The Experts below are selected from a list of 51 Experts worldwide ranked by ideXlab platform
Daniel C. Devor - One of the best experts on this subject based on the ideXlab platform.
-
Pharmacological activation of cloned intermediate- and small-conductance Ca2+-activated K+channels
American journal of physiology. Cell physiology, 2000Co-Authors: Colin A. Syme, Aaron C. Gerlach, Ashvani K. Singh, Daniel C. DevorAbstract:We previously characterized 1-ethyl-2-benzimidazolinone (1-EBIO), as well as the clinically useful benzoxazoles, chlorzoxazone (CZ), and Zoxazolamine (ZOX), as pharmacological activators of the int...
Khaled M Houamed - One of the best experts on this subject based on the ideXlab platform.
-
Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds
J Pharmacol Exp Ther, 2001Co-Authors: Yun Dong Cao, J C Dreixler, J D Roizen, M T Roberts, Khaled M HouamedAbstract:Using the patch clamp technique we investigated the effects of the centrally acting muscle relaxant chlorzoxazone and three structurally related compounds, 1-ethyl-2-benzimidazolinone (1-EBIO), Zoxazolamine, and 1,3-dihydro-1-[2-hydroxy-5-(triflu oromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one (NS 1619) on recombinant rat brain SK2 channels (rSK2 channels) expressed in HEK293 mammalian cells. SK channels are small conductance K(+) channels normally activated by a rise in intracellular Ca(2+) concentration; they modulate the electrical excitability in neurons and neuroendocrine cells. When applied externally, chlorzoxazone, 1-EBIO, and Zoxazolamine activated rSK2 channel currents in cells dialyzed with a nominally Ca(2+)-free intracellular solution. The activation was reversible, reproducible, and depended on the chemical structure and concentration. The order of potency was 1-EBIO > chlorzoxazone > Zoxazolamine. Activation of rSK2 channels by chlorzoxazone, 1-EBIO, and Zoxazolamine declined at higher drug concentrations. Zoxazolamine, when applied in combination with chlorzoxazone or 1-EBIO, partially inhibited the rSK2 channel current responses, suggesting a partial-agonist mode of action. 1-EBIO failed to activate rSK2 channel currents when applied to excised inside-out membrane patches exposed to a Ca(2+)-free intracellular solution. In contrast, 1-EBIO activated rSK2 currents in a concentration-dependent manner when coapplied to the patches with a solution containing 20 nM free Ca(2+). NS 1619 did not activate rSK2 channel currents; it inhibited rSK2 channel currents activated by the other three test compounds or by high intracellular Ca(2+). We conclude that chlorzoxazone and its derivatives act through a common mechanism to modulate rSK2 channels, and SK channel modulation in the brain may partly underlie the clinical effects of chlorzoxazone.
-
Modulation of Recombinant Small-Conductance Ca21-Activated K1 Channels by the Muscle Relaxant Chlorzoxazone and Structurally Related Compounds
2000Co-Authors: Ying-jun Cao, J C Dreixler, J D Roizen, M T Roberts, Khaled M HouamedAbstract:Using the patch clamp technique we investigated the effects of the centrally acting muscle relaxant chlorzoxazone and three structurally related compounds, 1-ethyl-2-benzimidazolinone (1-EBIO), Zoxazolamine, and 1,3-dihydro-1-[2-hydroxy-5-(triflu oromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one (NS 1619) on recombinant rat brain SK2 channels (rSK2 chan-nels) expressed in HEK293 mammalian cells. SK channels are small conductance K1 channels normally activated by a rise in intracellular Ca21 concentration; they modulate the electrical excitability in neurons and neuroendocrine cells. When applied externally, chlorzoxazone, 1-EBIO, and Zoxazolamine activated rSK2 channel currents in cells dialyzed with a nominally Ca21-free intracellular solution. The activation was reversible, repro-ducible, and depended on the chemical structure and concen
Colin A. Syme - One of the best experts on this subject based on the ideXlab platform.
-
Pharmacological activation of cloned intermediate- and small-conductance Ca2+-activated K+channels
American journal of physiology. Cell physiology, 2000Co-Authors: Colin A. Syme, Aaron C. Gerlach, Ashvani K. Singh, Daniel C. DevorAbstract:We previously characterized 1-ethyl-2-benzimidazolinone (1-EBIO), as well as the clinically useful benzoxazoles, chlorzoxazone (CZ), and Zoxazolamine (ZOX), as pharmacological activators of the int...
K. K. Anand - One of the best experts on this subject based on the ideXlab platform.
-
Hepatoprotective activity of verbenalin on experimental liver damage in rodents
Fitoterapia, 1998Co-Authors: B. Singh, K. K. Anand, Ajit Kumar Saxena, B. K. Chandan, O. P. Suri, K.a. Suri, Naresh Kumar SattiAbstract:The effects of an oral administration of verbenalin were studied for its hepatoprotective activity. Hexobarbitone-induced sleeping time, Zoxazolamine-induced paralysis time, bromosulphalein (BSP) retention, serum levels of transominases, bilirubin and total protein were used as indices of liver injury. A significant hepatoprotective effect was observed as evident from shortened hexobarbitone sleeping time and Zoxazolamine paralysis time in mice which were increased by CCl 4 treatment. Further, pre- and post-treatment with verbenalin reduced plasma BSP in mice, serum transaminases and biliribin in rats in a dose-dependent manner as compared to CCl 4 - treated animals. Verbenalin did not show any sign of toxicity and the minimum lethal dose was greater than 3.0 g/kg when given orally or intraperitoneally in mice.
-
Hepatoprotective studies of a fraction from the fruits of Terminalia belerica Roxb. on experimental liver injury in rodents
Phytotherapy Research, 1994Co-Authors: K. K. Anand, B. B. Singh, Ajit Kumar Saxena, B. K. Chandan, V. N. GuptaAbstract:The effects of an orally administered fraction (TB5) from the fruits of Terminalia belerica in experimental liver injury induced by carbon tetrachloride (CCI4) were studied. Hexobarbitone-induced sleep, Zoxazolamine-induced paralysis, transaminases, bilirubin, total protein in serum and microsomal lipid peroxidation and triglycerides in liver were used as indices of liver injury. A significant hepatoprotective effect was observed as evident from shortened hexobarbitone ‘sleep time’ and Zoxazolamine ‘paralysis time’ when compared with CCI4 alone. Pre- and post-treatment of TB5 reduced, in a dose dependent manner, the elevated levels of serum tranaminases and bilirubin in rats, thus demonstrating its effect both as a prophylactic and curative. Its protective effects on microsomal lipid peroxidation and triglycerides in liver suggest a restorative effect in the process of CCI4-induced liver damage. TB5 did not show any signs of toxicity up to oral doses of 3.2 g/kg in mice.
Aaron C. Gerlach - One of the best experts on this subject based on the ideXlab platform.
-
Pharmacological activation of cloned intermediate- and small-conductance Ca2+-activated K+channels
American journal of physiology. Cell physiology, 2000Co-Authors: Colin A. Syme, Aaron C. Gerlach, Ashvani K. Singh, Daniel C. DevorAbstract:We previously characterized 1-ethyl-2-benzimidazolinone (1-EBIO), as well as the clinically useful benzoxazoles, chlorzoxazone (CZ), and Zoxazolamine (ZOX), as pharmacological activators of the int...
