Disease relevance of KBio2_005243

• In a rat brain tumor model, we infused minoxidil sulfate (MS), a selective K(ATP) channel activator, to obtain sustained, enhanced, and selective drug delivery, including various sized molecules, across the BTB to brain tumors [1].

High impact information on KBio2_005243

• Electrophysiological mechanisms of minoxidil sulfate-induced vasodilation of rabbit portal vein [2].
• The electrophysiological and mechanical properties of the vasodilator minoxidil sulfate (MNXS) were examined in isolated smooth muscle cells and strips from rabbit portal vein [2].
• Both pinacidil and RP-49,356 induce measurable Rb+ flux in isolated vibrissa follicles and a hair epithelial cell line whereas neither minoxidil nor minoxidil sulfate had measurable effects [3].
• Formation of minoxidil sulfate is catalyzed by specific PAPS-dependent sulfotransferase(s) and minoxidil-sulfating activities have been previously reported to be present in liver and hair follicles [4].
• Assays of minoxidil sulfotransferase activity indicated that vibrissae follicles metabolize minoxidil to minoxidil sulfate [5].

Biological context of KBio2_005243

• Ionic mechanism of minoxidil sulfate-induced shortening of action potential durations in guinea pig ventricular myocytes [6].
• BRL 34915 (IC50 = 4.7 X 10(-8) M), minoxidil sulfate (IC50 = 1.4 X 10(-7) M) and diazoxide (IC50 = 5 X 10(-6) M) elicited concentration-dependent relaxations of the spontaneous, myogenic contractions in venous strips [7].
• Our interest in the sulfation process arose because direct action of minoxidil sulfate had been implicated both in vivo [3,4] and in vitro [5] in blood pressure control processes [8].

Anatomical context of KBio2_005243

• Minoxidil sulfate is the active metabolite that stimulates hair follicles [5].
• Ionic and secretory response of pancreatic islet cells to minoxidil sulfate [9].
• Evidence from contractile, radioisotope ion flux and electrophysiological studies suggest that minoxidil sulfate (MNXS) acts as a K+ channel opener in vascular smooth muscle [10].
• The mechanism of smooth muscle relaxing effect of minoxidil sulfate (MxSO4) was investigated in isolated rabbit superior mesenteric artery [11].
• In isolated rabbit mesenteric artery, the antagonistic effects of U-37883A (0.5-5 microM) were studied against vasorelaxation produced by cromakalim (0.5 microM), minoxidil sulfate (5 microM), pinacidil (1 microM) and RP-49356 (1 microM) [12].

Associations of KBio2_005243 with other chemical compounds

• The KATP antagonism was functionally studied as the inhibition of vasodilation produced by various KATP openers as follows: pinacidil (1 microM), minoxidil sulfate (5 microM), cromakalim (0.5 microM) and RP-49356 (1 microM) [13].
• BRL 34915 [6-cyano-3,4-dihydro-2,2-dimethyl-trans-4-(2-oxo-1-pyrrolidyl) 2H-benzo(b) pyran-3-ol], minoxidil sulfate and diazoxide may relax vascular smooth muscle via hyperpolarization due to an opening of membrane potassium channels [7].
• Further studies demonstrated that PNU-99963 (1) inhibited relaxations by other KATP openers, such as cromakalim (0.5 microM) and minoxidil sulfate (5 microM); (2) was more potent than the other known vascular KATP blockers (glyburide and PNU-37883A); and (3) acted as a KATP blocker in isolated rat aorta as well as dog coronary artery [14].
• Radioactivity which was extracted into ethyl acetate and shown by HPLC to elute with authentic minoxidil sulfate was counted by scintillation counting [15].

Gene context of KBio2_005243

• At least one of the 3 PST-encoding genes is responsible for forming minoxidil sulfate in the lower outer root sheath of anagen hair follicles [16].
• Sulfotransferase activity in platelets from 48 adult males ranged from 0.9-13.2 pmol minoxidil sulfate produced/10(7) platelets per 30 min (mean 4.91 +/- 2.84 pmol/10(7) platelets per 30 min +/- SD) [15].
• Moreover, topical application of 1% minoxidil sulfate to the anterior dorsal skin of rats in telogen stimulated hair growth and increased the mRNA expressions of HGF and MMP-2 [17].
• Minoxidil sulfate and pinacidil, well-known activators of the ATP-sensitive K+ (KATP) channel, induce hair growth in clinical studies [18].

Analytical, diagnostic and therapeutic context of KBio2_005243

• Patch-clamp techniques were used to study pharmacological effects of minoxidil sulfate (MNXS) on the membrane currents of enzymatically isolated guinea pig ventricular myocytes [6].
• In the experiment group, 50 mg/kg/day of minoxidil sulfate was administered by orogastric tube and the same amount of saline solution was administered to the control group [19].

References