacoby et al, 1993). We have experienced that plants with medicinal use in the overactive airways disorders, usually possess PDE inhibitory effect, co-exist with other spasmolytic mechanisms (Shah and Gilani, 2010;Khan et al, 2012b;Rehman et al, 2012).…”

Pharmacology of RWJ 29009, A New Potassium Channel Activator

“…Like other potassium channel activators (8,15,19,20) RWJ 29009 has prominent vasorelaxant effects. It potently relaxes isolated vascular preparations precontracted with a wide variety of vasoconstrictors.…”

“…RWJ 29009 is an effective vasorelaxant in a number of other types of isolated vascular smooth muscle (21). Figure 3 shows that RWJ 29009 relaxes isolated canine circumflex coronary and femoral artery and canine saphenous vein all precontracted with 0.03 phl endothelin-1.…”